Page last updated: 2024-11-12
verubulin
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
verubulin: antineoplastic; a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11414799 |
| CHEMBL ID | 492399 |
| SCHEMBL ID | 2232326 |
| MeSH ID | M0513767 |
Synonyms (38)
| Synonym |
|---|
| n-(4-methoxyphenyl)-n,2-dimethyl-quinazolin-4-amine |
| verubulin |
| CHEMBL492399 |
| mx-128495 |
| azixa |
| verubulin (usan/inn) |
| D10029 |
| 827031-83-4 |
| mpc 6827 |
| verubulin [usan:inn] |
| unii-x97o9ftb92 |
| x97o9ftb92 , |
| n-(4-methoxyphenyl)-n,2-dimethylquinazolin-4-amine |
| 4-quinazolinamine, n-(4-methoxyphenyl)-n,2-dimethyl- |
| AKOS015994561 |
| verubulin [who-dd] |
| verubulin [usan] |
| verubulin [inn] |
| verubulin, mpc-6827 |
| EE-0048 |
| SCHEMBL2232326 |
| AC-25267 |
| 88U , |
| NCGC00387248-01 |
| FT-0703165 |
| DB05585 |
| BCP09127 |
| mpc-6827 (hydrochloride) |
| SB19790 |
| AMY32185 |
| HY-14907 |
| CS-0003626 |
| nsc-758773 |
| nsc758773 |
| Q27293718 |
| A864363 |
| bdbm50557539 |
| CIB03183 |
Research Excerpts
Overview
Verubulin (MPC-6827) is a microtubule-destabilizing agent that achieves high concentrations in the brain.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Verubulin is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals." | ( A phase 2 trial of verubulin for recurrent glioblastoma: a prospective study by the Brain Tumor Investigational Consortium (BTIC). Chamberlain, MC; Fadul, CE; Grimm, S; Kim, L; Phuphanich, S; Recht, L; Rosenfeld, S; Zhu, JZ, 2014) | 1.45 |
| "Verubulin (MPC-6827) is a microtubule-destabilizing agent that achieves high concentrations in the brain. " | ( Phase I trial of verubulin (MPC-6827) plus carboplatin in patients with relapsed glioblastoma multiforme. Aiken, RD; Akerley, WA; Beelen, AP; Colman, H; De Groot, JF; Evans, BA; Glantz, M; Grossmann, KF; Jensen, RL; Matsuoko, Y; Olsen, JJ; Olson, JJ; Yu, M, 2012) | 2.16 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Close collaboration with cardiology colleagues for early indicators of serious cardiac adverse events will likely minimize toxicity while optimizing the therapeutic potential of VDAs and ultimately enhancing patient outcomes." | ( Cardiovascular toxicity profiles of vascular-disrupting agents. Lenihan, DJ; Subbiah, IM; Tsimberidou, AM, 2011) | 0.37 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (6)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 0.0028 | 0.0000 | 0.5369 | 10.0000 | AID1709289 |
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0056 | 0.0006 | 0.8007 | 8.5000 | AID1709291 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0084 | 0.0000 | 0.4830 | 8.8000 | AID1709290 |
| Tubulin beta-2B chain | Bos taurus (cattle) | IC50 (µMol) | 1.0000 | 0.2500 | 1.8838 | 8.7000 | AID1339685 |
| Similar to alpha-tubulin isoform 1 | Bos taurus (cattle) | IC50 (µMol) | 1.0000 | 0.2500 | 1.8779 | 8.7000 | AID1339685 |
| Similar to alpha-tubulin isoform 1 | Bos taurus (cattle) | IC50 (µMol) | 1.0000 | 0.2500 | 1.8656 | 8.7000 | AID1339685 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (169)
Molecular Functions (39)
Ceullar Components (37)
Bioassays (113)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID414617 | Induction of apoptosis in human T47D cells assessed as G2/M DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1625715 | Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1625734 | Toxicity in mouse xenografted with human H460 cells assessed as mortality at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID414608 | Induction of apoptosis in human T47D cells assessed as G1 phase DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID414621 | AUC (0 to infinity) in C57BL/6 mouse brain at 2.5 mg/kg, iv | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID414610 | Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709295 | Potency index, ratio of IC50 for erlotinib to IC50 for test compound for inhibition of VEGFR2 in human U251 cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1380398 | Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors. |
| AID1709298 | Induction of microtubule depolymerization in rat A10 cells incubated for over night by immunofluorescence method | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1709302 | Resistant index, ratio of IC50 for cytotoxicity against human HeLa cells expressing WT-beta3 to IC50 for cytotoxicity against human HeLa cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1469207 | Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469221 | Inhibition of porcine brain tubulin polymerization measured every 60 secs for 90 mins by DAPI staining based fluorescence assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1709297 | Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID414607 | Induction of apoptosis in human T47D cells assessed as G1 phase DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709301 | Cytotoxicity against human HeLa cells over expressing WT-beta3 assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1625837 | Toxicity in mouse allografted with mouse C26 cells assessed as body weight loss at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID414605 | Induction of apoptosis in human T47D cells assessed as S phase DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709291 | Inhibition of PDGFRbeta in human SH-SY5Y cells preincubated for 60 mins followed by PDGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1709303 | Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1771025 | Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1380399 | Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors. |
| AID1709311 | Antiangiogenic activity in Leghorn chicken fertilized egg chorioallantoic membrane assessed as reduction in VEGF/bFGF stimulated neovascularization after 40 hrs by microscopic based CAM assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1771031 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1709292 | Potency index, ratio of IC50 for sunitinib to IC50 for test compound for inhibition of EGFR in human A431 cell | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1469222 | Inhibition of porcine brain tubulin polymerization at 7.5 uM measured every 60 secs for 90 mins by DAPI staining based fluorescence assay relative to control | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469223 | Antiproliferative activity against HLF after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID414620 | Induction of apoptosis in human Jurkat cells assessed as sub-diploid DNA content at 10 nM after 18 hrs by flow cytometry in presence of caspase inhibitor MX-1013 | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1771038 | Half life in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
| AID1469205 | Growth inhibition of human HCT116 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469262 | Antiproliferative activity against human LO2 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469218 | Growth inhibition of human HepG2/DOX cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469204 | Growth inhibition of human A549 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469210 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1399020 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID1469202 | Selectivity index, ratio of IC50 for human LO2 cells to IC50 for human A549 cells | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1771041 | Intrinsic clearance in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
| AID1469220 | Resistance factor, ratio of IC50 for human HepG2/DOX cells to IC50 for human HepG2 cells | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID414623 | Antitumor activity against human MX1 cells xenografted in Crl:Nu/Nu-nuBR mouse assessed as tumor growth inhibition at 10 mg/kg, iv administered once weekly for 3 weeks | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709294 | Potency index, ratio of IC50 for sunitinib to IC50 for test compound for inhibition of PDGFRbeta in human SH-SY5Y cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID375808 | Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs by HTS assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers. |
| AID473427 | Ratio of AUC in brain to plasma in mouse at 2.5 mg/kg, iv | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring. |
| AID1469263 | Antiproliferative activity against human BJ cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1469208 | Growth inhibition of human LoVo cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1709299 | Ratio of EC50 for induction of microtubule depolymerization in rat A10 cells to IC50 for antiproliferative activity against human MDA-MB-435 cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1380400 | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors. |
| AID414618 | Induction of apoptosis in human T47D cells assessed as G2/M DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID473426 | Inhibition of tubulin polymerization | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring. |
| AID1709305 | Resistant index, ratio of IC50 for cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 cells to IC50 for cytotoxicity against human SK-OV-3 cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1625714 | Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1709310 | Cytotoxicity against human U-251 cells assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1399019 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID414626 | Ratio of AUC (0 to infinity) in C57BL/6 mouse brain to AUC (0 to infinity) in C57BL/6 mouse plasma at 2.5 mg/kg, iv | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1625713 | Antiproliferative activity against human SKOV3 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1399018 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID1469206 | Growth inhibition of human HepG2 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1771032 | Antiproliferative activity against human A549/Taxol cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1771036 | Half life in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
| AID1771034 | Antiproliferative activity against human LCC6MDR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1469264 | Selectivity index, ratio of IC50 for human BJ cells to IC50 for human A549 cells | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID414614 | Growth inhibition of human SNU398 cells after 48 hrs by celltiter assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID414612 | Growth inhibition of human T47D cells after 48 hrs by celltiter assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID473423 | Induction of apoptosis in human T47D cells assessed as caspase activation | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring. |
| AID1399021 | Antiproliferative activity against human RKO cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID414619 | Induction of apoptosis in human Jurkat cells assessed as sub-diploid DNA content at 10 nM after 18 hrs by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709304 | Cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1771026 | Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1625838 | Toxicity in mouse allografted with mouse C26 cells assessed as mortality at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1709309 | Cytotoxicity against human A-431 cells assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1469219 | Resistance factor, ratio of IC50 for human A549/CDDP cells to IC50 for human A549 cells | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1709293 | Potency index, ratio of IC50 for sunitinib to IC50 for test compound for inhibition of VEGFR2 in human U251 cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID414609 | Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1469209 | Growth inhibition of human RKO cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID414624 | Antitumor activity against human MX1 cells xenografted in Crl:Nu/Nu-nuBR mouse assessed as tumor growth inhibition at 5 mg/kg, iv administered once weekly for 3 weeks | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1771037 | Intrinsic clearance in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
| AID1709289 | Inhibition of EGFR in human A431 cells preincubated for 60 mins followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID414611 | Induction of apoptosis in human SNU398 cells assessed as caspase activation after 24 hrs by HTS assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1771059 | Binding affinity to immobilized bovine brain tubulin by SPR assay | |||
| AID1380402 | Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors. |
| AID1771090 | Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID414613 | Growth inhibition of human HCT116 cells after 48 hrs by celltiter assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1469261 | Antimigratory activity against human A549 cells assessed as suppression of wound healing at 4 nM after 24 hrs by phase contrast microscopic method | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID473425 | Selectivity ratio EC50 for human H1299 cells over EC50 for human T47D cells | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring. |
| AID1469203 | Selectivity index, ratio of IC50 for HLF to IC50 for human A549 cells | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1380403 | Inhibition of porcine brain tubulin polymerization measured every 60 secs for 90 mins by DAPI dye based fluorescence assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors. |
| AID1469211 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID414606 | Induction of apoptosis in human T47D cells assessed as S phase DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1771040 | Half life in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
| AID414615 | Induction of apoptosis in human T47D cells assessed as sub-diploid DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID375807 | Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs by HTS assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers. |
| AID1771039 | Intrinsic clearance in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis | |||
| AID1469212 | Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID414625 | AUC (0 to infinity) in C57BL/6 mouse plasma at 2.5 mg/kg, iv | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709290 | Inhibition of VEGFR2 in human U251 cells preincubated for 60 mins followed by VEGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1625809 | Inhibition of porcine brain tubulin polymerization at 10 uM preincubated for 5 mins followed by GTP addition measured every 2 mins by spectrophotometry | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1771028 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1709288 | Potency index, ratio IC50 for erlotinib to IC50 for test compound for antiangiogenic activity in Leghorn chicken fertilized egg chorioallantoic membrane | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID414622 | Antitumor activity against human MX1 cells xenografted in Crl:Nu/Nu-nuBR mouse assessed as tumor growth inhibition at 7.5 mg/kg, iv administered once weekly for 3 weeks | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1771035 | Antiproliferative activity against human MDA-MB-231/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1469217 | Growth inhibition of human A549/CDDP cells after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents. |
| AID1709296 | Potency index, ratio of IC50 for erlotinib to IC50 for test compound for inhibition of PDGFRbeta in human SH-SY5Y cells | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1625733 | Toxicity in mouse xenografted with human H460 cells assessed as body weight loss at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1625716 | Solubility of the compound in 2.5% ethanol/2.5% Tween-80 at 1 mg | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID473424 | Induction of apoptosis in human H1299 cells assessed as caspase activation | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring. |
| AID414616 | Induction of apoptosis in human T47D cells assessed as sub-diploid DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID1709300 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability by Sulforhodamine B assay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1380401 | Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors. |
| AID1399022 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (23)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (13.04) | 29.6817 |
| 2010's | 12 (52.17) | 24.3611 |
| 2020's | 8 (34.78) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 22.21
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (22.21) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (13.04%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 20 (86.96%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||