erdafitinib: inhibitor of fibroblast growth factor receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 67462786 |
| CHEMBL ID | 3545376 |
| SCHEMBL ID | 2583760 |
| MeSH ID | M000614131 |
| Synonym |
|---|
| S8401 |
| CS-4988 |
| SCHEMBL2583760 |
| erdafitinib [usan:inn] |
| unii-890e37nhmv |
| erdafitinib [orange book] |
| balversa |
| 1346242-81-6 |
| jnj-42756493 |
| erdafitinib [who-dd] |
| erdafitinib |
| 1,2-ethanediamine, n1-(3,5-dimethoxyphenyl)-n2-(1-methylethyl)-n1-(3-(1-methyl-1h-pyrazol-4-yl)-6-quinoxalinyl)- |
| erdafitinib [mi] |
| erdafitinib [jan] |
| 890E37NHMV , |
| erdafitinib [usan] |
| pan-fgfr tyrosine kinase inhibitor jnj-42756493 |
| erdafitinib [inn] |
| HY-18708 |
| AC-30222 |
| CHEMBL3545376 |
| jnj 42756493 |
| n'-(3,5-dimethoxyphenyl)-n'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-n-propan-2-ylethane-1,2-diamine |
| gtpl9039 |
| compound 4 [wo2011135376] |
| jnj42756493 |
| AKOS030526429 |
| 5sf , |
| n-(3,5-dimethoxyphenyl)-n'-(1-methylethyl)-n-[3-(1-methyl-1h-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine |
| erdafitinib (usan/inn) |
| D10927 |
| balversa (tn) |
| mfcd28502040 |
| A857165 |
| DB12147 |
| n1-(3,5-dimethoxyphenyl)-n2-isopropyl-n1-(3-(1-methyl-1h-pyrazol-4-yl)quinoxalin-6-yl)ethane-1,2-diamine |
| BCP20346 |
| jnj-42756493 (erdafitinib) |
| EX-A2564 |
| erdafitinib; jnj-42756493 |
| AS-35040 |
| Q27077213 |
| SB16854 |
| AMY31119 |
| CCG-269200 |
| nsc781556 |
| nsc-781556 |
| NCGC00475735-01 |
| n-(3,5-dimethoxyphenyl)-n'-(1-methylethyl)-n-[3-(1-methyl-1h-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine;erdafitinib |
| bdbm50525939 |
| DTXSID001027936 |
| erdafitinib(jnj-42756493) |
| compound 4 (wo2011135376) |
| erdafitinibum |
| B0084-470835 |
| n-(3,5-dimethoxyphenyl)-3-(1-methyl-1h-pyrazol-4-yl)-n-{2-[(propan-2-yl)amino]ethyl}quinoxalin-6-amine |
Erdafitinib is an oral, selective pan-FGFR tyrosine kinase inhibitor with activity in FGFR-altered advanced urothelial carcinoma. It is a first-in-class pan inhibitor of fibroblast growth factor receptor 1-4 that has garnered global regulatory approval.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Erdafitinib is the first treatment targeting susceptible fibroblast growth factor receptor (FGFR) genetic alterations in patients with locally advanced or metastatic urothelial carcinoma. " | ( Utility of Kolliphor RH 40 in micellar sensitized fluorescence of the novel tyrosine kinase inhibitor "Erdafitinib": Application to human plasma. Belal, F; El-Enany, N; Elawady, T; Khedr, A, 2022) | 2.38 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Grade 3-4 treatment-emergent adverse events of any causality occurred in 72 (71%) of 101 patients." | ( Efficacy and safety of erdafitinib in patients with locally advanced or metastatic urothelial carcinoma: long-term follow-up of a phase 2 study. Akapame, S; Burgess, EF; Duran, I; Fleming, MT; García-Donas, J; Huddart, RA; Joshi, M; Loriot, Y; Mellado, B; Monga, M; Necchi, A; O'Hagan, A; Park, SH; Rezazadeh Kalebasty, A; Santiago-Walker, AE; Siefker-Radtke, AO; Tagawa, ST; Varlamov, S; Zakharia, Y, 2022) | 1.03 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "A population pharmacokinetic (PK) model was developed using data pooled from 6 clinical studies (3 in healthy volunteers and 3 in cancer patients) to characterize total and free plasma concentrations of erdafitinib following single- and multiple-dose administration, to understand clinically relevant covariates, and to quantify the inter- and intraindividual variability in erdafitinib PK." | ( Population Pharmacokinetics of Total and Free Erdafitinib in Adult Healthy Volunteers and Cancer Patients: Analysis of Phase 1 and Phase 2 Studies. Dosne, AG; Li, LY; Ouellet, D; Perez-Ruixo, JJ; Stuyckens, K; Valade, E, 2020) | 1 |
| "A population pharmacokinetic (PK)-pharmacodynamic (PD) model was developed using data from 345 patients with cancer." | ( Erdafitinib's effect on serum phosphate justifies its pharmacodynamically guided dosing in patients with cancer. Avadhani, A; De Porre, P; Dosne, AG; Faelens, R; Leirens, Q; Li, LY; O'Hagan, A; Ouellet, D; Perez Ruixo, JJ; Poggesi, I; Stuyckens, K; Valade, E, 2022) | 2.16 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Whether such therapies can, and should, be combined with immune checkpoint inhibitors (ICI's) is an area of major research interest." | ( Urothelial carcinoma: the development of FGFR inhibitors in combination with immune checkpoint inhibitors. Galsky, MD; Patel, V; Qin, Q, 2020) | 0.56 |
| " This article describes a physiologically based pharmacokinetic (PBPK) model for erdafitinib to assess the drug-drug interaction (DDI) potential of CYP3A4 and CYP2C9 inhibitors and CYP3A4/CYP2C9 inducers on erdafitinib pharmacokinetics (PK) in patients with cancer exhibiting higher AGP levels and in populations with different CYP2C9 genotypes." | ( Prediction of the drug-drug interaction potential of the α1-acid glycoprotein bound, CYP3A4/CYP2C9 metabolized oncology drug, erdafitinib. De Zwart, L; Goris, I; Jacobs, F; Li, LY; Mamidi, RNVS; Monshouwer, M; Poggesi, I; Scheers, E; Snoeys, J; Verboven, P; Wynant, I, 2021) | 1.05 |
| 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 |
| " Interindividual variability in PK parameters was moderate for oral clearance and central volume of distribution, and large for absorption rate and peripheral volume of distribution." | ( Population Pharmacokinetics of Total and Free Erdafitinib in Adult Healthy Volunteers and Cancer Patients: Analysis of Phase 1 and Phase 2 Studies. Dosne, AG; Li, LY; Ouellet, D; Perez-Ruixo, JJ; Stuyckens, K; Valade, E, 2020) | 0.82 |
Erdafitinib is available in tablet form, and the current recommended daily dosing is 8 mg, with dose escalation to 9 mg after 14 to 21 days of therapy if tolerated. Phosphate is used as a biomarker for erdaf itinib's efficacy and safety.
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 13.1373 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 13.1373 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fibroblast growth factor receptor 4 | Homo sapiens (human) | IC5 (µMol) | 0.0057 | 0.0057 | 0.0057 | 0.0057 | AID1845262 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 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. |
| 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. |
| 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. |
| AID1897369 | Inhibition of FGFR1 (unknown origin) at 10 nM relative to control | |||
| AID1845293 | Inhibition of FGFR1 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1897420 | Induction of apoptosis in human SNU-16 cells assessed as live cells at 100 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 86.36%) | |||
| AID1880030 | Inhibition of FGFR3 K650M mutant (unknown origin) by radiometric kinase activity assay | |||
| AID1897386 | Synergistic antiproliferative activity against human SNU-16 cells assessed as combination index at 3.125 to 100 nM incubated for 72 hrs in presence of vorinostat by Chou-Talalay method | |||
| AID1668202 | Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved f | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10 | Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2. |
| AID1897383 | Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
| AID1897381 | Antiproliferative activity against human KATO III stomach cancer cell line assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
| AID1880035 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1880021 | Inhibition of wild-type FGFR1 (unknown origin) by radiometric kinase activity assay | |||
| AID1897412 | Induction of apoptosis in human SNU-16 cells assessed as live cells at 1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 86.36%) | |||
| AID1717930 | Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1897422 | Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 100 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 5.72%) | |||
| AID1897423 | Induction of apoptosis in human SNU-16 cells assessed as dead cells at 100 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 4.78%) | |||
| AID1897492 | Toxicity in BALB/c nude mouse xenografted with human HCT-116 cells assessed as reduction in body weight at 15 mg/kg/day, po administered for 18 days and measured every 3 days | |||
| AID1880039 | Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1897418 | Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 10 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 5.72%) | |||
| AID1880041 | Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1845295 | Inhibition of FGFR2 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1845262 | Inhibition of FGFR4 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1897461 | Inhibition of FGFR1 phosphorylation in human SNU-16 cells assessed as reduction in pFGFR1 expression incubated for 36 hrs by Western blot analysis | |||
| AID1880036 | Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1897367 | Inhibition of FGFR1 (unknown origin) | |||
| AID1897462 | Inhibition of ERK phosphorylation in human HCT-116 cells assessed as reduction in pERK expression incubated for 36 hrs by Western blot analysis | |||
| AID1897366 | Inhibition of HDAC6 (unknown origin) | |||
| AID1897464 | Inhibition of AKT phosphorylation in human SNU-16 cells assessed as reduction in pAKT expression at 1 to 100 nM incubated for 36 hrs by Western blot analysis | |||
| AID1911602 | Inhibition of FGFR2 (unknown origin) using FLT3 as substrate incubated for 30 mins in presence of ATP by time-resolved fluorescence energy-transfer assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Discovery of 1,6-Naphthyridin-2(1 |
| AID1668211 | Selectivity index, ratio of IC50 for N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells to IC50 for human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 pepti | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10 | Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2. |
| AID1897409 | Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 0.1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.14%) | |||
| AID1897380 | Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
| AID1897413 | Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.14%) | |||
| AID1897368 | Inhibition of FGFR1 (unknown origin) at 100 nM relative to control | |||
| AID1778524 | Inhibition of FGFR1 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1880026 | Inhibition of FGFR2 V564F mutant (unknown origin) by radiometric kinase activity assay | |||
| AID1897374 | Inhibition of HDAC8 (unknown origin) | |||
| AID1778525 | Inhibition of FGFR2 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1897417 | Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 10 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.14%) | |||
| AID1601516 | Inhibition of N-terminal GST-tagged recombinant human FGFR1 (456 to 765 amino acids) incubated for 60 mins by time-resolved fluorescence kinase assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
| AID1911604 | Inhibition of FGFR4 (unknown origin) using FLT3 as substrate incubated for 45 mins in presence of ATP by time-resolved fluorescence energy-transfer assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Discovery of 1,6-Naphthyridin-2(1 |
| AID1601519 | Inhibition of human FGFR4 incubated for 45 mins by time-resolved fluorescence kinase assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
| AID1897415 | Induction of apoptosis in human SNU-16 cells assessed as dead cells at 1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 4.78%) | |||
| AID1845294 | Inhibition of FGFR3 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1880025 | Inhibition of FGFR1 V561M mutant (unknown origin) by radiometric kinase activity assay | |||
| AID1717908 | Hepatic extraction ratio in rat liver microsomes preincubated for 3 mins followed by NADPH addition and measured after 60 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1880024 | Inhibition of wild-type FGFR4 (unknown origin) by radiometric kinase activity assay | |||
| AID1897495 | Toxicity in BALB/c nude mouse xenografted with human SNU-16 cells assessed as reduction in body weight at 15 mg/kg/day, ip administered for 18 days and measured every 3 days | |||
| AID1880028 | Inhibition of FGFR2 N549H mutant (unknown origin) by radiometric kinase activity assay | |||
| AID1897387 | Synergistic antiproliferative activity against human KATO III stomach cancer cell line assessed as combination index at 3.125 to 100 nM incubated for 72 hrs in presence of vorinostat by Chou-Talalay method | |||
| AID1897379 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
| AID1911605 | Inhibition of VEGFR2 (unknown origin) using FLT3 as substrate incubated for 60 mins in presence of ATP by time-resolved fluorescence energy-transfer assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Discovery of 1,6-Naphthyridin-2(1 |
| AID1880034 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1897408 | Induction of apoptosis in human SNU-16 cells assessed as live cells at 0.1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 86.36%) | |||
| AID1897365 | Inhibition of HDAC1 (unknown origin) | |||
| AID1897372 | Inhibition of FGFR4 (unknown origin) | |||
| AID1601518 | Inhibition of N-terminal His6-tagged recombinant human FGFR3 (447 to 761 residues) incubated for 60 mins by time-resolved fluorescence kinase assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
| AID1880040 | Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1880038 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1880027 | Inhibition of FGFR3 V555M mutant (unknown origin) by radiometric kinase activity assay | |||
| AID1601507 | Inhibition of VEGFR2 (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
| AID1897384 | Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
| AID1897385 | Synergistic antiproliferative activity against human HCT-116 cells assessed as combination index at 0.156 to 5 uM incubated for 72 hrs in presence of vorinostat by Chou-Talalay method | |||
| AID1897460 | Inhibition of FGFR1 phosphorylation in human HCT-116 cells assessed as reduction in pFGFR1 expression incubated for 36 hrs by Western blot analysis | |||
| AID1880023 | Inhibition of wild-type FGFR3 (unknown origin) by radiometric kinase activity assay | |||
| AID1897416 | Induction of apoptosis in human SNU-16 cells assessed as live cells at 10 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 86.36%) | |||
| AID1897382 | Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | |||
| AID1897465 | Inhibition of AKT phosphorylation in human HCT-116 cells assessed as reduction in pAKT expression at >10 uM incubated for 36 hrs by Western blot analysis | |||
| AID1897371 | Inhibition of FGFR3 (unknown origin) | |||
| AID1897421 | Induction of apoptosis in human SNU-16 cells assessed as early apoptotic cells at 100 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 3.14%) | |||
| AID1880022 | Inhibition of wild-type FGFR2 (unknown origin) by radiometric kinase activity assay | |||
| AID1911601 | Inhibition of FGFR1 (unknown origin) using FLT3 as substrate incubated for 60 mins in presence of ATP by time-resolved fluorescence energy-transfer assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Discovery of 1,6-Naphthyridin-2(1 |
| AID1897463 | Inhibition of ERK phosphorylation in human SNU-16 cells assessed as reduction in pERK expression incubated for 36 hrs by Western blot analysis | |||
| AID1897411 | Induction of apoptosis in human SNU-16 cells assessed as dead cells at 0.1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 4.78%) | |||
| AID1897370 | Inhibition of FGFR2 (unknown origin) | |||
| AID1897414 | Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 5.72%) | |||
| AID1880037 | Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay | |||
| AID1880029 | Inhibition of FGFR3 K650E mutant (unknown origin) by radiometric kinase activity assay | |||
| AID1778526 | Inhibition of FGFR3 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1897389 | Induction of cell cycle arrest in human SNU-16 cells assessed as accumulation of cells at G0/G1 phase at 0.1 to 100 nM incubated for 24 hrs by PI staining based flow cytometry analysis | |||
| AID1897410 | Induction of apoptosis in human SNU-16 cells assessed as late apoptotic cells at 0.1 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 5.72%) | |||
| AID1897373 | Inhibition of HDAC2 (unknown origin) | |||
| AID1897489 | Antitumor activity against human SNU-16 cells xenografted in BALB/c nude mouse assessed as reduction in tumor growth at 15 mg/kg/day, ip administered for 18 days and measured every 3 days | |||
| AID1897419 | Induction of apoptosis in human SNU-16 cells assessed as dead cells at 10 nM incubated for 72 hrs by annexin-V/FITC propidium iodide staining based flow cytometry analysis (Rvb = 4.78%) | |||
| AID1601517 | Inhibition of human FGFR2 incubated for 30 mins by time-resolved fluorescence kinase assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
| AID1778527 | Inhibition of FGFR4 (unknown origin) | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1668206 | Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence a | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10 | Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2. |
| AID1911603 | Inhibition of FGFR3 (unknown origin) using FLT3 as substrate incubated for 60 mins in presence of ATP by time-resolved fluorescence energy-transfer assay | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Discovery of 1,6-Naphthyridin-2(1 |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 23 (26.14) | 24.3611 |
| 2020's | 65 (73.86) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (63.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 12 (13.64%) | 5.53% |
| Reviews | 26 (29.55%) | 6.00% |
| Case Studies | 9 (10.23%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 41 (46.59%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||