Page last updated: 2024-11-12

monomethyl auristatin e

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Cross-References

ID SourceID
PubMed CID11542188
CHEMBL ID2103835
SCHEMBL ID5402144
MeSH IDM0479916

Synonyms (39)

Synonym
HY-15162
n-methyl-l-valyl-n-[(3r,4s,5s)-1-{(2s)-2-[(1r,2r)-3-{[(1s,2r)-1-hydroxy-1-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-n-methyl-l-valinamide
DASWEROEPLKSEI-UIJRFTGLSA-N
mmae
474645-27-7
monomethyl auristatin e
mmae peptide
mmae, monomethyl auristatin e
l-valinamide, n-methyl-l-valyl-n-((1s,2r)-4-((2s)-2-((1r,2r)-3-(((1r,2s)-2-hydroxy-1- methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)-1-pyrrolidinyl)-2- methoxy-1-((1s)-1-methylpropyl)-4-oxobutyl)-n-methyl-
n-methyl-l-valyl-n-((1s,2r)-4-((2s)-2-((1r,2r)-3-(((1r,2s)-2-hydroxy-1-methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1s)-1-methylpropyl)-4-oxobutyl)-n-methyl-l-valinamide
n(sup 2)-(n-methyl-l-valyl)-n(sup 1)-((1s,2r)-4-((2s)-2-((1r,2r)-3-(((1r,2s)-2-hydroxy-1-methyl-2- phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1s)- 1-methylpropyl)-4-oxobutyl)-n(sup 1)-methyl-l-valinamide
v7i58rc5ej ,
unii-v7i58rc5ej
CS-0837
CHEMBL2103835
S7721
sgd-1010
monomethylauristatin e [mi]
BP-22278
AKOS025312191
(2s)-n-[(2s)-1-[[(3r,4s,5s)-1-[(2s)-2-[(1r,2r)-3-[[(1s,2r)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamide
SCHEMBL5402144
monomethyl auristatin e (mmae)
4q5 ,
n-methyl-l-valyl-n-[(1s,2r)-4-[(2s)-2-[(1r,2r)-3-[[(1r,2s)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1s)-1-methylpropyl]-4-oxobutyl]-n-methyl-l-valinamide
mfcd22124498
(2s)-n-[(3r,4s,5s)-1-[(2s)-2-[(1r,2r)-2-{[(1s,2r)-1-hydroxy-1-phenylpropan-2-yl]carbamoyl}-1-methoxy-2-methylethyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-n,3-dimethyl-2-[(2s)-3-methyl-2-(methylamino)butanamido]butanamide
(s)-n-((3r,4s,5s)-1-((s)-2-((1r,2r)-3-(((1r,2r)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxohe
mmae (monomethyl auristatin e)
Q6901739
(s)-n-((3r,4s,5s)-1-((s)-2-((1r,2r)-3-(((1s,2r)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-n,3-dimethyl-2-((s)-3-methyl-2-(methylamino)butanamido)butanamide
AMY9235
CCG-270400
nsc-832263
nsc832263
FD9056
nsc791792
nsc-791792
DTXSID101028844

Research Excerpts

Overview

Monomethyl auristatin E (MMAE) is an extremely potent peptide drug. It is currently used in the form of antibody drug conjugates (ADCs) for treating different cancers. MMAE is a potent anti-cancer microtubule-targeting agent (MTA)

ExcerptReferenceRelevance
"Monomethyl auristatin E (MMAE) is a potent tubulin inhibitor that is used as the payload for four FDA-approved antibody-drug conjugates (ADC). "( Payload-Binding Fab Fragments Increase the Therapeutic Index of MMAE Antibody-Drug Conjugates.
Balthasar, JP; Bordeau, BM; Chen, P; Nguyen, TD; Polli, JR, 2023
)
2.35
"Monomethyl auristatin E (MMAE) is a potent anti-cancer microtubule-targeting agent (MTA) used as a payload in three approved MMAE-containing antibody drug conjugates (ADCs) and multiple ADCs in clinical development to treat different types of cancers. "( Microtubule and tubulin binding and regulation of microtubule dynamics by the antibody drug conjugate (ADC) payload, monomethyl auristatin E (MMAE): Mechanistic insights into MMAE ADC peripheral neuropathy.
Azarenko, O; Best, RL; Chih, S; Feinstein, SC; Genualdi, C; Jordan, MA; LaPointe, NE; Miller, H; Shen, BQ; Stagg, NJ; Wilson, L, 2021
)
2.27
"Monomethyl auristatin E (MMAE) is an extremely potent peptide drug that is currently used in the form of antibody drug conjugates (ADCs) for treating different cancers. "( Cyclic RGD-Peptide-Functionalized Polylipopeptide Micelles for Enhanced Loading and Targeted Delivery of Monomethyl Auristatin E.
Deng, C; Qiu, M; Sun, H; Wang, X; Zhang, J; Zhong, Z, 2018
)
2.14

Toxicity

ExcerptReferenceRelevance
" Most common adverse events were infusion-related reaction (22/45; 49%) and fatigue (20/45; 44%)."( A phase 1 study evaluating safety and pharmacokinetics of losatuxizumab vedotin (ABBV-221), an anti-EGFR antibody-drug conjugate carrying monomethyl auristatin E, in patients with solid tumors likely to overexpress EGFR.
Ansell, PJ; Barch, D; Calvo, E; Cleary, JM; Gifford, M; Hu, B; Juric, D; Moreno, V; Ocampo, C; Roberts-Rapp, L; Shapiro, GI; Tolcher, AW; Vanderwal, CA; Xiong, H, 2020
)
0.76
" The most common adverse events were fatigue, nausea, abdominal pain, constipation, blurred vision, diarrhea, and anemia."( An open-label phase I dose-escalation study of the safety and pharmacokinetics of DMUC4064A in patients with platinum-resistant ovarian cancer.
Barroilhet, L; Burris, H; Choeurng, V; Commerford, R; Gutierrez, M; Humke, E; Liu, J; Moore, K; Royer-Joo, S; Vaze, A; Wang, JS; Wang, Y, 2021
)
0.62
" The highest non-severely toxic dose of RC88-ADC was 5 mg/kg in monkeys after repeated dosing."( Preclinical safety profile of RC88-ADC:a novel mesothelin-targeted antibody conjugated with Monomethyl auristatin E.
Jiang, J; Li, S; Tang, N; Wang, L; Xin, W, 2023
)
1.13

Pharmacokinetics

ExcerptReferenceRelevance
" The objective of this work was to build a physiologically based pharmacokinetic (PBPK) model to assess MMAE-drug interactions for vc-MMAE ADCs."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
0.42
" The model was developed using in silico and in vitro data and in vivo pharmacokinetic data from anti-CD22-vc-MMAE ADC."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
0.42
"The pharmacokinetic profile of acMMAE and unconjugated MMAE following administration of anti-CD22-vc-MMAE was well described by simulations using the developed PBPK model."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
0.42
" We developed a mechanism-based platform model that can describe and predict the complex pharmacokinetic (PK) behavior of ADCs with protease-cleavable valine-citrulline (VC) linker linked to Monomethylmonomethyl auristatin F/E by incorporating known mechanisms of ADC disposition."( Development and Translational Application of an Integrated, Mechanistic Model of Antibody-Drug Conjugate Pharmacokinetics.
Carrasco-Triguero, M; Fielder, P; Gadkar, K; Leipold, DD; Lin, K; Milojic-Blair, M; Ramanujan, S; Rubinfeld, B; Saad, OM; Samineni, D; Sukumaran, S; Wang, B; Xu, K; Zhang, C, 2017
)
0.46
" The goal of this analysis was to develop a platform model that simultaneously described antibody-conjugated MMAE (acMMAE) pharmacokinetic (PK) data from eight vc-MMAE ADCs, against different targets and tumor indications; and to assess differences and similarities of model parameters and model predictions, between different compounds."( Platform model describing pharmacokinetic properties of vc-MMAE antibody-drug conjugates.
Agarwal, P; Chen, SC; Fine, BM; Gibiansky, L; Girish, S; Jin, JY; Kågedal, M; Koppada, N; Li, C; Lu, D; Saad, O; Samineni, D; Wang, B; Wang, X; Xu, J, 2017
)
0.46
" Pharmacokinetic analysis of H-Zt/g4-MMAE was determined using hydrophobic interaction chromatography and a MMAE ADC ELISA kit."( Therapeutic efficacy, pharmacokinetic profiles, and toxicological activities of humanized antibody-drug conjugate Zt/g4-MMAE targeting RON receptor tyrosine kinase for cancer therapy.
Chen, LH; Feng, L; Hu, CY; Jun, ES; Kim, SC; Suthe, SR; Tong, XM; Wang, MH; Wang, WL; Weng, TH; Wu, ZG; Yao, HP, 2019
)
0.51
"H-Zt/g4-MMAE is superior in eradication of pancreatic cancer xenografts with favorable pharmacokinetic profiles and manageable toxicological activities."( Therapeutic efficacy, pharmacokinetic profiles, and toxicological activities of humanized antibody-drug conjugate Zt/g4-MMAE targeting RON receptor tyrosine kinase for cancer therapy.
Chen, LH; Feng, L; Hu, CY; Jun, ES; Kim, SC; Suthe, SR; Tong, XM; Wang, MH; Wang, WL; Weng, TH; Wu, ZG; Yao, HP, 2019
)
0.51
" Population pharmacokinetic (PK) and exposure-response models were developed to quantify sources of PK variability and relationships between exposure and safety/efficacy end points in ECHELON-1."( Population Pharmacokinetic Modeling and Exposure-Response Assessment for the Antibody-Drug Conjugate Brentuximab Vedotin in Hodgkin's Lymphoma in the Phase III ECHELON-1 Study.
Collins, GP; Endres, CJ; Gomez-Navarro, J; Mould, DR; Song, G; Suri, A; Venkatakrishnan, K, 2019
)
0.51
" Pharmacokinetic analysis of losatuxizumab vedotin showed exposures appeared to be approximately dose-proportional."( A phase 1 study evaluating safety and pharmacokinetics of losatuxizumab vedotin (ABBV-221), an anti-EGFR antibody-drug conjugate carrying monomethyl auristatin E, in patients with solid tumors likely to overexpress EGFR.
Ansell, PJ; Barch, D; Calvo, E; Cleary, JM; Gifford, M; Hu, B; Juric, D; Moreno, V; Ocampo, C; Roberts-Rapp, L; Shapiro, GI; Tolcher, AW; Vanderwal, CA; Xiong, H, 2020
)
0.76
" For the first time, we developed a physiologically based pharmacokinetic (PBPK) model-based approach to assess CYP3A-mediated drug-drug interaction (DDI) risk for polatuzumab vedotin (Polivy), an anti-CD79b-vc-monomethyl auristatin E (MMAE) antibody-drug conjugate (ADC)."( Physiologically Based Pharmacokinetic Model-Informed Drug Development for Polatuzumab Vedotin: Label for Drug-Drug Interactions Without Dedicated Clinical Trials.
Chen, Y; Ding, H; Girish, S; Jin, J; Li, C; Lu, D; Ma, F; Mao, J; Miles, D; Samineni, D; Shi, R; Wright, M, 2020
)
0.74
" The exposure of acMMAE was dose proportional, with a half-life of ~6 days."( An open-label phase I dose-escalation study of the safety and pharmacokinetics of DMUC4064A in patients with platinum-resistant ovarian cancer.
Barroilhet, L; Burris, H; Choeurng, V; Commerford, R; Gutierrez, M; Humke, E; Liu, J; Moore, K; Royer-Joo, S; Vaze, A; Wang, JS; Wang, Y, 2021
)
0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
" This study evaluated the CYP3A-mediated drug-drug interaction potential of brentuximab vedotin and the excretion of MMAE."( CYP3A-mediated drug-drug interaction potential and excretion of brentuximab vedotin, an antibody-drug conjugate, in patients with CD30-positive hematologic malignancies.
Alley, SC; Chen, R; Cooper, M; Gopal, AK; Goy, A; Grove, LE; Han, TH; Lynch, CM; Matous, JV; O'Connor, OA; Ramchandren, R, 2013
)
0.39
" Therefore, evaluating the drug-drug interaction (DDI) potential associated with MMAE is important in the clinical development of ADCs."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
0.42
" For the first time, we developed a physiologically based pharmacokinetic (PBPK) model-based approach to assess CYP3A-mediated drug-drug interaction (DDI) risk for polatuzumab vedotin (Polivy), an anti-CD79b-vc-monomethyl auristatin E (MMAE) antibody-drug conjugate (ADC)."( Physiologically Based Pharmacokinetic Model-Informed Drug Development for Polatuzumab Vedotin: Label for Drug-Drug Interactions Without Dedicated Clinical Trials.
Chen, Y; Ding, H; Girish, S; Jin, J; Li, C; Lu, D; Ma, F; Mao, J; Miles, D; Samineni, D; Shi, R; Wright, M, 2020
)
0.74

Dosage Studied

ExcerptRelevanceReference
" Glembatumumab vedotin had a relatively short t(1/2) , prompting the evaluation of more frequent dosing schedules."( Glembatumumab vedotin, a conjugate of an anti-glycoprotein non-metastatic melanoma protein B mAb and monomethyl auristatin E for the treatment of melanoma and breast cancer.
Junutula, JR; Naumovski, L, 2010
)
0.58
" Pharmacokinetic data showed approximately dose proportional systemic exposure and a mean plasma half-life of around 4 days, supporting the dosing schedule."( Phase I Study of the Investigational Anti-Guanylyl Cyclase Antibody-Drug Conjugate TAK-264 (MLN0264) in Adult Patients with Advanced Gastrointestinal Malignancies.
Almhanna, K; Cruz, C; Faris, JE; Fasanmade, AA; Jung, J; Kalebic, T; Messersmith, W; Rodon, J; Ryan, DP; Wyant, T, 2016
)
0.43
" Time-dependence of clearance had no effect beyond the first dosing cycle."( Platform model describing pharmacokinetic properties of vc-MMAE antibody-drug conjugates.
Agarwal, P; Chen, SC; Fine, BM; Gibiansky, L; Girish, S; Jin, JY; Kågedal, M; Koppada, N; Li, C; Lu, D; Saad, O; Samineni, D; Wang, B; Wang, X; Xu, J, 2017
)
0.46
" In addition, depatux-m dosing has been limited by corneal side effects common to MMAF conjugates."( Characterization of ABBV-221, a Tumor-Selective EGFR-Targeting Antibody Drug Conjugate.
Benatuil, L; Boghaert, ER; Buchanan, FG; Cao, D; DeVries, PJ; Durbin, KR; Falls, HD; Gan, HK; Hsieh, CM; Loberg, LI; Meulbroek, JA; Mitten, MJ; Mudd, SR; Panchal, SC; Phillips, AC; Ralston, SL; Reilly, EB; Reuter, DR; Scott, AM; Vaidya, KS; Voorbach, MJ, 2018
)
0.48
" This model can be used to inform clinical strategies such as adaptations to dosing regimen and/or treatment duration as well as inform clinical eligibility to reduce the incidence of grade ≥ 2 PN."( Time-to-Event Modeling of Peripheral Neuropathy: Platform Analysis of Eight Valine-Citrulline-Monomethylauristatin E Antibody-Drug Conjugates.
Fine, BM; Gillespie, WR; Girish, S; Jin, JY; Kågedal, M; Li, C; Lu, D; Samineni, D, 2019
)
0.51
" Here, we describe the biodistribution and toxicology assessments in Sprague-Dawley rats after intravenous dosing with the aim of elucidating the relationships between these biological outcomes and the underlying physicochemical properties of non-targeted ADCs."( Reducing the antigen-independent toxicity of antibody-drug conjugates by minimizing their non-specific clearance through PEGylation.
Burke, PJ; Cochran, JH; Lyon, RP; Pittman, PG; Simmons, JK, 2020
)
0.56
"3 mg/kg over 3 h per 21-day cycle, with alternate dosing schedules utilized (2 weeks on/1 week off or weekly) to mitigate infusion reactions."( A phase 1 study evaluating safety and pharmacokinetics of losatuxizumab vedotin (ABBV-221), an anti-EGFR antibody-drug conjugate carrying monomethyl auristatin E, in patients with solid tumors likely to overexpress EGFR.
Ansell, PJ; Barch, D; Calvo, E; Cleary, JM; Gifford, M; Hu, B; Juric, D; Moreno, V; Ocampo, C; Roberts-Rapp, L; Shapiro, GI; Tolcher, AW; Vanderwal, CA; Xiong, H, 2020
)
0.76
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (61)

Assay IDTitleYearJournalArticle
AID768618Antiproliferative activity against human A549 cells after 4 days by XTT assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy.
AID1854921Antitumor activity against KK-LC-1-positive human MKN-45 cells xenografted in male BALB/c nude mouse assessed as tumor volume2022European journal of medicinal chemistry, Nov-05, Volume: 241An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer.
AID1508474Growth inhibition of human SF268 cells after 48 hrs by SRB assay2018Journal of natural products, 03-23, Volume: 81, Issue:3
Antineoplastic Agents. 605. Isoquinstatins.
AID768605Antitumor activity against mouse LLC cells allografted in C57/BL6 mouse assessed as reduction in tumor weight at 0.1 mg/kg, iv administered on day 7, 11 and 14 post transplantation measured on day 20 relative to control2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy.
AID1854901Induction of mitotic arrest in KK-LC-1-positive human NUGC-4 cells xenografted in nude mouse assessed as number of pHH3-positive nuclei in tumor at 4 nmol, iv administered as single dose and measured after 24 hrs by pHH3 immunohistochemical staining metho2022European journal of medicinal chemistry, Nov-05, Volume: 241An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer.
AID1508473Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2018Journal of natural products, 03-23, Volume: 81, Issue:3
Antineoplastic Agents. 605. Isoquinstatins.
AID768606Cytotoxicity against human non-small cell lung cancer cells at 0.5 to 1 nM after 4 days by XTT assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy.
AID1896535Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
AID1508477Growth inhibition of human DU145 cells after 48 hrs by SRB assay2018Journal of natural products, 03-23, Volume: 81, Issue:3
Antineoplastic Agents. 605. Isoquinstatins.
AID1896537Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
AID1171856Apparent intrinsic clearance in human liver hepatocytes at 1 uM2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
AID1501974Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
AID1478513Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Antineoplastic Agents. 603. Quinstatins: Exceptional Cancer Cell Growth Inhibitors.
AID1501972Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
AID1508476Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay2018Journal of natural products, 03-23, Volume: 81, Issue:3
Antineoplastic Agents. 605. Isoquinstatins.
AID1813534Acute toxicity in iv dosed Wistar male rat assessed as maximum non-lethal dose2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1501973Growth inhibition of human SF268 cells after 48 hrs by SRB assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
AID1896534Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
AID1813535Acute toxicity in Wistar rat assessed as decrease in motor activity2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1501971Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
AID1508472Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay2018Journal of natural products, 03-23, Volume: 81, Issue:3
Antineoplastic Agents. 605. Isoquinstatins.
AID1478512Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Antineoplastic Agents. 603. Quinstatins: Exceptional Cancer Cell Growth Inhibitors.
AID1501975Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
AID1813522Cytotoxicity against human 22Rv1 cells expressing PMSA measured using MTT assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1389361Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations.
AID768617Antiproliferative activity against human KB cells after 4 days by XTT assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy.
AID1501976Growth inhibition of human DU145 cells after 48 hrs by SRB assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antineoplastic Agents. 604. The Path of Quinstatin Derivatives to Antibody Drug Conjugates.
AID1389363Permeability of the compound at 200 umol/L after 5 hrs by PAMPA2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations.
AID1854879Cytotoxicity against KK-LC-1-negative human HGC-27 cells incubated for 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer.
AID1478510Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Antineoplastic Agents. 603. Quinstatins: Exceptional Cancer Cell Growth Inhibitors.
AID1171855Apparent intrinsic clearance in human liver microsomes at 1 uM2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
AID1638694Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of an SSTR2-Targeting Maytansinoid Conjugate (PEN-221) with Potent Activity in Vitro and in Vivo.
AID1171852Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
AID1478511Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Antineoplastic Agents. 603. Quinstatins: Exceptional Cancer Cell Growth Inhibitors.
AID1478508Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Antineoplastic Agents. 603. Quinstatins: Exceptional Cancer Cell Growth Inhibitors.
AID1389360Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations.
AID1895044Cytotoxicity against human MES-SA/Dx5 cells assessed as inhibition in cell growth2021Journal of natural products, 05-28, Volume: 84, Issue:5
Spliceostatins and Derivatives: Chemical Syntheses and Biological Properties of Potent Splicing Inhibitors.
AID768616Antiproliferative activity against human MDA-MB-231 cells after 4 days by XTT assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy.
AID1478509Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Antineoplastic Agents. 603. Quinstatins: Exceptional Cancer Cell Growth Inhibitors.
AID1896519Toxicity in CD-1 mouse assessed as body weight loss at 0.4 mg/kg,ip administrated upto 20 days for every 5 days2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
AID1813524Induction of intracellular reactive oxygen species production in human 22Rv1 cells incubated for 1 hr measured at CC50 concentration by amperometric method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1502929Antiproliferative activity against human U87 cells after 72 hrs by MTS assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Cytotoxic Prenylated Stilbenes Isolated from Macaranga tanarius.
AID1813538Acute toxicity in Wistar rat assessed as decrease in porphyrin release from nose mucous membrane at 30 mg/kg, iv2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1896538Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
AID1171853Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
AID1854878Cytotoxicity against KK-LC-1-positive human MKN-45 cells incubated for 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer.
AID1502930Antiproliferative activity against human A549 cells after 72 hrs by MTS assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Cytotoxic Prenylated Stilbenes Isolated from Macaranga tanarius.
AID1896533Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-96 assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
AID1813533Acute toxicity in iv dosed ICR male mouse assessed as maximum non-lethal dose2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1813523Cytotoxicity against human PC-3 cells not expressing PMSA measured using MTT assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1813537Acute toxicity in Wistar rat assessed as decrease in porphyrin release from eye mucous membrane at 30 mg/kg, iv2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1813525Induction of intracellular reactive oxygen species production in human PC-3 cells incubated for 1 hr measured at CC50 concentration by amperometric method2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1895048Cytotoxicity against human MES-SA cells assessed as inhibition in cell growth2021Journal of natural products, 05-28, Volume: 84, Issue:5
Spliceostatins and Derivatives: Chemical Syntheses and Biological Properties of Potent Splicing Inhibitors.
AID1895049Cytotoxicity against HEK293T cells assessed as inhibition in cell growth2021Journal of natural products, 05-28, Volume: 84, Issue:5
Spliceostatins and Derivatives: Chemical Syntheses and Biological Properties of Potent Splicing Inhibitors.
AID1813536Acute toxicity in Wistar rat assessed as damage in liver at 30 mg/kg, iv2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
AID1508475Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay2018Journal of natural products, 03-23, Volume: 81, Issue:3
Antineoplastic Agents. 605. Isoquinstatins.
AID1854877Cytotoxicity against KK-LC-1-positive human NUGC-4 cells incubated for 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Nov-05, Volume: 241An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer.
AID1854918Antitumor activity against KK-LC-1-positive human MKN-45 cells xenografted in male BALB/c nude mouse assessed as reduction in tumor growth2022European journal of medicinal chemistry, Nov-05, Volume: 241An auristatin-based peptide-drug conjugate targeting Kita-Kyushu lung cancer antigen 1 for precision chemoradiotherapy in gastric cancer.
AID1171854Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
AID1389362Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations.
AID1896536Cytotoxicity against human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs in presence of TTR by CellTiter-96 assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (211)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (6.16)29.6817
2010's136 (64.45)24.3611
2020's62 (29.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.15

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.

MetricThis Compound (vs All)
Research Demand Index56.15 (24.57)
Research Supply Index5.42 (2.92)
Research Growth Index5.60 (4.65)
Search Engine Demand Index85.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (4.63%)5.53%
Reviews9 (4.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other197 (91.20%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]