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MRTX849(Adagrasib)

  Cat. No.:  DC26136   Featured
Chemical Structure
2326521-71-3
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More than 5000 active chemicals with high quality for research!
Field of application
MRTX849(Adagrasib) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bou
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2326521-71-3
Chemical Name: 2-((S)-4-(7-(8-chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile
Synonyms: MRTX849,MRTX-849,MRTX 849
SMILES: N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
Formula: C32H35ClFN7O2
M.Wt: 604.12
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Publication: [1]. Christensen JG, et al. The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2019 Oct 28. pii: CD-19-1167. [2]. Kyriakos P. Papadopoulos, et al. A ph
Description: MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction[1][2].
In Vivo: MRTX849 inhibits KRASG12C signaling in cell lines harboring this mutation, and results in tumor regression in a broad spectrum of KRASG12C animal models[2].
In Vitro: In cell lines, MRTX849 inhibits growth and viability of cells harboring KRASG12C mutations, but not in cells with other mutant forms or of wild-type KRAS[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC72237 BI-0474 BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.
DC70234 AZD4625 AZD4625 is a potent, selective, covalent allosteric inhibitor of mutant GTPase KRAS G12C with IC50 of 3 nM, inhibitor H358 cell proliferation with GI50 of 4 nM.AZD4625 is a clinical development candidate for the treatment of KRASG12C positive tumors.
DC26136 MRTX849(Adagrasib) MRTX849(Adagrasib) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bou
DC7344 ZCL 278 ZCL278 is a Cdc42 small molecule modulator that directly binds to Cdc42 (Kd=11.4 uM) and inhibits Cdc42-intersectin interaction.
DC8725 NSC 23766 NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase.
DC7467 ML-098 ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).
DC9906 K-Ras-IN-1 K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.
DC8816 ARS-853 ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.
DC12031 ARS-1630 ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound..
DC10725 ARS-1620 ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.
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