2326521-71-3

2326521-71-3 structure

Name: Adagrasib(MRTX849)
Chemical Name: MRTX849
CAS Number: 2326521-71-3
Molecular Formula: C₃₂H₃₅ClFN₇O₂
Molecular Weight: 604.12
Catalog: Signaling Pathways GPCR/G Protein Ras
Create Date: 2019-12-08 17:21:19
Modify Date: 2024-01-09 19:11:58
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].

Name	MRTX849

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Ras
Target	KRAS G12C[1]
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].
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].
References	[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 phase I/II multiple expansion cohort trial of MRTX849 in patients with advanced solid tumors with KRAS G12C mutation. Journal of Clinical Oncology 2019 37:15_suppl, TPS3161-TPS3161.

Molecular Formula	C₃₂H₃₅ClFN₇O₂
Molecular Weight	604.12