Adagrasib(MRTX849)

Names

[ Name ]:
Adagrasib(MRTX849)

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₅ClFN₇O₂

[ Molecular Weight ]:
604.12

Related Compounds

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