Adagrasib(MRTX849)

Modify Date: 2024-01-09 19:11:58

Adagrasib(MRTX849) Structure
Adagrasib(MRTX849) structure
Common Name Adagrasib(MRTX849)
CAS Number 2326521-71-3 Molecular Weight 604.12
Density N/A Boiling Point N/A
Molecular Formula C32H35ClFN7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Adagrasib(MRTX849)


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].

 Names

Name MRTX849

 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
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
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