Biological Activity

MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor. MRTX849 (Adagrasib) maximizes inhibition by irreversibly locking the KRAS molecule in its inactive state, thereby preventing tumor cell growth which results in tumor cell death. MRTX849 (Adagrasib) exhibited significantly improved half-life and penetration into the tumor, shutting down KRAS signaling for the entire dosing interval, and showing a higher degree of antitumor activity than previous KRAS mutant-selective inhibitors.

Product Citations

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  iScience. 2023 Jan 28;26(2):106080..

  Global profiling of AMG510 modified proteins identified tumor suppressor KEAP1 as an off-target
  MRTX849 (Adagrasib) purchased from AbMole

Chemical Information

Molecular Weight	604.12
Formula	C32H35ClFN7O2
CAS Number	2326521-71-3
Solubility (25°C)	DMSO ≥ 30 mg/mL
Storage	-20°C, dry, sealed

References

[1] Hallin J, et al. Cancer Discov. The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Pat lents.