2561529-96-0

2561529-96-0 structure
2561529-96-0 structure
  • Name: MRTX849 acid
  • Chemical Name: MRTX849 acid
  • CAS Number: 2561529-96-0
  • Molecular Formula: C34H37ClFN7O4
  • Molecular Weight: 662.15
  • Catalog: Signaling Pathways GPCR/G Protein Ras
  • Create Date: 2021-10-27 18:49:53
  • Modify Date: 2024-01-12 23:54:02
  • MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].

Name MRTX849 acid
Description MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].
Related Catalog
Target

KRas G12C

In Vitro LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1]. LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1].
References

[1]. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.

Molecular Formula C34H37ClFN7O4
Molecular Weight 662.15
Hazard Codes Xi
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