2629314-68-5

2629314-68-5 structure
2629314-68-5 structure
  • Name: MRTX9768
  • Chemical Name: MRTX9768
  • CAS Number: 2629314-68-5
  • Molecular Formula: C24H17FN6O
  • Molecular Weight: 424.43
  • Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
  • Create Date: 2021-09-11 09:27:09
  • Modify Date: 2024-01-09 19:08:20
  • MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors[1].

Name MRTX9768
Description MRTX9768 is a potent, orally active PRMT5 inhibitor. MRTX9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors[1].
Related Catalog
Target

PRMT5[1]

In Vitro MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].
In Vivo In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors[1].
References

[1]. Christopher R. et al. Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr LB003.

Molecular Formula C24H17FN6O
Molecular Weight 424.43