MRTX9768

Modify Date: 2024-01-09 19:08:20

MRTX9768 Structure
MRTX9768 structure
Common Name MRTX9768
CAS Number 2629314-68-5 Molecular Weight 424.43
Density N/A Boiling Point N/A
Molecular Formula C24H17FN6O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MRTX9768


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].

 Names

Name MRTX9768

 MRTX9768 Biological Activity

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.

 Chemical & Physical Properties

Molecular Formula C24H17FN6O
Molecular Weight 424.43