MRTX9768

Names

[ Name ]:
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]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[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

Related Compounds

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