MRTX9768

MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor[1].

Product Specifications

CAS Number

[2629314-68-5]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mrtx9768.html

Concentration

10mM

Purity

99.60

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N#CC1=C(C2=C(C3=CC4=C(C(NN=C4CN)=O)C=C3)C=NN2C)C(F)=CC5=C1C=CC=C5

Molecular Formula

C24H17FN6O

Molecular Weight

424.43

References & Citations

[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.|[2]Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252.|[3]Matthew A. Marx, et al. Fragment-based discovery of MRTX9768, a synthetic lethal- based inhibitor designed to bind the PRMT5•MTA complex and selectively target MTAPDEL tumors. AACR ANNUAL MEETING 2021:APRIL 10-15, 2021 AND MAY 17-21, 2021.