Navlimetostat

Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study[1][2].

Product Specifications

CAS Number

[2630904-45-7]

Product Name Alternative

MRTX-1719; BMS-986504

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mrtx-1719.html

Purity

99.40

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC1=C(C=C(C(C#N)=[C@]1[C@]2=C(C3=CC=C4C(C(CN)=NNC4=O)=C3)C=NN2C)OC5CC5)Cl

Molecular Formula

C23H18ClFN6O2

Molecular Weight

464.88

Precautions

H302, H315, H319

References & Citations

[1]Lars D Engstrom, et al. MRTX1719 is an MTA-cooperative PRMT5 inhibitor that exhibits synthetic lethality in preclinical models and patients with MTAP deleted cancer. Cancer Discov. 2023 Aug 8; CD-23-0669.|[2]Christopher R Smith, et al. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers. J Med Chem. 2022 Feb 10;65 (3) :1749-1766.