Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $714 | Backorder | |
10 mg | $1,140 | Backorder |
Description | MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. 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].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1]. [1]. Christopher R. Smith, et al. Abstract LB003: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors. AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA.[2]. Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252. |
In vitro | MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with significant selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1]. MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. |
In vivo | In xenograft studies, oral administration of MRTX9768 exhibits dose-dependent inhibition of SDMA in MTAP-del tumors, while showing reduced SDMA modulation in bone marrow[1]. |
Cas No. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O: 40 mg/mL (86.79 mM), Sonication is recommended. DMSO: 90 mg/mL (195.27 mM), Sonication is recommended. |
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.