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| | INDEX NAME NOT YET ASSIGNED Basic information |
| Product Name: | INDEX NAME NOT YET ASSIGNED | | Synonyms: | 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-3-fluoro-1-naphthonitrile;MRTX 9768;SDMA,toxicity,glioblastoma,orally,MRTX9768,low,Inhibitor,hematological,MRTX-9768,MTAP,CDKN2A,MRTX 9768,inhibit,Histone Methyltransferase,anticancer,PRMT5-MTA | | CAS: | 2629314-68-5 | | MF: | C24H17FN6O | | MW: | 424.43 | | EINECS: | | | Product Categories: | | | Mol File: | 2629314-68-5.mol |  |
| | INDEX NAME NOT YET ASSIGNED Chemical Properties |
| density | 1.44±0.1 g/cm3(Predicted) | | storage temp. | -20°C, protect from light | | solubility | DMSO : 30 mg/mL (70.68 mM; ultrasonic and warming and heat to 60°C) | | pka | 11.36±0.40(Predicted) |
| | INDEX NAME NOT YET ASSIGNED Usage And Synthesis |
| Biological Activity | 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].
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 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. |
| | INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials |
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