INDEX NAME NOT YET ASSIGNED
- Product Name
- INDEX NAME NOT YET ASSIGNED
- CAS No.
- 2629314-68-5
- Chemical Name
- INDEX NAME NOT YET ASSIGNED
- Synonyms
- MRTX 9768;2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-3-fluoro-1-naphthonitrile;SDMA,toxicity,glioblastoma,orally,MRTX9768,low,Inhibitor,hematological,MRTX-9768,MTAP,CDKN2A,MRTX 9768,inhibit,Histone Methyltransferase,anticancer,PRMT5-MTA
- CBNumber
- CB28992743
- Molecular Formula
- C24H17FN6O
- Formula Weight
- 424.43
- MOL File
- 2629314-68-5.mol
INDEX NAME NOT YET ASSIGNED Property
- 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 Chemical Properties,Usage,Production
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
Raw materials
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