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

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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)

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Hazard and Precautionary Statements (GHS)

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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

Preparation Products

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INDEX NAME NOT YET ASSIGNED Suppliers

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2629314-68-5, INDEX NAME NOT YET ASSIGNEDRelated Search:

MRTX-849 MRTX0902 MRTX1133 MRTX-1719 MRTX-EX185

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

2629314-68-5

C24H17FN6O