INDEX NAME NOT YET ASSIGNED manufacturers
- MRTX9768
-
- $338.00 / 1mg
-
2024-11-19
- CAS:2629314-68-5
- Min. Order:
- Purity: 98.48%
- Supply Ability: 10g
|
| | 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) | | form | Solid | | pka | 11.36±0.40(Predicted) | | color | White to light brown |
| | INDEX NAME NOT YET ASSIGNED Usage And Synthesis |
| Uses | MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor[1]. | | 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]. | | in vivo | 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].
MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors (such as glioblastoma)[1][2].
MRTX9768 (PO dose 30 mg/kg in CD-1 mouse and beagle dog, 10 mg/kg in cynomolgus monkey) has a favorable ADME profile (>50% bioavailability in mice and dogs, moderate to high clearance, No changes in RBC parameters when administered well above efficacious concentrations (1000 mg/kg))[3].
MRTX9768 (100 mg/kg, orally, BID, 6/21 days) results in SDMA inhibition maintaining 3 days after dosing is stopped[3].
| | IC 50 | PRMT5 | | 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 |
|