PVM/MA
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PVM/MA
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CAS No:
1644545-52-7
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Formula:
C14H13ClF6N6
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Chemical Name:
PVM/MA
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Synonyms:
PF06291874;E-7386;FM381 FM-381;6-(6-chloropyridin-2-yl)-N2,N4-bis((R)-1,1,1-trifluoropropan-2-yl)-1,3,5-triazine-2,4-diamine;PVM/MA;S-N-NITROSO-2-METHYLPIPERIDINE;PCB138/160;FLEABUSTERSRXPOWDER
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CAS No:
Description
Vorasidenib is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity. Upon administration, vorasidenib specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations. In addition, vorasidenib is able to penetrate the blood-brain barrier (BBB). IDH1 and 2, metabolic enzymes that catalyze the conversion of isocitrate into a-KG, play key roles in energy production and are mutated in a variety of cancer cell types. In addition, mutant forms of IDH1 and 2 catalyze the formation of 2HG and drive cancer growth by blocking cellular differentiation and inducing cellular proliferation.
Characteristics
1.491±0.06 g/cm3(Predicted)
467.5±55.0 °C(Predicted)
1.49±0.41(Predicted)
Store at -20°C
Drug Information
1,3,5-Triazine-2,4-diamine, 6-(6-chloro-2-pyridinyl)-N2,N4-bis((1R)-2,2,2-trifluoro-1-methylethyl)-
PVM/MA Use and Manufacturing
PF-06291874 is a novel and potent glucagon receptor antagonist for the potential treatment of diabetes mellitus. PF-06291874, has a lower molcular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing.
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