BAY-1436032, CAS 1803274-65-8

Formulation: A solid

Formal Name: 2-[[4-(trifluoromethoxy)phenyl]amino]-1-[(1R,5R)-3,3,5-trimethylcyclohexyl]-1H-benzimidazole-5-propanoic acid

Purity: ≥98%

Formula Markup: C26H30F3N3O3

Formula Weight: 489,5

Shelf life (days): 1460

CAS Number: 1803274-65-8

Notes: BAY-1436032 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50 = 0.015 µM for both IDH1R132H and IDH1R132C).{65228} It is selective for mutant IDH1 over wild-type IDH1 and IDH2 (IC50s = 20 and >100 µM, respectively). BAY-1436032 inhibits production of α-hydroxyglutaric acid (2-HG; Item Nos. 25894 / 16374) in HEK293 cells expressing IDH1R132H, IDH1R132C, IDH1R132G, IDH1R132S, and IDH1R132L, but not IDH1R100Q, IDH2R172K, IDH2R172W, or IDH2R172M. It also inhibits 2-HG production in LN-229 glioblastoma and HCT116 colorectal carcinoma cells overexpressing IDH1R132H (IC50s = 73 and 47 nM, respectively), as well as in HT-1080 sarcoma cells endogenously expressing IDH1R132C (IC50 = 135 nM). BAY-1436032 (150 mg/kg) reduces tumor growth and increases survival in an NCH551b IDH1R132H mutant secondary glioblastoma patient-derived xenograft (PDX) mouse model. It also induces myeloid differentiation of IDH1R132C mutant acute myeloid leukemia (AML) cells in mice when administered at doses of 45 and 150 mg/kg.{65229}

• Artikelnummer: CAY35709-500
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 35709-500
• Green Labware: Nein
• Verpackungseinheit: 500 µg
• Mengeneinheit: STK
• Methode: Reinstoffe