BMS-265246

• CAT Number: I004172
• CAS Number: 582315-72-8
• Molecular Formula: C18H17F2N3O2
• Molecular Weight: 345.30
• Purity: ≥95%
• Synonyms: (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
• Target: Cyclin-Dependent Kinases
• Solubility: DMSO 20 mg/ml; Water <1 mg/ml
• Storage: 3 years -20℃ powder
• IC50: 6 nM(for CDK1/cyclin B); 9 nM(for CDK2/cyclin E)
• IUPAC Name: (4-butoxy-2H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
• InChI: InChI=1S/C18H17F2N3O2/c1-3-4-5-25-17-11(8-21-18-12(17)9-22-23-18)16(24)15-13(19)6-10(2)7-14(15)20/h6-9H,3-5H2,1-2H3,(H,21,22,23)
• InChIKey: SCFMWQIQBVZOQR-UHFFFAOYSA-N
• SMILES: CCCCOC1=C(C=NC2=NNC=C12)C(=O)C3=C(C=C(C=C3F)C)F

BMS-265246（Cat No.:I004172）is a selective inhibitor of the enzyme phosphatidylinositol 3-kinase (PI3K), particularly targeting the p110α isoform. By inhibiting PI3K, BMS-265246 disrupts key signaling pathways involved in cell growth, survival, and metabolism, making it a promising candidate in cancer research. Its potential therapeutic applications include treating various malignancies, especially those with aberrant PI3K signaling. Preclinical studies have shown efficacy in reducing tumor growth and enhancing the effects of other anticancer agents. Ongoing research aims to further elucidate its safety profile and optimal use in combination therapies for improved cancer treatment outcomes.

Reference

[1]. Misra RN, Xiao H, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8.
Abstract
Structure-activity studies of 1H-pyrazolo[3,4-b]pyridine 1 have resulted in the discovery of potent CDK1/CDK2 selective inhibitor 21h, BMS-265246 (CDK1/cycB IC(50)=6 nM, CDK2/cycE IC(50)=9 nM). The 2,6-difluorophenyl substitution was critical for potent inhibitory activity. A solid state structure of 21j, a close di-fluoro analogue, bound to CDK2 shows the inhibitor resides coincident with the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone.