BI-2536

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM). It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice. It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells. BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.Formal Name: 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide. CAS Number: 755038-02-9. Molecular Formula: C28H39N7O3. Formula Weight: 521.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 210, 249, 345 nm. SMILES: O=C1[C@@H](CC)N(C2CCCC2)C3=NC(NC4=C(OC)C=C(C(NC5CCN(C)CC5)=O)C=C4)=NC=C3N1C. InChi Code: InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1. InChi Key: XQVVPGYIWAGRNI-JOCHJYFZSA-N.