BAY-1816032

BAY-1816032 is an inhibitor of the mitotic checkpoint serine/threonine protein kinase BUB1 (IC50 = 6.1 nM). It is selective for BUB1 over FLT3 (IC50 = 4.2 µM) and 15 other kinases (IC50s = >10 µM for all). BAY-1816032 inhibits proliferation of a variety of cancer cells (median IC50 = 1.4 µM) and acts synergistically with the mitotic inhibitor paclitaxel (Cay-10461) to increase the rate of chromosomal segregation defects during mitosis in HeLa cells. It reduces tumor growth in a SUM149 mouse xenograft model when administered at a dose of 25 mg/kg and has an additive effect on reducing tumor growth when used in combination with paclitaxel in the same model.Formal Name: 2-[3,5-difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]-ethanol. CAS Number: 1891087-61-8. Molecular Formula: C27H24F2N6O4. Formula Weight: 534.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 14 mg/mL, DMSO: 10 mg/mL, Ethanol: Slightly soluble, PBS (pH 7.2): 0.20 mg/mL. lambdamax: 217, 257, 309 nm. SMILES: FC1=C(CN2N=C(C3=C2C=CC=C3)C4=NC(NC5=C(OC)C=NC=C5)=C(OC)C=N4)C(F)=CC(OCCO)=C1. InChi Code: InChI=1S/C27H24F2N6O4/c1-37-23-13-30-8-7-21(23)32-26-24(38-2)14-31-27(33-26)25-17-5-3-4-6-22(17)35(34-25)15-18-19(28)11-16(12-20(18)29)39-10-9-36/h3-8,11-14,36H,9-10,15H2,1-2H3,(H,30,31,32,33). InChi Key: QVOGVAVHOLLLAZ-UHFFFAOYSA-N.