BI-6727

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis. It inhibits proliferation of multiple cancer cell lines with EC50 values ranging from 11-37 nM and prevents the growth of various human carcinoma xenografts in mice. BI-6727 was found to reverse ABC-efflux transporter-mediated multidrug resistance activity through its inhibition of the transport activity of ABCB1 and ABCG2, thus promoting mitotic arrest in resistant cancer cells.Formal Name: N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide. CAS Number: 755038-65-4. Synonyms: Volasertib. Molecular Formula: C34H50N8O3. Formula Weight: 618.8. Purity: >98%. 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: 330 nm. SMILES: CC[C@@H]1C(N(C)C2=CN=C(NC3=C(OC)C=C(C(N[C@@H]4CC[C@@H](N5CCN(CC6CC6)CC5)CC4)=O)C=C3)N=C2N1C(C)C)=O. InChi Code: InChI=1S/C34H50N8O3/c1-6-28-33(44)39(4)29-20-35-34(38-31(29)42(28)22(2)3)37-27-14-9-24(19-30(27)45-5)32(43)36-25-10-12-26(13-11-25)41-17-15-40(16-18-41)21-23-7-8-23/h9,14,19-20,22-23,25-26,28H,6-8,10-13,15-18,21H2,1-5H3,(H,36,43)(H,35,37,38)/t25-,26-. InChi Key: SXNJFOWDRLKDSF-STROYTFGSA-N.