产品介绍
Product Description
Biochem/physiol Actions
Orally active, ATP-competitive, potent and selective polo-like kinase (PLK) inhibitor with anti-cancer efficacy in cultures and in vivo.
Volasertib (BI 6727) is an orally active, ATP-competitive, potent and selective polo-like kinase (PLK) inhibitor (PLK1/2/3 IC50 = 0.87/5/56 nM by kinase assay with 7.5 μM ATP) with no significant inhibitory potency (at 10 μM) toward a panel of >50 other kinases. Volasertib exhibits antiproliferation efficacy in cancer cultures (IC50 from 11 to 37 nM) and in mice in vivo via i.v. (20-30 mg/kg/wk or 10-25 mg/kg 2x a wk; HCT-116 & CXB1 xenografts) or p.o. (7-10 mg/kg/d, 15-25 mg/kg 2x a wk, 50-70 mg/kg/wk; NCI-H460, HCT-116 & CXB1 xenografts).
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | -10 to -25°C |
| SMILES string | N5(CCN(CC5)CC6CC6)[C@@H]1CC[C@H](CC1)NC(=O)c2cc(c(cc2)Nc3nc4c(cn3)N(C(=O)[C@H](N4C(C)C)CC)C)OC |
| 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-,28-/m1/s1 |
| InChI key | SXNJFOWDRLKDSF-STROYTFGSA-N |
