Volasertib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Volasertib (BI 6727) 是一种有效的选择性 Polo 样激酶 (PLK) 抑制剂，对 PLK1、2 和 3 的 IC50 分别为 0.87、5 和 56 nM。

Volasertib (BI 6727) is a potent, selective Polo-like kinase (PLK) inhibitor with IC50 of 0.87, 5 and 56 nM for PLK1, 2 and 3, respectively; displays no inhibitory activity against a panel of >50 other kinases; inhibits proliferation of multiple cell lines derived from various cancer tissues, including HCT116 (EC50=23 nM) and NCI-H460 (EC50=21 nM),BRO (EC50=11 nM), and hematopoietic cancer cell HL-60 (EC50=32 nM); demonstrates marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer.Blood Cancer Phase 3 Clinical.

Cell Proliferation Assay Cell Line:Multiple cell lines Concentration:0.01-10000 nM Incubation Time:72 hours Result:Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC50=23 nmol/L) and lung (NCI-H460, EC50=21 nmol/L), melanoma (BRO, EC50=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC50=15 nmol/L; HL-60, EC50=32 nmol/L; THP-1, E50=36 nmol/L and Raji, EC50=37 nmol/L) with EC50 values of 11 to 37 nmol/L.Apoptosis Analysis Cell Line:NCI-H460 cells Concentration:100 nM Incubation Time:24, 48, 72 hours Result:G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours. Cell Cycle Analysis Cell Line:NCI-H460 cells Concentration:10, 30, 100, 300, 1000 nM Incubation Time:24 hours Result:Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.

Animal Model:Female BomTac:NMRI-Foxn1nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)Dosage:A total weekly dose of 50 mg/kg Administration:Oral; once a week, twice a week, or daily; for 40 days Result:Showed comparable efficacy and were well tolerated. Animal Model:Female BomTac:NMRI-Foxn1nu mice and male Wistar rats of the strain Crl:WI Dosage:35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis) Administration:IV 5-minute infusion; a single dose 5-minute infusion Result:Had high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h).

BI 6727 | BI-6727 | BI6727

Cell Cycle/DNA Damage

PLK

PLK1

Cancer

Blood cancer

755038-65-4

618.8126

C34H50N8O3

>98% (HPLC)

10 mM in DMSO

O=C(N[C@H]1CC[C@@H](N2CCN(CC3CC3)CC2)CC1)C4=CC=C(NC(N=C5N(C(C)C)[C@@H]6CC)=NC=C5N(C)C6=O)C(OC)=C4

Benzamide, 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-

(-20℃)

With Ice Pack

≥ 2 years