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BI 6727
- Volasertib
- Optical Purity: Optically pure
- Moderately soluble in DMSO
- MF: C34H50N8O3
- MW: 618.81
Description
BI 6727 is a highly potent polo-like kinase 1 inhibitor with a reported enzyme IC50 value of 0.87 nM and antiproliferative EC50 values of 11–37 nM across cancer cell lines.
Volasertib disrupts mitotic progression, spindle formation and cytokinesis, leading to G2/M arrest and apoptosis. Its pharmacokinetic profile and cellular potency make it a key tool for mitotic kinase, cancer and taxane-resistance research.
Key Features
- Highly potent PLK1 inhibitor
- Enzyme IC50: 0.87 nM
- Cellular antiproliferative EC50: 11–37 nM
- Induces mitotic arrest and apoptosis
Applications
- PLK1 kinase and target-engagement assays
- Mitotic spindle and G2/M checkpoint studies
- Cancer-cell proliferation models
- Taxane-resistance and combination-treatment research
More Information
| Parent CAS No. | 755038-65-4 |
|---|---|
| Chemical Name | N-((trans)-4-(4-(cyclopropylmethyl)piperazin-1-yl)cyclohexyl)-4-((R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxybenzamide |
| SMILES | C12N(C(C)C)[C@H](CC)C(=O)N(C)C=1C=NC(NC1C(OC)=CC(C(=O)N[C@H]3CC[C@H](N4CCN(CC5CC5)CC4)CC3)=CC=1)=N2 |&1:5,26,29,r| |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | SXNJFOWDRLKDSF-XKHVUIRMSA-N |
| CID | 10461508 |
| Short Description | PLK1 inhibitor |
References
- D Rudolph et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin. Cancer Res. 2009, 15(9), 3094-3102.
- P Schöffski. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009, 14(6), 559-570.
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