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BI 2536
- Optical Purity: >99% e.e.
- Soluble in DMSO
- MF: C28H39N7O3
- MW: 521.65
Description
BI 2536 is a potent and selective polo-like kinase 1 (PLK1) inhibitor with an IC50 value of 0.83 nM. It shows 4-fold selectivity over PLK2 and 11-fold over PLK3 and is widely used to study PLK1-dependent regulation of mitosis.
By inhibiting PLK1, BI 2536 induces mitotic arrest and subsequent apoptosis in human cancer cell lines, making it a useful tool compound for research on cell-cycle control, spindle assembly, and cancer biology.
Key Features
- Potent and selective PLK1 inhibitor
- IC50: 0.83 nM
- Shows selectivity over PLK2 and PLK3
- Induces mitotic arrest and apoptosis
Applications
- PLK1 and polo-like kinase pathway research
- Cell-cycle and mitosis studies
- Spindle assembly checkpoint research
- Apoptosis and cancer cell biology
- In vitro and in vivo cancer research models
Prime Source Information:
BI 2536 from Axon Medchem is an optically pure drug reference standard with >99% enantiomeric excess (e.e.) of the R-enantiomer. Axon Medchem also offers its opposite enantiomer (S)-BI 2536 (Axon 4192) for comparative studies.
More Information
| Parent CAS No. | 755038-02-9 |
|---|---|
| Chemical Name | 4-((R)-8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide |
| SMILES | C1(NC2C=CC(C(NC3CCN(C)CC3)=O)=CC=2OC)N=C2N([C@@H](C(=O)N(C)C2=CN=1)CC)C1CCCC1 |&1:23,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1 |
| InChiKey | XQVVPGYIWAGRNI-JOCHJYFZSA-N |
| CID | 11364421 |
| Short Description | PLK1 inhibitor |
References
- M Steegmaier et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Curr Biol 2007, 17, 316-322.
- P Lénárt et al. The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1. Curr Biol 2007, 17(4), 304-15.
- M Sebastian et al. The Efficacy and Safety of BI 2536, a Novel Plk-1 Inhibitor, in Patients with Stage IIIB/IV Non-small Cell Lung Cancer Who Had Relapsed after, or Failed, Chemotherapy. J. Thor. Oncol. 2010, 5(7), 1060-1067.
- HJ Stewart et al. The polo-like kinase inhibitor BI 2536 exhibits potent activity against malignant plasma cells and represents a novel therapy in multiple myeloma. Exp. Hematol. 2011, 39(3), 330-338.
- List of publications utilizing BI 2536 (Axon 1129) purchased from Axon Medchem
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