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BI-2536

Chemical Structure : BI-2536

CAS No.: 755038-02-9

BI-2536 (BI 2536;BI2536)

Catalog No.: PC-45847Not For Human Use, Lab Use Only.

BI-2536 is a potent and selective inhibitor of PLK1 with IC50 of 0.83 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BI-2536 is a potent and selective inhibitor of PLK1 with IC50 of 0.83 nM.
BI-2536 also weakly inhibits the activities of PLK2 and PLK3 (IC50=3.5 nM and 9.0 nM, respectively), displays >1,000-fold selectivity to a panel of 63 other protein kinases.
BI-2536 causes a mitotic arrest and induces apoptosis in human cancer cell lines, inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens.
BI-2536 also inhibits BRD4 with IC50 of 25 nM.

Physicochemical Properties

M.Wt 521.6544
Formula C28H39N7O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzamide, 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-

References

1. Steegmaier M, et al. Curr Biol. 2007 Feb 20;17(4):316-22. Epub 2007 Feb 8.

2. Chen L, et al. ACS Med Chem Lett. 2015 May 18;6(7):764-9.

3. Nappi TC, et al. Cancer Res. 2009 Mar 1;69(5):1916-23.

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