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           APIs&Intermediates Chemicals of Shanghai APIs Chemical Co., Ltd 

           

             

 

Product Indentification
 

 

Name:   BI 2536
Synonyms:   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)benzamide; Boehringer PLK-1 inhibitor
CAS Registry Number:   755038-02-9
Molecular Formula:   C28H39N7O3
Molecular Weight:    521.65
Molecular Structure:    

 

 

                    Purity:99%min

 

 

                    Storage: 4 deg.                 

 

 

                    For Research Use Only

 

 

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     Search CAS 755038-02-9  in google
     Search C28H39N7O3  in google

 

 

 

Biological Activity of BI 2536:


BI 2536 is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1, derived from human, mouse and rat) (with IC50of 0.83 nM), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations. Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division.
This compound showed a more than 1000-fold selectivity relative to a panel of 63 other protein kinases, but it also affected the activities of Plk2 at an IC50 of 3.5 nM and, to a slightly lesser extent, the activity of Plk3 (IC50 9.0 nM).
The half-maximal effective concentration (EC50) values in a panel of 32 human cancer cell lines ranged 225 nM.
BI 2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens.

 

 

 

 

 

 

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