Chemical Name : BI2536/BI-2536/
CAS : 755038-02-9
Storage:-20C 2 years
GSK461364, a selective i.v. thiophene amide inhibitor of PLK1, induced selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. GSK461364 is an ATP-competitive inhibitor of Plk1 and forms a rapidly reversible complex with Plk1. It has a 400-fold greater potency for Plk1 than for Plk2 and Plk3.In vitro, this compound showed antiproliferative activity in ��120 cancer cell lines tested. IC50 values were ��50 nM in ��83% of the cell lines tested. GSK461364 demonstrated tumor growth inhibition in animal models. In these xenograft models, GSK461364 showed antitumor activity ranging from complete tumor growth inhibition to growth delay. Interestingly, the compound caused dose-dependent mitotic arrest in Colo205 xenografts in vivo.
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