|Description||ETP-46321 is a potent and orally bioavailable PI3K α, δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing. ETP-46321 PK/PD studies showed time dependent downregulation of AKT(Ser473) phosphorylation, which correlates with compound levels in tumor tissue and demonstrating to be efficacious in a GEMM mouse tumor model driven by a K-Ras(G12V) oncogenic mutation. Treatment with ETP-46321 resulted in significant tumor growth inhibition.|
|Synonyms||ETP-46321; ETP46321; ETP 46321|
|Current Developer||Spanish National Cancer Research Centre (CNIO), Madrid, Spain.|
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