Lerociclib , also known as G1T38, is an oral, potent and selective CDK4/6 inhibitor for the treatment of Rb competent tumors. Biochemical profiling demonstrates G1T38 is a competitive, nanomolar inhibitor of CDK4/6 with highly selectivity for CDK4-cyclin D1 and CDK6-cyclin D3. G1T38 exhibits a low EC50>3 μM in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models.
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