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INX-315 is an inhibitor of the cyclin-dependent kinase 2 (Cdk2)/cyclin E1 and Cdk2/cyclin A2 complexes (IC50s = 0.6 and 2.5 nM, respectively).1 It is selective for Cdk2/cyclin E1 and Cdk2/cyclin A2 complexes over other Cdk/cyclin complexes (IC50s = 15.1-349 nM). INX-315 induces cell cycle arrest at the G1 phase in OVCAR-3 ovarian cancer and MKN1 gastric carcinoma cells. It selectively reduces the viability of ovarian cancer cells that contain an amplification for CCNE1, the gene encoding cyclin E1, (IC50s = 10-64 nM) over ovarian cancer cells that do not contain a CCNE1 amplification (IC50s = 159-3,560 nM). INX-315 (100 mg/kg) reduces tumor volume in patient-derived xenograft (PDX) mouse models of CCNE1-amplified gastric adenocarcinoma and ovarian cancer.
WARNING This product is not for human or veterinary use.
1. INX-