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P276-00 is a novel inhibitor for CDK-1, CDK4 and CDK9 with IC50 of 79 nM, 63 nM and 20 nM, respectively [1].

CDK (cyclin-dependent kinase) plays an important role in cell cycle progression via promoting the G1/S cell cycle transition. Many studies have shown that more CDKs are overexpressed in cancer cells than in normal cells, which explain the reason of cancer cells divide uncontrollably[2]. The overexpression of CDK1/4/6 contributes to the phosphorylation of retinoblastoma protein (RB) via binding to CCND1 and results in the release of E2F transcription of genes required for cell cycle progression [3].

P276-00 is a novel inhibitor of CDK (cyclin-dependent kinase) with the ability of arresting the cells in G1/S phase transcription. When tested with NSCLC cell lines, P276-00 showed high ability of inhibiting cell proliferate thus decreased the colony forming potential via blocking cell cycle [4]. In head and neck squamous carcinoma cell line (FaDu, Detroits-562, SCC-25), treated with P276-00 for 12 hours could significantly inhibit cell ability with IC50 value ranging from 0.8 to 1.7 uM for different cell lines via decreasing the expression of CCND1[2].

In SCID mice model with H460 xenograft, treatment of P276-00 could down regulate the expression of CDK1 thus induced tumor regression [4]. When tested with HNSCC tumor xenograft mouse model, P276-00 treatment showed anti-cancer ability with a 48% tumor growth inhibition [2].

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