FIT-039

Cdk9抑制剂（Cdk9/cyclinT1的IC50=5.8µM）；30µM时对Cdk9/cyclinT1的选择性优于Cdk4/cyclinD3，10µM时对Cdk2/cyclinA2、Cdk2/cyclinE1、Cdk5/p25、Cdk6/cyclinD3和Cdk7/cyclin/MAT1的选择性优于Cdk9/cyclinT1；10µM时抑制GSK3α、GSK3β、PKN1、haspin、p70S6K、DYRK1B、DYRK3和IRR；抑制HeLa细胞中HSV-1的DNA复制（IC50=0.69µM）；以1.25-10%w/w的比例局部使用时，可减轻HSV-1感染小鼠的皮肤病变并提高其存活率；300mg/kg剂量可降低HPV16型阳性CaSki宫颈癌小鼠异种移植模型中的肿瘤生长。A Cdk9 inhibitor (IC50 = 5.8 µM for Cdk9/cyclin T1); selective for Cdk9/cyclin T1 over Cdk4/cyclin D3 at 30 µM and Cdk2/cyclin A2, Cdk2/cyclin E1, Cdk5/p25, Cdk6/cyclin D3, and Cdk7/cyclin/MAT1 at 10 µM; inhibits GSK3α, GSK3β, PKN1, haspin, p70S6K, DYRK1B, DYRK3, and IRR at 10 µM; inhibits DNA replication of HSV-1 in HeLa cells (IC50 = 0.69 µM); reduces skin lesions and improves survival in HSV-1-infected mice when applied topically at 1.25-10% w/w; reduces tumor growth in an HPV type 16-positive Ca Ski cervical cancer mouse xenograft model at 300 mg/kg.分子式C17H18FN3S分子量315.4FC1=CC=C(N2CCCCC2)C(NC(C3=CC=NC=C3)=S)=C1