JNJ-7706621是一种pan-CDK抑制剂，对CDK1/2抑制作用最强，IC₅₀为9 nM/4 nM，作用于CDK1/2比作用于CDK3/4/6选择性高6倍以上。也能有效抑制Aurora A/B，对Plk1和Wee1没有抑制活性。JNJ-7706621作用于CDK1和2具有高度有效性, IC₅₀为3-9 nM。JNJ-7706621也抑制CDK3, 4,和6, IC₅₀为58-253 nM。JNJ-7706621抑制Aurora-A和B，IC₅₀分别为11和15 nM。

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

JNJ7706621

White solid

DMSO : ≥ 125 mg/mL (316.97 mM)

CDK2/CyclinE ,CDK2/CyclinA ,CDK1/CyclinB ,Aurora A ,Aurora B

JNJ-7706621 also shows some inhibition to VEGF-R2, FGF-R2, and GSK3β, with IC50 of 154-254 nM. JNJ-7706621 shows inhibitory effect on a panel of human cancer cell types, including HeLa, HCT-116, SK-OV-3, PC3, DU145, A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with IC50 of 112-514 nM, independent of p53, retinoblastoma, or P-glycoprotein status. JNJ-7706621 is several-fold less potent at inhibiting growth of normal cell types, including MRC-5, HASMC, HUVEC, and HMVEC, with IC50 of 3.67-5.42 μM. In HeLa or U937 cells, JNJ-7706621 (0.5-3 μM) delays exit from G1, arrests cells in G2-M, induces endoreduplication, activates apoptosis, and reduces colony formation. In a HeLa cell line, incremental treatment with increasing concentrations of JNJ-7706621 leads to a 16-fold resistance, which may be mediated by ABCG2.

In mouse xenograft model of A375 melanoma human tumor, JNJ-7706621 (100 or 125 mg/kg) causes tumor regression.