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3-Methylthienyl-carbonyl-JNJ-7706621

CAS No. : 443798-09-2

MCE 站：3-Methylthienyl-carbonyl-JNJ-7706621

产品活性：3-Methylthienyl-carbonyl-JNJ-7706621 是一种有效和选择性的细胞周期蛋白依赖性激酶 (CDK) 抑制剂，对 CDK1/cyclin B 和 CDK2/cyclin A 的 IC₅₀ 值分别为 6.4 nM 和 2 nM。3-Methylthienyl-carbonyl-JNJ-7706621 还显示出对 GSK-3 (IC₅₀=0.041 μM) 的有效抑制和对 CDK4，VEGF-R2，and FGF-R2 (IC₅₀=0.11, 0.13, 0.22 μM) 的适度效力。3-Methylthienyl-carbonyl-JNJ-7706621 可用于癌症的研究。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  PI3K/Akt/mTOR  |  Protein Tyrosine Kinase/RTK

作用靶点：CDK  |  GSK-3  |  VEGFR  |  FGFR

In Vitro: 3-Methylthienyl-carbonyl-JNJ-7706621 shows potent potency against GSK-3 (IC₅₀=0.041 μM) ａnd modest potency against CDK4, VEGF-R2, ａnd FGF-R2 (IC₅₀=0.11, 0.13, 0.22 μM, respectively).
3-Methylthienyl-carbonyl-JNJ-7706621 inhibits cell proliferation, with IC₅₀s of 0.28 μM, 0.25 μM, 0.45 μM, 0.75 μM, 0.59 μM ａnd 0.12 μM for HeLa, HCT-116, A375, SK-OV-3, MDA-MB-231 ａnd PC-3 cells, respectively.

In Vivo: 3-Methylthienyl-carbonyl-JNJ-7706621 (75-125 mg/kg; i.p. once daily for 32 days) inhibits the A375 human melanoma tumor growth ａnd prolongs the survival in nude mice.
3-Methylthienyl-carbonyl-JNJ-7706621 exhibits oral bioavailability (nude mouse 2%, rat 8%, dog 63.3%), terminal elimination half-lives (nude mouse 1.70, rat 2.20 and, dog 2.36 h) ａnd C_max (nude mouse 0.21, rat 2.5, dog 4.58 μM) following oral administration (nude mouse 30, rat 30 , dog 10 mg/kg).
3-Methylthienyl-carbonyl-JNJ-7706621 exhibits terminal elimination half-lives (nude mouse 0.51, rat 0.64 and, dog 3.89 h), C_max (nude mouse 6.4, rat 23.2, dog 2.19 μM) ａnd AUC (nude mouse 3.2, rat 11.4, dog 2.45 μM•h) following intravenous administration (nude mouse 3, rat 3 and, dog 1 mg/kg).

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