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，andFGF-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。
| 生物活性 | 3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor ofcyclin-dependent kinase(CDK), withIC50s of 6.4 nM and 2 nM forCDK1/cyclin BandCDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition ofGSK-3(IC50=0.041 μM) and modest potency againstCDK4,VEGF-R2, andFGF-R2(IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research ofcancer[1]. |
| IC50& Target[1] | CDK2/cyclinA 2 nM (IC50) | CDK1/cyclinB 6.4 nM (IC50) | CDK4 0.11 μM (IC50) | FGFR2 0.22 μM (IC50) | VEGFR2 0.13 μM (IC50) | GSK3 41 nM (IC50) |
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体外研究
(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)[1].
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[1].
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体内研究
(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[1].
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 Cmax(nude mouse 0.21, rat 2.5, dog 4.58 μM) following oral administration (nude mouse 30, rat 30 , dog 10 mg/kg)[1].
3-Methylthienyl-carbonyl-JNJ-7706621 exhibits terminal elimination half-lives (nude mouse 0.51, rat 0.64 and, dog 3.89 h), Cmax(nude mouse 6.4, rat 23.2, dog 2.19 μM) and AUC (nude mouse 3.2, rat 11.4, dog 2.45 μMoh) following intravenous administration (nude mouse 3, rat 3 and, dog 1 mg/kg)[1].
| Animal Model: | Male athymic mice were implanted with A375 human melanoma cells[1] | | Dosage: | 75, 100, 125 mg/kg | | Administration: | I.p. once daily for 32 days | | Result: | Reduced the tumor growth.
Survival was increased by about 3 weeks compared with vector alone. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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