3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK) , with IC 50 s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A , respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 ( IC 50 =0.041 μM) and modest potency against CDK4 , VEGF-R2 , and FGF-R2 ( IC 50 =0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.

3-Methylthienyl-carbonyl-JNJ-7706621 shows potent potency against GSK-3 (IC 50 =0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC 50 =0.11, 0.13, 0.22 μM, respectively)[1]. 3-Methylthienyl-carbonyl-JNJ-7706621 inhibits cell proliferation, with IC 50 s 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].

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 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)[1]. 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)[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.

443798-09-2

C14H14N6O3S2

378.43

3-Methylthienyl-carbonyl-JNJ-7706621

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years