3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy.

CDK4:0.11 μM (IC50), VEGFR2:0.13 μM (IC50), CDK1-CyclinB:6.4 nM (IC50), GSK-3:41 nM (IC50), FGFR2:0.22 μM (IC50), CDK2-CyclinA:2 nM (IC50)

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.