3-Methylthienyl-carbonyl-JNJ-7706621 

3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC₅₀s 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 (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 can be used for the research of cancer^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

378.43

C₁₄H₁₄N₆O₃S₂

443798-09-2

O=S(C1=CC=C(NC2=NN(C(C3=C(C)C=CS3)=O)C(N)=N2)C=C1)(N)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Lin R, et, al. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.  [Content Brief]