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KI3405JNJ-7706621QuoteQuote

Chemical Characteristic

Product NameJNJ-7706621
CAS No.443797-96-4
Molecular Weight 394.36
FormulaC15H12F2N6O3S
Chemical Name4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide
Smilesc1(ccc(cc1)Nc1nn(c(n1)N)C(=O)c1c(cccc1F)F)S(=O)(=O)N
Chemical Structure

Biological activities

JNJ-7706621 is a dual inhibitor of cyclin-dependent kinases (CDKs) and aurora kinases. JNJ-7706621 inhibits CDK1 and CDK2 with IC50s of 6 and 2 nM, respectively.[1] JNJ-7706621 inhibits CDK3, Aurora-A and Aurora-B kinases with IC50s of 58, 11 and 15 nM, respectively.[2] In cell based assays, JNJ-7706621 displays anti-proliferative activity against various human tumor cells (HeLa, HCT116, and A375) with IC50s of 280, 250, and 450 nM, respectively.[1] JNJ-7706621 delays exit from G1, arrests cells in G2-M, and induces endoreduplication. In human cancer cells (HASMC, and HMVEC), treatment with JNJ-7706621 inhibits cell growth independent of p53, retinoblastoma, or P-glycoprotein status and activates apoptosis and reduces colony formation.[2] Administration ip of JNJ-7706621 (100 mg/kg) exhibits 95% tumor growth inhibition in A375 (human melanoma cell) in nude mice xenograft model.[1]

Protocols

In vitro, JNJ-7706621 is dissolved in DMSO.[3]

References

[1] Huang S, et al. Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorg Med Chem Lett. 2006, 16(14): 3639-3641.
[2] Emanuel S, et al. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 2005, 65(19): 9038-9046.
[3] Matsuhashi A, et al. Growth suppression and mitotic defect induced by JNJ-7706621, an inhibitor of cyclin-dependent kinases and aurora kinases. Curr Cancer Drug Targets. 2012, 12(6): 625-639.

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