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(JNJ7706621; JNJ 7706621)
JNJ-7706621 Chemical Structure
|Product name: JNJ-7706621|
|Cat. No.: HY-10329|
JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6; also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
IC50 Value: 9 nM(CDK1/Cyclin B); 4 nM(CDK2/Cyclin A); 3 nM(CDK2/Cyclin E); 11 nM (Aurora-A)
Target: CDK1/2; Aurora A/B
in vitro: JNJ-7706621 shows some inhibition to VEGF-R2, FGF-R2, and GSK3β, with IC50 of 154-254 nM. JNJ-7706621 shows inhibitory effect on a panel of human cancer cell types, including HeLa, HCT-116, SK-OV-3, PC3, DU145, A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with IC50 of 112-514 nM, independent of p53, retinoblastoma, or P-glycoprotein status. JNJ-7706621 is several-fold less potent at inhibiting growth of normal cell types, including MRC-5, HASMC, HUVEC, and HMVEC, with IC50 of 3.67-5.42 μM. In HeLa or U937 cells, JNJ-7706621 (0.5-3 μM) delays exit from G1, arrests cells in G2-M, induces endoreduplication, activates apoptosis, and reduces colony formation. In a HeLa cell line, incremental treatment with increasing concentrations of JNJ-7706621 leads to a 16-fold resistance, which may be mediated by ABCG2.
in vivo: In mouse xenograft model of A375 melanoma human tumor, JNJ-7706621 (100 or 125 mg/kg) causes tumor regression.
|M.Wt||394.36||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.5358 mL||12.6788 mL||25.3575 mL|
|5 mM||0.5072 mL||2.5358 mL||5.0715 mL|
|10 mM||0.2536 mL||1.2679 mL||2.5358 mL|
. Huang, Shenlin; Connolly, Peter J.; Lin, Ronghui; Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorganic & Medicinal Chemistry Letters (2006), 16(14), 3639-3641.
. Matsuhashi A, Ohno T, Kimura M, Hara A, Saio M, Nagano A, Kawai G, Saitou M, Takigami I, Yamada K, Okano Y, Shimizu K.Growth suppression and mitotic defect induced by JNJ-7706621, an inhibitor of cyclin-dependent kinases and aurora kinases.Curr Cancer Drug Targets. 2012 Jul;12(6):625-39.
. Danhier F, Ucakar B, Magotteaux N, Brewster ME, Préat V.Active and passive tumor targeting of a novel poorly soluble cyclin dependent kinase inhibitor, JNJ-7706621.Int J Pharm. 2010 Jun 15;392(1-2):20-8. Epub 2010 Mar 11.
. Emanuel S, Rugg CA, Gruninger RH, Lin R, Fuentes-Pesquera A, Connolly PJ, Wetter SK, Hollister B, Kruger WW, Napier C, Jolliffe L, Middleton SA.The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases.Cancer Res. 2005 Oct 1;65(19):9038-46.
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