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Products are for research use only. Not for human use. We do not sell to patients.
(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||
DMSO ≥75mg/mL Water <1.2mg/mL Ethanol ≥2.8mg/mL
|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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AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38(alpha), Tyk2, JNK2, Met and Tie2.
AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.
AT9283 is a small molecule a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), JAK2 and JAK3, Aurora A and Aurora B, respectively.
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AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6.
AZD1152 (barasertib), pro-drug of barasertib-hQPA(HY-10126), is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.
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6-BIO(6-Bromoindirubin-3(acute)-oxime) is a potent and selective inhibitor of GSK-3 and CDK1–cyclinB complex with IC50 of 5 nM /320 nM/83 nM for GSK-3(alpha)(beta)/CDK1/CDK5 respectively.
BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.