Products

Online Inquiry

Name

Email *

Phone *

Company/Institution

Country or Region

Quantity

Services & Products Interested *

Project Description

Our Products Cannot Be Used As Medicines Directly For Personal Use.

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

JNJ-7706621

inquiry

Cat No.

CEI-0898

Description

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. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

CAS No.

443797-96-4

Molecular Weight

394.36

Storage

2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.

Targets

CDK1/Cyclin B, CDK2/Cyclin A, CDK2/Cyclin E, Aurora-A, Aurora-B

IC50

9 nM; 4 nM; 3 nM; 11 nM; 15 nM

Molecular Formula

C15H12F2N6O3S

Solubility

DMSO 79 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL

In vitro

JNJ-7706621 also 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.