[CAS NO. 443797-96-4]  JNJ-7706621

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PRODUCTS SPECIFICATIONS [443797-96-4]

Store
Catalog
SLK-S1249
Brand
Selleck
CAS
443797-96-4

DESCRIPTION [443797-96-4]

Overview

MDLMFCD11100270
Molecular Weight394.36
Molecular FormulaC15H12F2N6O3S
SMILESNC1=NC(NC2=CC=C(C=C2)S(N)(=O)=O)=NN1C(=O)C1=C(F)C=CC=C1F

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.5358 mL12.6788 mL25.3575 mL
5 mM0.5072 mL2.5358 mL5.0715 mL
10 mM0.2536 mL1.2679 mL2.5358 mL
50 mM0.0507 mL0.2536 mL0.5072 mL

Description

JNJ-7706621 is pan- inhibitor with the highest potency on CDK1/2 with of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

Features

A broad-spectrum inhibitor.

Targets


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.