| Cat.No.: | BSM-0016 |
| Product Name: | JNJ-7706621 |
| CAS No.: | 443797-96-4 |
| 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. |
| Molecular Weight: | 394.36 |
| Storage: | 2 years -20°C Powder; 2 weeks 4°C in DMSO; 6 months -80°C 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. |
| Warning: | For Research Use Only! Not For Use in Humans. |
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