BX-320 |
| Catalog No.GC48433 |
Le BX-320 est un inhibiteur sélectif, compétitif pour l'ATP, actif par voie orale et direct de PDK1 avec une CI50 de 30 nM dans un format de dosage direct de la kinase. Le BX-320 induit également l'apoptose. Effet anticancéreux.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 702676-93-5
Sample solution is provided at 25 µL, 10mM.
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BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 30 nM).1 It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 µM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 µM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 µM). BX-320 (200 mg/kg) inhibits the growth of lung tumors in a LOX melanoma mouse model of blood-borne metastasis.
1.Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20)19867-19874(2005)
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