BX-320 |
| Catalog No.GC48433 |
BX-320은 직접 키나제 분석 형식에서 IC50이 30nM인 선택적 ATP-경쟁적 경구 활성 및 직접 PDK1 억제제입니다. BX-320은 또한 apoptosis를 유도합니다. 항암 효과.
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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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