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BX-320

カタログ番号GC48433

BX-320 は、直接キナーゼアッセイ形式で 30 nM の IC50 を持つ、選択的、ATP 競合性、経口活性、および直接 PDK1 阻害剤です。 BX-320 はアポトーシスも誘導します。抗がん効果。

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BX-320 化学構造

Cas No.: 702676-93-5

サイズ 価格 在庫数 個数
500µg
$77.00
在庫あり
1mg
$116.00
在庫あり
5mg
$462.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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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Average Rating: 5 ★★★★★ (Based on Reviews and 35 reference(s) in Google Scholar.)

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