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BX-320

CAS No. : 702676-93-5

MCE 站：BX-320

产品活性：BX-320 是一种选择性的、ATP 竞争性的、口服有效的直接 PDK1 抑制剂，IC₅₀ 为 30 nM。BX-320 还诱导细胞凋亡 (apoptosis)。具有抗癌作用。

研究领域：PI3K/Akt/mTOR

作用靶点：PDK-1

In Vitro: BX-320 binds to the ATP binding site of PDK1. BX-320 also inhibits Chck1, c-Kit, KDR, PKA, CDK2b/cyclin E, GSK3β, PKC with IC₅₀s of 0.82, 0.89, 1.4, 1.4, 1.5, 4.0, ａnd 5.7 μM, respectively.
BX-320 blocks PDK1/Akt signaling in tumor cells ａnd inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
BX-320 inhibits the growth of MDA-468 breast cancer cells (IC₅₀=0.6 μM) ａnd induces apoptosis. BX-320 promotes a 12-fold induction of caspase-3/7 activity after 48 h of treatment (IC₅₀=0.5 μm), indicating a strong proapoptotic response.
BX-320 (0.3-10 μM; for 18 hours) greatly reduces the amount of both p-Thr308-Akt ａnd p-Thr386-S6K1.

In Vivo: BX-320 (oral dosing with 200 mg/kg, twice a day for 21 days) shows efficacy in a blood-borne metastasis model. BX-320 inhibits the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. BX-320 has efficacy in an in vivo tumor model, which may reflect an inhibition of productive implantation of tumor cells in the lung or an inhibition of subsequent tumor growth.

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