BX-320

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BX-320 

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。

BX-320

BX-320 Chemical Structure

CAS No. : 702676-93-5

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生物活性

BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect[1].

体外研究
(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[1].
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[1].
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[1].
BX-320 (0.3-10 μM; for 18 hours) greatly reduces the amount of both p-Thr308-Akt and p-Thr386-S6K1[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MDA-468 breast cancer cells
Concentration: 31.6 nM, 100 nM, 316.22 nM, 1 μM, 3.162 μM, 10 μM, and 31.6 μM
Incubation Time: 72 hours
Result: Blocked the growth of MDA-468 cells (IC50=0.6 μM), which are PTEN-negative breast tumor cells expressing high levels of activated Akt.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 0, 0.3, 1, 3, 10 μM
Incubation Time: 18 hours
Result: Reduced the amount of both phospho-Thr308-Akt and phospho-Thr386-S6K1.

体内研究
(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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic (nu/nu) female mice, 6-8 weeks old[1]
Dosage: 200 mg/kg; dose volume was 10 mL/kg
Administration: Oral gavage twice daily (12 h apart)
Result: Significantly inhibited the growth of lung tumors in this model.

分子量

547.45

Formula

C23H31BrN8O3
CAS 号

702676-93-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
  • 1.

    BX-320 is dissolved in 20% (w/v) hydroxypropyl-β-cyclodextrin (20 mg/mL) adjusted to pH 4[1].

参考文献

  • [1]. Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

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