BX-517
货号:
IB1930
品牌:
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是一种有效的,选择性的 PDK1 抑制剂。 |
| CAS | 850717-64-5 |
| 分子式 | C15H14N4O2 |
| 分子量 | 282.3 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 单位 | 瓶 |
| 生物活性 | BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.[1] |
| IC50 | 6 nM (PDK1)[1] |
| In Vitro | BX-517 blocks activation of Akt in tumor cells, is potent with IC50 of 0.1-1.0 μM[1]. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases[2]. |
| SMILES | NC(NC1=CC=C(NC(/C2=C(C)C3=CC=CN3)=O)C2=C1)=O |
| 靶点 | PDK-1 |
| 数据来源文献 | [1]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25.
[2]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. |
| 规格 | 5mg 10mg |