S80262 |
I-BET151 |
| 源叶(MedMol) | 98% |
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- 产品描述： I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively
- 靶点： pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]
- 体内研究： I-BET151 demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%). I-BET151 (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice.
- 参考文献：
1. Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. 2. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.
- 溶解性： DMSO : ≥ 100 mg/mL (240.71 mM)
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.407 ml 12.035 ml 24.071 ml 5 mM 0.481 ml 2.407 ml 4.814 ml 10 mM 0.241 ml 1.204 ml 2.407 ml 50 mM 0.048 ml 0.241 ml 0.481 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
