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I-BET151 dihydrochloride

CAS No. : 1883545-47-8

MCE 站：I-BET151 dihydrochloride

产品活性：I-BET151 dihydrochloride (GSK1210151A dihydrochloride) 是一种 BET 溴结构域 (BET bromodomain) 抑制剂，抑制 BRD4，BRD2 和 BRD3 的 pIC₅₀ 分别为 6.1，6.3 和 6.6。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: I-BET151 dihydrochloride (1 μM; 72 hours) treatment displays the majority of live cells resided in the G₀ phase ａnd commensurate with a dose- ａnd time-dependent decrease in cell proliferation ａnd abrogation of bromodeoxyuridine incorporation.
I-BET151 dihydrochloride (100 nM; 72 hours) causes a significant dose- ａnd time-dependent decrease in the proportion of myeloma cells in S/G₂ phase.

In Vivo: I-BET151 dihydrochloride 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 dihydrochloride 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 dihydrochloride (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.

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