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I-BET151 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
I-BET151 dihydrochloride图片
CAS NO:1883545-47-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
GSK1210151A dihydrochloride
产品介绍
I-BET151 dihydrochloride (GSK1210151A dihydrochloride) 是一种 BET 溴结构域 (BET bromodomain) 抑制剂,抑制BRD4BRD2BRD3pIC50分别为 6.1,6.3 和 6.6。
生物活性

I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is aBET bromodomaininhibitor which inhibitsBRD4,BRD2, andBRD3withpIC50of 6.1, 6.3, and 6.6, respectively[1][2].

IC50& Target

pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]

体外研究
(In Vitro)

I-BET151 dihydrochloride (1 μM; 72 hours) treatment displays the majority of live cells resided in the G0phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].
I-BET151 dihydrochloride (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2phase[2].

Cell Viability Assay[2]

Cell Line:H929 cells
Concentration:1 μM
Incubation Time:72 hours
Result:Displays the majority of live cells resided in the G0phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.

Cell Proliferation Assay[2]

Cell Line:H929 cells
Concentration:100 nM
Incubation Time:72 hours
Result:Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2phase.
体内研究
(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%)[1].
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[2].

Animal Model:Mice (model of subcutaneous myeloma)[2]
Dosage:50 mg/kg
Administration:I.p.; daily for 21 days
Result:Reduced rate of tumor size doubling than vehicle-treated mice.
分子量

488.37

Formula

C23H23Cl2N5O3

CAS 号

1883545-47-8

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.