I-BET151 dihydrochloride(Synonyms: GSK1210151A dihydrochloride)

发表于由

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。

I-BET151 dihydrochloride (Synonyms: GSK1210151A dihydrochloride)

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。

I-BET151 dihydrochloride(Synonyms: GSK1210151A dihydrochloride)

I-BET151 dihydrochloride Chemical Structure

CAS No. : 1883545-47-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

I-BET151 dihydrochloride 的其他形式现货产品:

I-BET151

生物活性

I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 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 G0 phase 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/G2 phase[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 G0 phase 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/G2 phase.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务