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I-BET151 (Synonyms: GSK1210151A) 纯度: 99.81%
I-BET151 (GSK1210151A) 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 Chemical Structure
CAS No. : 1300031-49-5
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1377 | In-stock | |
5 mg | ¥1252 | In-stock | |
10 mg | ¥1989 | In-stock | |
50 mg | ¥6412 | In-stock | |
100 mg | ¥9360 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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I-BET151 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Epigenetics Compound Library
- Histone Modification Research Compound Library
- Anti-Cancer Compound Library
- Reprogramming Compound Library
- Anti-Blood Cancer Compound Library
生物活性 |
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[1][2]. |
IC50 & Target |
pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1] |
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体外研究 (In Vitro) |
I-BET151 (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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay[2]
Cell Proliferation Assay[2]
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体内研究 (In Vivo) |
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%)[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
415.44 |
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Formula |
C23H21N5O3 |
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CAS 号 |
1300031-49-5 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (240.71 mM) * “≥” means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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