BI-3802
目录号: PL07455 纯度: ≥99%
CAS No. :2166387-65-9
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中文名称
BI-3802
英文名称
BI-3802
英文别名
2-((6-((5-Chloro-2-((3S,5R)-3,5-dimethylpiperidin-1-yl)pyrimidin-4-yl)amino)-1-methyl-2-oxo-1,2-dihydroquinolin-3-yl)oxy)-N-methylacetamide;2-[6-[[5-Chloranyl-2-[(3~{s},5~{r})-3,5-Dimethylpiperidin-1-Yl]pyrimidin-4-Yl]amino]-1-Methyl-2-Oxidanylidene-Quinolin-3-Yl]oxy-~{n}-Methyl-Ethanamide;U52;BI-3802
Cas No.
2166387-65-9
分子式
C24H29ClN6O3
分子量
484.98
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
BI-3802 是一种高效的 BCL6 降解剂,能够抑制 BCL6 的Bric-à-brac (BTB) 结构域,IC50 值 ≤3 nM。BI-3802 可诱导 BCL6 蛋白聚集,并促进 E3 连接酶 SIAH1 介导的蛋白降解。BI-3802 具有抗肿瘤活性。
生物活性
BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC 50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity.
性状
Solid
IC50 & Target[1][2]
IC50: ≤ 3 nM (BCL6 BTB)
体外研究(In Vitro)
BI-3802 shows an IC50 of 43 nM for the cellular BCL6.
BI-3802 increases the interaction between BCL6 and SIAH1 (EC50 = 64 nM).
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Kerres N, et al. Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6. Cell Rep. 2017 Sep 19;20(12):2860-2875.
[2]. Miko?aj S?abicki, et al. Small-molecule-induced polymerization triggers degradation of BCL6. Nature. 2020 Nov 18.
溶解度数据
In Vitro: DMSO : 6.67 mg/mL (13.75 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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