CCT367766 formic
目录号: PL10634 纯度: ≥98%
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Medlife所售产品仅用于科学研究(非临床研究),非药品不可食用,不可用于人体或动物的临床诊断和治疗,我们不为个人提供产品及服务。产品COA等资料,可至下方“质量控制”中下载。
中文名称
CCT367766 formic
英文名称
CCT367766 formic
包装储存
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
CCT367766 formic 是一种有效的口服活性蛋白,第三代异功能和基于 Cereblon 配体的 pirin 靶向蛋白降解探针 (PDP,或 PROTAC),在低浓度时就可以减少 pirin 蛋白的表达。CCT367766 formic 对 CRBN-DDB1 复合物表现出中等亲和力,其 IC50 值为 490 nM。CCT367766 formic 对重组的 pirin 和 CRBN 具有良好的亲和力,其 Kd 值分别为 55 nM 和 120 nM。CCT367766 formic 阐释了一种有用的的化学工具来研究一些未被开发的蛋白质。
生物活性
CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC 50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with K d values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein.
性状
Solid
IC50 & Target[1][2]
CRBN-DDB1 490 nM (IC50)
体外研究(In Vitro)
CCT367766 formic (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells.
CCT367766 formic (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells.
CCT367766 formic (0.5-50 nM; 2 hours) dose-dependently rescuses pirin expression from pretreatment of chlorobisamide in SK-OV-3 cells. 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
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.
溶解度数据
In Vitro: DMSO : ≥ 250 mg/mL (251.91 mM)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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