BRD4 degrader AT1|2098836-45-2|-陌孚医药/Medlife

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BRD4 degrader AT1

目录号: PL10620 纯度: ≥98%

CAS No. :2098836-45-2

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中文名称	BRD4 degrader AT1
英文名称	BRD4 degrader AT1
英文别名	BRD4 degrader AT1;AT 1;(2S,4R)-1-((R)-2-acetamido-3-((6-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)hexyl)thio)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-(2R)-2-Acetamido-3-[[6-[2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamido]hexyl]thio]-3-methylbutanoyl]-4-hydroxy-N-[4-(4-methylthiazol-5-yl)benzyl)pyr
Cas No.	2098836-45-2
分子式	C₄₈H₅₈ClN₉O₅S₃
分子量	972.68
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情	BRD4 degrader AT1 是由von Hippel-Lindau配体和BRD4配体相连的PROTAC，具有Brd4高度选择性，在细胞中对 Brd4^BD2 的 K_d 值为 44 nM。
生物活性	BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a K d of 44 nM for Brd4 in cells.
性状	Solid
IC50 & Target[1][2]	Kd: 44 nM (Brd4, cell assay), 38.8 nM (Brd4 QVK, cell assay), 111 nM (Brd2, cell assay), 94 nM (Brd2, cell assay), 35 nM (Brd3, cell assay), 39 nM (Brd3, cell assay), 75 nM (Brd4, cell assay), 35 nM (Brd2 KEA, cell assay)
体外研究(In Vitro)	BRD4 degrader AT1 is a highly selective Brd4 degrader, with a Kd of 44 nM, for Brd4 in cells. BRD4 degrader AT1 also shows Kds of 38.8 nM for a mutant Brd4 (QVK), 111 ± 14 nM for Brd2, 94 ± 9 nM for Brd2, 35 ± 3 nM for Brd3, 39 ± 8 nM for Brd3, 75 ± 23 nM for Brd4 and 35 ± 4 nM for a Brd2 mutant (KEA). BRD4 degrader AT1 (1-3 μM) causes remarkable Brd4-selective depletion and has no or little activity against Brd2 and Brd3. 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；In solvent -80°C 6 months
参考文献	[1]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.

溶解度数据	In Vitro: DMSO : 100 mg/mL (102.81 mM; Need ultrasonic)配制储备液

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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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