dCBP-1

目录号: PL10627 纯度: ≥99%
dCBP-1 是一种基于 Cereblon 配体的 p300/CBP 的有效且选择性的异双功能降解剂。dCBP-1 在杀死多发性骨髓瘤细胞方面非常有效,并降低了驱动 MYC 表达的致癌增强子活性。
CAS No. :2484739-25-3
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中文名称
dCBP-1
英文名称
dCBP-1
英文别名
dCBP-1;5H-​Pyrazolo[4,​3-​c]​pyridine-​5-​carboxamide, 3-​[7-​(difluoromethyl)​-​3,​4-​dihydro-​6-​(1-​methyl-​1H-​pyrazol-​4-​yl)​-​1(2H)​-​quinolinyl]​-​1-​[1-​[15-​[[2-​(2,​6-​dioxo-​3-​piperidinyl)​-​2,​3-​dihydro-​1,​3-​dioxo-​1H-​isoindol-​5-​yl]​amino]​-​1-​oxo-​4,​7,​10,​13-​tetraoxapentadec-​1-​yl]​-​4-​piperidinyl]​-​1,​4,​6,​7-​tetrahydro-​N-​methyl-;3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-1-[1-[3-[2-[2-[2-[2-[[2;3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-1-[1-[3-[2-[2-[2-[2-[[2
Cas No.
2484739-25-3
分子式
C51H63F2N11O10
分子量
1028.11
包装储存
-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述
dCBP-1 是一种基于 Cereblon 配体的 p300/CBP 的有效且选择性的异双功能降解剂。dCBP-1 在杀死多发性骨髓瘤细胞方面非常有效,并降低了驱动 MYC 表达的致癌增强子活性。
产品详情
dCBP-1 是一种基于 Cereblon 配体的 p300/CBP 的有效且选择性的异双功能降解剂。dCBP-1 在杀死多发性骨髓瘤细胞方面非常有效,并降低了驱动 MYC 表达的致癌增强子活性。
生物活性
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
性状
Solid
IC50 & Target[1][2]
p300/CBP Cereblon
体外研究(In Vitro)
dCBP-1 (10-1000 nM; 6 hours) treatment shows near-complete degradation of p300/CBP in MM1S cells. dCBP-1 is also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34.
Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 reveals almost complete loss of both CBP and p300 between 10 and 1000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment. 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 moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.
溶解度数据
In Vitro: DMSO : 50 mg/mL (48.63 mM; ultrasonic and warming and heat to 80°C)配制储备液
搜索质检报告(COA)
[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.

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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