MS645
目录号: PL13454 纯度: ≥98.0%
CAS No. :2250091-96-2
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中文名称
MS645
英文名称
MS645
英文别名
MS645;CF6;2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6)
Cas No.
2250091-96-2
分子式
C48H54Cl2N10O2S2
分子量
938.04
包装储存
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
MS645 是一种 BET bromodomains (BrD) 抑制剂,对于 BRD4-BD1/BD2 的 Ki 值为 18.4 nM。MS645 在空间上限制 BRD4 BrDs 的二价抑制,从而导致实体肿瘤细胞中 BRD4 转录活性的持续抑制。
生物活性
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K i of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells.
性状
Solid
IC50 & Target[1][2]
BRD4(BD1BD2) 18.4 nM (Ki)
体外研究(In Vitro)
MS645 has cell growth inhibitory effects on noncancer cell lines of mouse macrophage RAW cells and nontumorigenic breast epithelial MCF10A with IC50s of 4.1 nM, 6.8 nM, 7.9 nM for triple-negative breast cancer (TNBC) cell lines HS5878T, BT549, and MCF 10A.
MS645 (15, 30, 60 nM) results in a dramatic reduction of c-Myc expression and an increase of p21, a tumor suppressor and cell-cycle inhibitor in HCC1806 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, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Ren C, et al. Spatially constrained tandem bromodomain inhibition bolsters sustained repression of BRD4 transcriptional activity for TNBC cell growth.Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):7949-7954.
溶解度数据
In Vitro: DMSO : 200 mg/mL (213.21 mM; Need ultrasonic)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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