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CPI-203 是一种选择性的,细胞通透的 BET 溴结构域抑制剂,抑制 BRD4,IC50值约为 37 nM。

CPI-203 是一种选择性的,细胞通透的 BET 溴结构域抑制剂,抑制 BRD4,IC50值约为 37 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 198 | In stock | |
| 5 mg | ¥ 535 | In stock | |
| 10 mg | ¥ 870 | In stock | |
| 25 mg | ¥ 1,480 | In stock | |
| 50 mg | ¥ 1,830 | In stock | |
| 100 mg | ¥ 2,310 | In stock | |
| 200 mg | ¥ 3,290 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 532 | In stock |
(S)-CPI203 相关产品
| 产品描述 | CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4). |
| 靶点活性 | BRD4:37 nM |
| 体外活性 | CPI203在体外和细胞内抑制BRD4,但不影响BRD4激酶在体外的活性。[1] CPI203对分析的9种MCL细胞系均表现出细胞静止效应,GI50范围从0.06到0.71μM,对来自健康捐献者的正常PBMCs的细胞毒性低。此外,通过针对IRF4和MYC,lenalidomide和CPI203有效激活了对bortezomib抵抗的MCL细胞中的细胞死亡程序。[2] |
| 激酶实验 | BRD4 α-screen assay: The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor. |
| 别名 | CPI203, CPI 203 |
| 分子量 | 399.9 |
| 分子式 | C19H18ClN5OS |
| CAS No. | 1446144-04-2 |
| Smiles | Cc1nnc2[C@H](CC(N)=O)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1 |
| 密度 | 1.51 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 50 mg/mL (125.03 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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