Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CPI-169 racemate (CPI 169) 是CPI-169的消旋体。CPI-169 是一种有效的选择性 EZH2 抑制剂,对 EZH2 WT、EZH2 Y641N 和 EZH1 的 IC50 分别为 0.24、0.51 和 6.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 467 | 现货 | ||
2 mg | ¥ 663 | 现货 | ||
5 mg | ¥ 930 | 现货 | ||
10 mg | ¥ 1,450 | 现货 | ||
25 mg | ¥ 3,190 | 现货 | ||
50 mg | ¥ 4,670 | 现货 | ||
100 mg | ¥ 6,650 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,200 | 现货 |
产品描述 | CPI-169 racemate (CPI 169) is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively. |
靶点活性 | EZH2 (Y641N):0.51 nM, EZH2 (WT):0.24 nM, EZH1:6.1 nM |
体外活性 | In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of <5 μM. [1] |
体内活性 | In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects. [1] |
激酶实验 | Biochemical Assays: Compound potency is also assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, PRC2 containing either EZH1 (160 pM), wt EZH2 (40 pM), or Y641N mutant EZH2 (80 pM, both EZH2 prepared in-house) is pre-incubated with 3H-SAM (0.9 μM), 2 μM H3K27me3 activating peptide (H2N-RKQLATKAAR(Kme3)SAPATGGVKKP-amide) and compounds (as 10 point duplicate dose response titrations) for 120 min in a buffer consisting of 50 mM Tris (pH 8.5), 1 mM DTT, 0.07 mM Brij-35, 0.1% BSA, and 0.8% DMSO in a total volume of 12.5 μl in a black 384 well plate. Reaction is initiated with biotinylated H3 substrate peptides (H3K27me1 for wt EZH2, H3K27me2 for Y641N mutant EZH2; H2N-RKQLATKAAR(Kmen)SAPATGGVKKP-NTPEGBiot) as a 2 μM stock in 12.5 μL and allowed to react at room temperature for 5 h. Quenching is accomplished by addition of 20 μl of STOP solution (50 mM Tris (pH 8.5), 200 mM EDTA, 2 mM SAH). 35 μL of the quenched solution is transferred to Streptavidin Flashplates, incubated overnight, washed, and read in a TopCount Reader. For titrations all compound dilutions are in DMSO, final DMSO concentrations are 0.8% (v/v), and turnover is kept to less than < 5%. IC50s are calculated using non-linear least square four parameter fits (GraphPad 6.0). |
细胞实验 | Relative cell numbers are assessed by Cell Titer-Glo (CTG) luminescent cell viability assay using an Envision instrument. GraphPad Prism 6.0 is used for curve fitting, IC50/GI50 and Hill coefficient (H) calculations. The GI90 is calculated using the formula: EC90 = (90 /100-90)1/H * EC50.(Only for Reference) |
动物实验 | Animal Models: Mice bearing KARPAS-422 subcutaneous xenograftsFormulation: 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2ODosages: 200 mg/kg, BIDAdministration: s.c. |
别名 | CPI 169, CPI-169, CPI169 |
分子量 | 528.66 |
分子式 | C27H36N4O5S |
CAS No. | 1450655-76-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 93 mg/mL (175.9 mM)
DMSO: 93 mg/mL (175.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.8916 mL | 9.4579 mL | 18.9157 mL | 47.2894 mL |
5 mM | 0.3783 mL | 1.8916 mL | 3.7831 mL | 9.4579 mL | |
10 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7289 mL | |
20 mM | 0.0946 mL | 0.4729 mL | 0.9458 mL | 2.3645 mL | |
50 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 mL | |
100 mM | 0.0189 mL | 0.0946 mL | 0.1892 mL | 0.4729 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CPI-169 racemate 1450655-76-1 Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase CPI 169 CPI169 racemate CPI-169 CPI169 CPI 169 racemate Inhibitor inhibitor inhibit