化合物CPI169 T6809
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 1450655-76-1 | ¥3,190.00 | 询底价 |
50 mg | 1450655-76-1 | ¥4,670.00 | 询底价 |
100 mg | 1450655-76-1 | ¥6,650.00 | 询底价 |
2 mg | 1450655-76-1 | ¥663.00 | 询底价 |
10 mg | 1450655-76-1 | ¥1,450.00 | 询底价 |
1 mL | 1450655-76-1 | ¥1,200.00 | 询底价 |
1 mg | 1450655-76-1 | ¥467.00 | 询底价 |
5 mg | 1450655-76-1 | ¥930.00 | 询底价 |
Product Introduction
Bioactivity
英文名: CPI-169 racemate
描述: 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。
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)
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).
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.
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]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 93 mg/mL (175.9 mM)
DMSO : 93 mg/mL (175.9 mM)
关键字: CPI169 racemate | CPI 169 racemate | CPI-169 racemate
相关产品: UNC1079 | BAY1238097 | MI-463 | BAZ1A-IN-1 | SNDX-5613 | ZXH-3-26 | A-485 | Bromosporine | BRD4 Inhibitor-10 | GNE-207
相关库: Anti-Aging Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Reprogramming Compound Library | Preclinical Compound Library | Histone Modification Compound Library | Chromatin Modification Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途