Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCF642 (AC1LYELL) 是蛋白质二硫键异构酶抑制剂(IC50:2.9 μM)。它在多发性骨髓瘤细胞中引起急性内质网应激,并伴随凋亡诱导的钙释放,表现出广泛的抗多发性骨髓瘤作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,710 | 现货 | ||
100 mg | ¥ 5,330 | 现货 | ||
500 mg | ¥ 10,900 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 619 | 现货 |
产品描述 | CCF642 (AC1LYELL) is a novel PDI-inhibiting compound with antimyeloma activity. |
靶点活性 | PDI:2.9 μmol/L |
体外活性 | In vitro, CCF642 inhibits PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. Computational modeling suggests a novel covalent binding mode in active-site CGHCK motifs. CCF642 causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release[1]. |
体内活性 | CCF642 displays potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolongs the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib[1]. |
激酶实验 | Inhibition of CB-839 on rHu-GAC: The enzymatic activity is measured in assay buffer containing 50 mM Tris-Acetate pH 8.6, 150 mM K2HPO4 , 0.25 mM EDTA, 0.1 mg/mL bovine serum albumin, 1 mM DTT, 2 mM NADP+ and 0.01% Triton X-100. To measure inhibition, the inhibitor (prepared in DMSO) is first pre-mixed with glutamine and glutamate dehydrogenase (GDH) and reactions are initiated by the addition of rHu-GAC. Final reactions contains 2 nM rHu-GAC, 10 mM glutamine, 6 units/mL GDH and 2% DMSO. Generation of NADPH is monitored by fluorescence (Ex340/Em460 nm) every minute for 15 minutes on a SpectraMax M5e plate reader. Relative fluorescence units (RFU) are converted to units of NADPH concentration (μM) using a standard curve of NADPH. Each assay plate incorporates control reactions that monitores the conversion of glutamate (1 to 75 μM) plus NADP+ to α-ketoglutarate plus NADPH by GDH. Under these assay conditions, up to 75 μM glutamate is stoichiometrically converts to α-ketoglutarate/NADPH by GDH. Initial reaction velocities are calculated by fitting the first 5 minutes of each progress curve to a straight line. Inhibition curves are fitted to a four-parameter dose response equation of the form: % activity = Bottom + (Top-Bottom)/(1+10^((LogIC50-X)*HillSlope)). |
别名 | AC1LYELL |
分子量 | 378.45 |
分子式 | C15H10N2O4S3 |
CAS No. | 346640-08-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.6 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6424 mL | 13.2118 mL | 26.4236 mL | 66.0589 mL |
5 mM | 0.5285 mL | 2.6424 mL | 5.2847 mL | 13.2118 mL | |
10 mM | 0.2642 mL | 1.3212 mL | 2.6424 mL | 6.6059 mL | |
20 mM | 0.1321 mL | 0.6606 mL | 1.3212 mL | 3.3029 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。
CCF642 346640-08-2 Others calcium Inhibitor PDI apoptosis isomerases disulfide CCF 642 myeloma AC1LYELL protein multiple release CCF-642 stress inhibit anti-multiple inhibitor