Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pracinostat (SB939) 是一种组蛋白去乙酰化酶抑制剂,对 HDACs 的IC50值为 40-140 nM,可用于研究癌症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 362 | 现货 | ||
2 mg | ¥ 529 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,570 | 现货 | ||
25 mg | ¥ 2,920 | 现货 | ||
50 mg | ¥ 4,290 | 现货 | ||
100 mg | ¥ 6,150 | 现货 | ||
500 mg | ¥ 12,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,390 | 现货 |
产品描述 | Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors. |
靶点活性 | HDAC1:49 nM, HDAC10:40 nM, HDAC3:43 nM, HDAC5:47 nM, HDAC4:56 nM |
体外活性 | 50 mg/kg SB939选择性刺激CT-116移植瘤组织生长.SB939对SAHA的肿瘤生长抑制率为94%.SB939作用于裸鼠,比SAHA具有更强的药物动力学效果和口服生物有效性.SB939抑制APCmin鼠腺瘤形成和提高血球密度,效果比5-氟尿嘧啶好.SB939作用于肿瘤模型(HCT-116,PC-3,A2780,MV4-11,Ramos),具有抗癌活性和高效性. |
体内活性 | SB939对HDAC的选择性比锌结合的非HDAC酶、受体和离子通道高100倍。SB939可显著抑制HDAC II类同工酶,HDAC4,HDAC5,HDAC7,HDAC9和HDAC10,IC50值范围为40 nM至137 nM,对HDAC6无此作用,其显示的IC50为1008 nM。它显著抑制HDAC IV类酶的HDAC11,IC50为93 nM,但对III类HDACs的SIRT1没有抑制活性。SB939对各种肿瘤细胞系,尤其是白血病细胞和皮肤T细胞淋巴瘤细胞显示出显著的抗增殖活性,IC50值范围从50 nM(H9细胞)至170 nM(HEL92.1.7细胞)。 |
激酶实验 | HDAC enzyme assay: All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2 and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software. |
细胞实验 | Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.(Only for Reference) |
别名 | SB939 |
分子量 | 358.48 |
分子式 | C20H30N4O2 |
CAS No. | 929016-96-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 26 mg/mL (72.5 mM)
DMSO: 67 mg/mL (186.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.7896 mL | 13.9478 mL | 27.8956 mL | 69.7389 mL |
5 mM | 0.5579 mL | 2.7896 mL | 5.5791 mL | 13.9478 mL | |
10 mM | 0.279 mL | 1.3948 mL | 2.7896 mL | 6.9739 mL | |
20 mM | 0.1395 mL | 0.6974 mL | 1.3948 mL | 3.4869 mL | |
50 mM | 0.0558 mL | 0.279 mL | 0.5579 mL | 1.3948 mL | |
DMSO | 100 mM | 0.0279 mL | 0.1395 mL | 0.279 mL | 0.6974 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。
Pracinostat 929016-96-6 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Inhibitor cancer SB939 inhibit SB-939 MBLAC2 SB 939 Histone deacetylases inhibitor