Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BIIB021 (CNF2024) 是一种可口服的合成 HSP90 抑制剂,Ki 值和EC50值分别为 1.7 nM 和 38 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 198 | 现货 | ||
5 mg | ¥ 455 | 现货 | ||
10 mg | ¥ 663 | 现货 | ||
25 mg | ¥ 1,130 | 现货 | ||
50 mg | ¥ 1,730 | 现货 | ||
100 mg | ¥ 2,650 | 现货 | ||
200 mg | ¥ 3,950 | 现货 | ||
500 mg | ¥ 6,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 497 | 现货 |
产品描述 | BIIB021 (CNF2024) is an orally-available, fully synthetic inhibitor of HSP90(Ki=1.7 nM, EC50=38 nM). |
靶点活性 | HSP90:1.7 nM(Ki) |
体外活性 | 在多种移植瘤模型中,口服BIIB021能够有效抑制肿瘤的生长.在L540cy肿瘤中,BIIB021(120 mg/kg ),能够抑制细胞的增殖. |
体内活性 | 在多种肿瘤细胞中(IC50=0.06-0.31 μM),BIIB021能够抑制细胞生长,如BT474,MCF-7,N87,HT29,H1650,H1299,H69和H82。在霍奇金淋巴瘤细胞中(IC50=0.24-0.8 μM),BIIB021抑制细胞增殖 ,如KM-H2,L428,L540,L540cy,L591,L1236和DEV。BIIB021诱导Hsp90蛋白(包括HER-2,Akt和Raf-1)的降解以及热休克蛋白Hsp70和Hsp27的上调表达。 |
激酶实验 | Hsp90 Binding Assay: For fluorescence polarization competition measurements, the FITC-geldanamycin probe (20 nM) is reduced with 2 mM TCEP at room temperature for 3 hours, after which the solution is aliquoted and stored at -80 °C until used. Recombinant human Hsp90α (0.8 nM) and reduced FITC-geldanamycin (2 nM) are incubated in a 96-well microplate at room temperature for 3 hours in the presence of assay buffer containing 20 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 2 mM DTT, 0.1 mg/mL BGG, and 0.1% (v/v) CHAPS. Following this preincubation, BIIB021 in 100% DMSO is then added to final concentrations of 0.2 nM to 10 μM (final volume 100 μL, 2% DMSO). The reaction is incubated for 16 hours at room temperature and fluorescence is then measured in an Analyst plate reader, excitation = 485 nm, emission = 535 nm. High and low controls contained no BIIB021 or no Hsp90, respectively. The data are fit to a four-parameter curve and IC50 is generated. |
细胞实验 | A modified tetrazolium salt assay is used to measure the IC50. Tumor cells are added to 96-well plates and propagated for 24 hours before BIIB021 addition. BIIB021 is added to the plated cells. DMSO (0.03-0.003%) is included as a vehicle control. After incubation phenazine methosulfate (stock concentration 1 mg/mL) and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (stock concentration 2 mg/mL) are mixed at a ratio of 1:20 and added to each well of a 96-well plate. Reduction of 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt gives rise to a soluble formazan product that is secreted into the culture medium. After 4 hours incubation, the formazan product is quantitated spectrophotometrically at a wavelength of 490 nm. Data are acquired using SOFTmaxPRO software, and 100% viability is defined as the A490 of DMSO-treated cells stained with 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (the mean A490 of cells treated with DMSO at a range of 0.03-0.003%). Percent viability of each sample is calculated from the A490 values as follows: % viability = (A490 nm sample / A490 nm DMSO-treated cells × 100). The IC50 is defined as the concentration that gives rise to 50% inhibition of cell viabilit(Only for Reference) |
别名 | BIIB 021, CNF2024, BIIB-021 |
分子量 | 318.76 |
分子式 | C14H15ClN6O |
CAS No. | 848695-25-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31.9 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1372 mL | 15.6858 mL | 31.3716 mL | 78.4289 mL |
5 mM | 0.6274 mL | 3.1372 mL | 6.2743 mL | 15.6858 mL | |
10 mM | 0.3137 mL | 1.5686 mL | 3.1372 mL | 7.8429 mL | |
20 mM | 0.1569 mL | 0.7843 mL | 1.5686 mL | 3.9214 mL | |
50 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5686 mL | |
100 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7843 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。
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