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BIIB021

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产品编号 T2286Cas号 848695-25-0
别名 CNF2024, BIIB-021, BIIB 021

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。

BIIB021
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BIIB021

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纯度: 99.82%
产品编号 T2286 别名 CNF2024, BIIB-021, BIIB 021Cas号 848695-25-0

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。

规格价格库存数量
1 mg
¥ 198
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5 mg
¥ 455
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10 mg
¥ 663
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25 mg
¥ 1,130
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50 mg
¥ 1,730
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100 mg
¥ 2,650
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200 mg
¥ 3,950
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500 mg
¥ 6,330
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1 mL x 10 mM (in DMSO)
¥ 497
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产品介绍

生物活性
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CNF2024, BIIB-021, BIIB 021
化学信息
分子量318.76
分子式C14H15ClN6O
CAS No.848695-25-0
SmilesCOc1c(C)cnc(Cn2cnc3c(Cl)nc(N)nc23)c1C
密度1.50 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 45 mg/mL (141.17 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.1372 mL15.6858 mL31.3716 mL156.8578 mL
5 mM0.6274 mL3.1372 mL6.2743 mL31.3716 mL
10 mM0.3137 mL1.5686 mL3.1372 mL15.6858 mL
20 mM0.1569 mL0.7843 mL1.5686 mL7.8429 mL
50 mM0.0627 mL0.3137 mL0.6274 mL3.1372 mL
100 mM0.0314 mL0.1569 mL0.3137 mL1.5686 mL

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计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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