化合物BIIB-021 T2286
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 |
---|---|---|---|
5 mg | 848695-25-0 | ¥455.00 | 询底价 |
200 mg | 848695-25-0 | ¥3,950.00 | 询底价 |
1 mg | 848695-25-0 | ¥198.00 | 询底价 |
100 mg | 848695-25-0 | ¥2,650.00 | 询底价 |
25 mg | 848695-25-0 | ¥1,130.00 | 询底价 |
10 mg | 848695-25-0 | ¥663.00 | 询底价 |
50 mg | 848695-25-0 | ¥1,730.00 | 询底价 |
1 mL | 848695-25-0 | ¥497.00 | 询底价 |
500 mg | 848695-25-0 | ¥6,330.00 | 询底价 |
Product Introduction
Bioactivity
英文名: BIIB021
描述: 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。
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)
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.
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。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 31.9 mg/mL (100 mM)
关键字: Heat shock proteins | BIIB021 | Autophagy | HSP | inhibit | CNF-2024 | CNF 2024 | Inhibitor
相关产品: Rifabutin | TRC051384 | Pimitespib | JG-98 | Shepherdin 79-87 acetate | PROTAC Hsp90α degrader 1 | MKT-077 | HSP27 inhibitor J2 | NDNA4 | Alvespimycin
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Autophagy Compound Library | Exosome Compound Library | Target-Focused Phenotypic Screening 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