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BIIB021
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIIB021图片
CAS NO:848695-25-0
包装:5mg, 10mg, 50mg, 100mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mM*1mL电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
CNF2024
产品介绍

生物活性

BIIB021是一种口服有效的,全部人工合成的,小分子HSP90抑制剂,Ki和EC50分别为1.7 nM和38 nM。BIIB021 结合到Hsp90的ATP结合袋中, 干涉Hsp90伴侣功能, 导致客户蛋白降解和肿瘤生长受抑制。BIIB021抑制肿瘤细胞 (BT474, MCF-7, N87, HT29, H1650, H1299, H69和H82) 增殖, IC50为0.06-0.31 μM。BIIB021诱导Hsp90客户蛋白包括HER-2, AKT, 和Raf-1的降解,以及 正向调节Hsp70 和Hsp27。


化学数据

分子量318.76
分子式C14H15ClN6O
CAS号848695-25-0
纯度99.72%
溶解性(25°C)DMSO 60 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系N87, MCF-7 and BT474 cell lines
方法Cell Proliferation Assay.
A modified tetrazolium salt assay was used to measure the inhibition of tumor cell growth. Cells were added to 96-well plates and propagated for 24 h before compound addition. The compound was serially diluted and added at a concentration range of 3 to 1,000 nmol/L to the plated cells. DMSO (0.03-0.003%) was included as a vehicle control. Cells were incubated in the presence of compound for 5 days. 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; Promega) were 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 gave rise to a soluble formazan product that was secreted into the culture medium. After 4 h incubation, the formazan product was quantitated spectrophotometrically at a wavelength of 490 nm. Data were acquired using SOFTmaxPRO software, and 100% viability was 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 was calculated from the A490 values as follows: % viability = (A490 nm sample / A490 nm DMSO-treated cells × 100). The IC50 was defined as the concentration that gave rise to 50% inhibition of cell viability.
浓度3 ~ 1000 nM
处理时间5 days

动物实验
动物模型nude mice bearing N87 stomach carcinoma tumors xenograft model
配制
剂量31, 62.5, and 125 mg/kg, once daily, from Monday to Friday, for 5 weeks
给药处理orally

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM3.1372 mL15.6858 mL31.3716 mL
5 mM0.6274 mL3.1372 mL6.2743 mL
10 mM0.3137 mL1.5686 mL3.1372 mL