BIIB021

目录号 M1679 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

BIIB021是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，K_i和EC50分别为1.7 nM和38 nM。

别名：CNF2024

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL	¥ 570	中国库存现货
5mg	¥ 500	中国库存现货
10mg	¥ 720	中国库存现货
50mg	¥ 1800	中国库存现货
100mg	¥ 2700	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.72%
COA
MSDS
H-NMR
LC/MS

产品信息

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，K_i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。

产品使用成果展示

	数据来源	Frontiers in Microbiology (2015). Figure 3. BIIB021
	方法	cell apoptosis assay
	细胞系/动物模型	NK cell lines
	浓度	5 μM
	处理时间	96 h
	实验结果	BIIB021 increased early apoptotic cells,defined as those positive forannexin V and negative for 7 AAD staining, in the two T cell lines, SNT16 and Jurkat, and two NK cell lines, SNK6 and KHYG1.

实验参考

体外实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	318.76
分子式	C14H15ClN6O
CAS号	848695-25-0
溶解性（25°C）	DMSO 60 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.1372 mL	15.6858 mL	31.3716 mL
5 mM	0.6274 mL	3.1372 mL	6.2743 mL
10 mM	0.3137 mL	1.5686 mL	3.1372 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m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K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Dickson et al. Ann Oncol. Phase II study of the HSP90-inhibitor BIIB021 in gastrointestinal stromal tumors.

[2] Xu et al. Drug Metab Dispos. In vitro metabolism of BIIB021, an inhibitor of heat shock protein 90, in liver microsomes and hepatocytes of rats, dogs, and humans and recombinant human cytochrome P450 isoforms.

[3] Dakappagari et al. Biomarkers. An investigation into the potential use of serum Hsp70 as a novel tumour biomarker for Hsp90 inhibitors.

[4] Zhang et al. Int J Cancer. BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance.

[5] Lundgren K, et al. Mol Cancer Ther. BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90.

获取最新目录册

其他相关的HSP产品
Hsp70-derived octapeptide Hsp70-derived octapeptide 是热休克蛋白70 (Hsp70) C 末端保守的八肽，可与 TPR 域相互作用。
p5 Ligand for Dnak and DnaJ p5 Ligand for Dnak and DnaJ 是一种九肽，对应于线粒体天冬氨酸氨基转移酶前序列的 23 个残基部分的主要结合位点。
Tertomotide hydrochloride Tertomotide hydrochloride是一种由16个氨基酸组成的多肽，包含来自人类端粒酶逆转录酶（TERT）的序列。Tertomotide可以穿透细胞，与HSP70和HSP90相互作用，同时能抑制淀粉样蛋白β和tau，以及抑制大脑内衰老相关信号传达途径，可用于衰老和阿尔茨海默病的相关研究。
BMS-986263 BMS-986263是一种小干扰RNA（siRNA），能靶向Hsp47，可用于特发性肺纤维化(IPF)的相关研究。
AT-533 AT-533 是一种有效的 Hsp90 和 HSV 抑制剂。

信号通路

产品类型