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BIIB021 {[allProObj[0].p_purity_real_show]}

货号：A615310 同义名： CNF2024

BIIB021是一种口服有效的 HSP90 抑制剂，Ki 值和 EC50 值分别为 1.7 nM 和 38 nM，具有较强的抗癌活性，用于癌症治疗研究。

BIIB021 化学结构 CAS号：848695-25-0
BIIB021 化学结构
CAS号：848695-25-0
BIIB021 3D分子结构
CAS号：848695-25-0
BIIB021 化学结构 CAS号：848695-25-0
BIIB021 3D分子结构 CAS号：848695-25-0
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BIIB021 纯度/质量文件 产品仅供科研

货号：A615310 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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BIIB021 生物活性

描述 HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. BIIB021 is a synthetic inhibitor of HSP90 with Ki value of 1.7nM (measured by Hsp90 binding assay). All the protein level the client protein tested, including HER-2, IGF-I receptor, AKT, Raf-1, Cdk4, Cdk6 and progesterone receptor, was decreased and the protein level of Hsp90α and Hsp70 was increased due to the inhibition of HSP90 by BIIB021 at concentration>100nM for 24h in MCF-7 cells. And this effect on the client protein can also be observed in the BT474 breast tumor xenograft model at 6h post dose of 30-120mg/kg BIIB021. The antiproliferation activity of BIIB021 can be observed in various cell lines, including BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82, with IC50 values ranging in 0.06-0.31μM. The antitumor effect of oral administration of BIIB021, five days per week for 4 weeks or 5 weeks, can be observed in several models, as tumor growth inhibition can be achieved by 87% at dose of 125mg/kg in N87 xenografts, 94% at dose of 120mg/kg in BT474 xenografts, 85% at dose of 120mg/kg in CWR22 xenografts, 70% at dose of 75mg/kg (BID) in U87 xenografts, 67% at dose of 124mg/kg in SKOV3 cells and 51% at dose of 124mg/kg in Panc-1 xenografts[1].
作用机制 BIIB021 exhibits competitive binding with geldanamycin and binds the ATP pocket of Hsp90.[1]

BIIB021 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
human BT474 cells Function assay Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells, IC50=0.14 μM 20608738
MCF7 cells Function assay Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2, EC50=38 nM 22938030
NCI-H1299 cells Function assay 12 h Reduction in oxygen consumption rate in human NCI-H1299 cells incubated for 12 hrs 25383915
sf9 cells Function assay 3 h Binding affinity to human N-terminal polyHis-tagged HSP90beta (D9 to E236) expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay, Ki=4 nM 24332488

BIIB021 动物研究

Dose Nude Mice[1] (p.o.): 30 mg/kg - 150 mg/kg
Administration p.o.
Pharmacokinetics
Animal Mice[1]
Dose 75 mg/kg
Administration p.o.
AUC0→last 2.3 μg·h/ml
T1/2 0.5 h
Tmax 5 min
Cmax 10.2 μg/ml

BIIB021 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00412412 Breast Cancer Phase 1 Completed - United States, Florida ... 展开 >> Research Site Tampa, Florida, United States, 33612 United States, New York Research Site New York, New York, United States, 10021 United States, Texas Research site Houston, Texas, United States, 77030 收起 <<
NCT00345189 Tumors Lympho... 展开 >>ma 收起 << Phase 1 Completed - United States, Arizona ... 展开 >> Research site Scottsdale, Arizona, United States, 85258 United States, Connecticut Research site New Haven, Connecticut, United States, 06520 United States, Texas Research site San Antonio, Texas, United States, 78245 United Kingdom Research site Sutton, Surrey, United Kingdom, SM2 5PT 收起 <<
NCT00344786 B-Cell Chronic Lymphocytic Leu... 展开 >>kemia 收起 << Phase 1 Terminated(Sponsor's decision) - United States, California ... 展开 >> Research Site San Diego, California, United States, 92093 United States, New York Research site New York, New York, United States, 10021 United States, Texas Research site Houston, Texas, United States, 77030 收起 <<

BIIB021 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.14mL

0.63mL

0.31mL

15.69mL

3.14mL

1.57mL

31.37mL

6.27mL

3.14mL

BIIB021 技术信息

CAS号848695-25-0
分子式C14H15ClN6O
分子量 318.76
SMILES Code COC1=C(C)C(CN2C=NC3=C2N=C(N)N=C3Cl)=NC=C1C
MDL No. MFCD15528939
别名 CNF2024
运输蓝冰
InChI Key QULDDKSCVCJTPV-UHFFFAOYSA-N
Pubchem ID 16736529
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 45 mg/mL(141.17 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

Tags: BIIB021 | 848695-25-0 | CNF2024 | BIIB 021 | BIIB-021 | CNF 2024 | CNF-2024 | HSP90 Inhibitor | Cell Cycle/DNA Damage | Metabolic Enzyme/Protease | Autophagy | HSP | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | BIIB021 纯度/质量文件 | BIIB021 生物活性 | BIIB021 细胞研究 | BIIB021 动物研究 | BIIB021 临床数据 | BIIB021 实验方案 | BIIB021 技术信息

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