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Luminespib(AUY922)
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。
Luminespib(AUY922)图片
CAS NO:747412-49-3
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 in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
NVP-AUY922
Luminespib
产品介绍

生物活性

Luminespib (AUY922)是一种高效的HSP90抑制剂,其对HSP90α/β的IC50为13 nM /21 nM,对HSP90家族成员GRP94和TRAP-1具有稍弱的作用,与任何HSP90配体均可紧密结合。体外研究时NVP-AUY922抑制多种人类肿瘤细胞系的增殖,GI50平均值为9 nM。NVP-AUY922作用于胃癌细胞时IC50值为2到40 nM。NVP-AUY922作用于BEAS-2B细胞IC50为28.49 nM。


化学数据

分子量465.54
分子式C26H31N3O5
CAS号747412-49-3
纯度99.98%
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41 human NSCLC cell lines in vitro: A427, A549, Calu-1, Calu-3, Calu-6, H23, H226, H358, H460, H520, H522, H596, H810, H838, H1155, H1299, H1385, H1435, H1437, H1563, H1568, H1581, H1651, H1703, H1755, H1793, H1836, H1944, H1975, H2030, H2073, H2106, H2110, H2135, H2172, H2228, H2286, H2342, H2405, HCC827, and SHP77
方法Proliferation assays
Cells were seeded in duplicate at 5,000-10,000 cells per well. The day after plating (day 1), NVP-AUY922 was added at 1 μM and 2-fold dilutions over 12 concentrations. Data were compared to untreated controls. Cells were counted on the day drug was added and five days later and these two counts were compared. Cells were harvested by trypsinization and counted immediately using a Coulter Z2 particle counter (Beckman Coulter Inc, Fullerton, CA). Percent growth inhibition, defined as 100 × (1 - [generations in treated wells/generations in untreated controls]) was determined. Experiments were performed in duplicate. Error bars represent standard error for each experiment. Non-linear curve fitting was performed by fitting curves to data points using the Proc NLIN function in SAS for Windows version 9.2 (SAS Institute, Inc., Cary, NC) using a basic four-parameter sigmoid model. IC50 (concentration needed to prevent 50% of cell population doublings) and IC100 (complete inhibition of proliferation) were the summary outcome measures interpolated from the resulting curves.
浓度0~100nM
处理时间5 days

动物实验
动物模型BT-474 Breast cancer xenograft model Tumor Xenografts
配制formulated in 60 mM lactic acid or 2.5% ethanol, 20% 50 mM tartaric acid, 77.5% (5% glucose in water [D5W] containing 1% Tween 80) vol/vol
剂量25 to 58 mg/kg once per week
给药处理intravenous

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 mM2.148 mL10.7402 mL21.4804 mL
5 mM0.4296 mL2.148 mL4.2961 mL
10 mM0.2148 mL1.074 mL2.148 mL