Luminespib (AUY922) 芦米司匹；鲁奈司匹

目录号 M1762 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

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。

别名：NVP-AUY922; Luminespib

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL in DMSO	¥ 480	中国库存现货
5mg	¥ 400	中国库存现货
10mg	¥ 560	中国库存现货
50mg	¥ 1880	中国库存现货
100mg	¥ 3120	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： 99.80%
COA
MSDS
H-NMR
HPLC

产品信息

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。

产品使用成果展示

	数据来源	PLoS One (2017). Figure 1. AUY922
	方法	FACS analysis
	细胞系/动物模型	ATC cells
	浓度	2.5, 5, 7.5, and 10 μM
	处理时间	24, 48, and 72 h
	实验结果	Taken together, our results demonstrate that AUY922, compared with other hsp90 inhibitors, potently results in growth inhibition and death of ATC cells.

实验参考

体外实验*
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

*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	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

*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	465.54
分子式	C26H31N3O5
CAS号	747412-49-3
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	2.148 mL	10.7402 mL	21.4804 mL
5 mM	0.4296 mL	2.148 mL	4.2961 mL
10 mM	0.2148 mL	1.074 mL	2.148 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] Okui T et al. Curr Cancer Drug Targets. Novel HSP90 Inhibitor NVP-AUY922 enhances the anti-tumor effect of temsirolimus against oral squamous cell carcinoma.

[2] Moser C et al. Anticancer Res. Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer.

[3] Best OG et al. Leuk Lymphoma. Heat shock protein-90 inhibitor, NVP-AUY922, is effective in combination with fludarabine against chronic lymphocytic leukemia cells cultured on CD40L-stromal layer and inhibits their activated/proliferative phenotype.

[4] Walsby E et al. Oncotarget. The Hsp90 inhibitor NVP-AUY922-AG inhibits NF-κB signaling, overcomes microenvironmental cytoprotection and is highly synergistic with fludarabine in primary CLL cells.

[5] Zaidi S et al. PLoS One. The HSP90 inhibitor NVP-AUY922 radiosensitizes by abrogation of homologous recombination resulting in mitotic entry with unresolved DNA damage.

[6] Ueno T et al. Lung Cancer. Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer.

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