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Luminespib

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Purity:99.25%

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COA HNMR HPLC

Luminespib

Catalog No. T1989Cas No. 747412-49-3

Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay).

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Pack Size	Price	Availability
5 mg	$52	In Stock
10 mg	$74	In Stock
25 mg	$148	In Stock
50 mg	$233	In Stock
100 mg	$382	In Stock
200 mg	$569	In Stock
500 mg	$917	In Stock
1 mL x 10 mM (in DMSO)	$57	In Stock

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Product Introduction

Bioactivity

Description	Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay).
In vitro	Luminespib (NVP-AUY922) potently inhibits HSP90 (Kd = 1.7 nmol/L) and proliferation of human tumor cells with GI50 values of approximately 2 to 40 nmol/L, inducing G(1)-G(2) arrest and apoptosis [1]. In 11 human gastric cancer cell lines, The IC50 values of NVP-AUY922 fell in the nanomolar range of 2–40 nM. The IC50 values for the cell lines NCI-N87 and SNU-216, cells with HER-2 amplification, were 3.23 nM and 11.99 nM, respectively [2]. NVP-AUY922 inhibited the proliferation of oral squamous cell carcinoma cells in vitro. NVP-AUY922 caused degradation of client protein inducing ErbB2, p-Akt, p-S6, HIF1-α and VEGF and up-regulation of HSP70 in HSC-2 oral squamous cell carcinoma [3].
In vivo	Daily dosing of NVP-AUY922 (50 mg/kg i.p. or i.v.) to athymic mice generated peak tumor levels at least 100-fold above cellular GI(50). This produced statistically significant growth inhibition and/or regressions in human tumor xenografts with diverse oncogenic profiles: BT474 breast tumor treated/control, 21%; A2780 ovarian, 11%; U87MG glioblastoma, 7%; PC3 prostate, 37%; and WM266.4 melanoma, 31% [1]. Luminespib was administered at 50 mg/kg daily i.p. to athymic mice bearing HCT116 human colon carcinoma xenografts. The rate of tumor growth was significantly inhibited by Luminespib administration, and treated tumor weights measured at day 12 were 49.8% of the control values [4].
Cell Research	Cell lines were grown in DMEM/10% FCS, 2 mmol/L glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines were free of Mycoplasma. Cell proliferation was determined using the sulforhodamine B (SRB) assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 was the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Cell cycle analysis was as described. Active caspase-3/7 was measured using a homogenous caspase assay kit [1].
Animal Research	In vivo, pharmacokinetic studies in female NCr athymic mice bearing WM266.4 human melanoma xenografts were essentially as described. NVP-AUY922 was dissolved in DMSO and diluted in sterile saline/Tween 20. A single dose of 50 mg/kg NVP-AUY922 was given i.v. or i.p. and groups of three animals were taken at intervals for pharmacokinetic analyses [1].
Alias	AUY922, VER-52296, NVP-AUY922

Chemical Properties

Molecular Weight	465.54
Formula	C26H31N3O5
Cas No.	747412-49-3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 16.67 mg/mL (35.8 mM)

5% DMSO+95% Saline: 4.3 mg/mL (9.24 mM, precipitation)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 29 mg/mL (62.3 mM)

Solution Preparation Table

Ethanol/5% DMSO+95% Saline

	1mg	5mg	10mg	50mg
1 mM	2.1480 mL	10.7402 mL	21.4804 mL	107.4022 mL
5 mM	0.4296 mL	2.1480 mL	4.2961 mL	21.4804 mL

Ethanol

	1mg	5mg	10mg	50mg
10 mM	0.2148 mL	1.0740 mL	2.1480 mL	10.7402 mL
20 mM	0.1074 mL	0.5370 mL	1.0740 mL	5.3701 mL
50 mM	0.0430 mL	0.2148 mL	0.4296 mL	2.1480 mL
100 mM	0.0215 mL	0.1074 mL	0.2148 mL	1.0740 mL

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