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Luminespib

Catalog No. T1989 CAS 747412-49-3

Synonyms: AUY922, VER-52296, NVP-AUY922

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Luminespib, CAS 747412-49-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 233.00
100 mg	In stock	$ 382.00
200 mg	In stock	$ 569.00
500 mg	In stock	$ 917.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 99.25%

Purity: 98.97%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay).
Targets&IC50	HSP90 β:21 nM (cell free), HSP90 α:7.8 nM (cell free)
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].

Synonyms	AUY922, VER-52296, NVP-AUY922
Molecular Weight	465.54
Formula	C26H31N3O5
CAS No.	747412-49-3

Storage

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

Solubility Information

DMSO: 86 mg/mL (184.7 mM)

Ethanol: 29 mg/mL (62.3 mM)

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

References and Literature

1. Eccles, Suzanne A., et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Research (2008), 68(8), 2850-2860. 2. Lee KH, et al. Antitumor activity of NVP-AUY922, a novel heat shock protein 90 inhibitor, in human gastric cancer cells is mediated through proteasomal degradation of client proteins. Cancer Sci. 2011 Jul;102(7):1388-95. 3. Okui T, et al. Antitumor effect of novel HSP90 inhibitor NVP-AUY922 against oral squamous cell carcinoma. Anticancer Res. 2011 Apr;31(4):1197-204. 4. Brough PA, et al. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem. 2008 Jan 24;51(2):196-218. 5. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent[J]. Scientific reports. 2018 Oct 8;8(1):14969. 6. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors[J]. European Journal of Medicinal Chemistry. 2020: 113030.

Citations

1. He C X, Lv Y, Guo M, et al. Complex Crystal Structure Determination of Hsp90 N-NVP-AUY922 and In Vitro Anti-NSCLC Activity of NVP-AUY922. Frontiers in oncology. 2022, 12: 847556-847556. 2. He C X, Lv Y, Guo M, et al. Complex Crystal Structure Determination of Hsp90N-NVP-AUY922 and In Vitro Anti-NSCLC Activity of NVP-AUY922. Frontiers in oncology. 2022, 12 3. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. European Journal of Medicinal Chemistry,. 2021 Feb 15;212:113030 4. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Scientific Reports. 2018 Oct 8;8(1):14969 5. Li J, Han X, Sun M, et al.Caspase-9 inhibition triggers Hsp90-based chemotherapy-mediated tumor intrinsic innate sensing and enhances antitumor immunity.Journal for Immunotherapy of Cancer.2023, 11(12).

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Metabolism Compound Library HIF-1 Signaling Pathway Compound Library ReFRAME Related Library Anti-Breast Cancer Compound Library Oxidation-Reduction Compound Library

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Keywords

Luminespib 747412-49-3 Apoptosis Autophagy Cytoskeletal Signaling Metabolism HSP VER 52296 AUY922 VER-52296 Inhibitor AUY-922 Heat shock proteins VER52296 AUY 922 inhibit NVP-AUY922 NVP-AUY 922 NVP-AUY-922 inhibitor

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