DC Chemicals Limited
China
Product Name: Luminespib (NVP-AUY922)
Price: $300.0/100mg $600.0/250mg $1200.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: NVP-AUY922
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

747412-49-3

747412-49-3 structure

747412-49-3 structure

Name: NVP-AUY922
Chemical Name: luminespib
CAS Number: 747412-49-3
Molecular Formula: C₂₆H₃₁N₃O₅
Molecular Weight: 465.541
Catalog: Biochemical Inhibitor Cytoskeletal Signaling HSP eg HSP90 inhibitor
Create Date: 2018-12-17 18:27:18
Modify Date: 2024-01-07 16:19:11
Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.

Name	luminespib
Synonyms	VER-52296 NVP-AUY-922 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(4-morpholin-4-ylmethylphenyl)isoxazole-3-carboxylic acid ethylamide 5-[2,4-dihydroxy-5-(propan-2-yl)phenyl]-N-ethyl-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxamide 3-Isoxazolecarboxamide, 5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]- LUMINESPIB 5-(2,4-Dihydroxy-5-isopropylphenyl)-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-1,2-oxazole-3-carboxamide 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide NVP-AUY922 AUY 922

Description	Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Cell Cycle/DNA Damage >> HSP Signaling Pathways >> Metabolic Enzyme/Protease >> HSP Research Areas >> Cancer
Target	HSP90α:7.8 nM (IC50) HSP90β:21 nM (IC50) GRP94:535 nM (IC50) TRAP-1:85 nM (IC50)
In Vitro	Luminespib is a potent and selective HSP90 inhibitor, with IC50s and Kis of 21 ± 16, 8.2 ± 0.7 nM against HSP90β and of 7.8 ± 1.8, 9.0 ± 5.0 nM for HSP90α. Luminespib shows weak activity against GRP94 and TRAP-1 wich IC50s of 535 ± 51 nM (Ki, 108 nM) and 85 ± 8 nM (Ki, 53 nM), respectively. Luminespib exhibits inhibitory effect on proliferation of various human tumor cell lines (2.3-49.6 nM), induces cell cycle arrest and apoptosis and depletes client proteins in human cancer cells (80 nM)[1]. Luminespib (100 nM) significantly reduces CD40L fibroblast-induced changes in immunophenotype and STAT3 signaling but with no effect on the viability of chronic lymphocytic leukemia (CLL) cells. Luminespib (500 nM) in combination with fludarabine more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor[2]. Luminespib shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. Luminespib (10 nM) reduces the expression and the epidermal growth factor (EGF)-mediated activation of EGFR and substantially disrupts EGF signaling in terms of diminishing downstream phosphorylation of ERKThr202/Tyr204. Luminespib (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF[3].
In Vivo	Luminespib (50, 75 mg/kg, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11 in human tumor xenografts[2]. Luminespib (50 mg/kg/week, 3×25 mg/kg/week) significantly reduces tumor growth rates and lowers tumor weights in the L3.6pl pancreatic cancer cell-bearing mice model[3].
Cell Assay	Cell lines are grown in DMEM/10% FCS, 2 mM glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines are free of Mycoplasma. Cell proliferation is determined using the 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 is the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Active caspase-3/7 is measured using a homogenous caspase assay kit[1].
Animal Admin	Mice[1] For efficacy studies, human tumor xenografts are established s.c. in athymic mice. WM266.4 cells are also injected i.v. to generate experimental lung metastases and PC3LN3 prostate carcinoma cells are implanted into the prostates of male mice. Dosing by i.p. with Luminespib commences when tumors are well established. Tumor growth is monitored and at study end samples are harvested for analysis[1].
References	[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]. Best OG, et al. 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. Leuk Lymphoma. 2012 Jul 9. [3]. Moser C, et al. Stoeltzing O.Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer. Anticancer Res. 2012 Jul;32(7):2551-61.

Density	1.2±0.1 g/cm3
Boiling Point	640.1±55.0 °C at 760 mmHg
Molecular Formula	C₂₆H₃₁N₃O₅
Molecular Weight	465.541
Flash Point	340.9±31.5 °C
Exact Mass	465.226379
PSA	108.06000
LogP	1.11
Vapour Pressure	0.0±2.0 mmHg at 25°C
Index of Refraction	1.597
Storage condition	-20°C