Luminespib

SKU: orb1306830

特色

描述

Luminespib (VER-52296) is a potent and selective HSP90 inhibitor targeting both HSP90α and HSP90β isoforms. It demonstrates significant antitumor activity in preclinical studies, including in vitro cell-based assays and in vivo models for head and neck squamous cell carcinoma and other malignancies.

研究领域

Cardiovascular Research, Cell Biology, Immunology & Inflammation

图片与验证

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Item 1 of 1

关键属性

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CAS 号	747412-49-3
MW	465.5
纯度	>99%
分子式	C₂₆H₃₁N₃O₅
SMILES	CCNC(=O)c1noc(c1-c1ccc(CN2CCOCC2)cc1)-c1cc(C(C)C)c(O)cc1O
靶点	HSP (Heat shock protein)
溶解性	Soluble in DMSO (up to 25 mg/ml)

生物活性

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靶点 IC50	HSP90 α:7.8 nM (cell free)\|TRAP1:85 nM\|HSP90 β:21 nM (cell free)\|GRP94:535 nM
体内	METHODS: To study the effect on H. pylori-associated gastritis, Patchouli alcohol (5-20 mg/kg) was administered orally to H. pylori infected mice once daily for two weeks. RESULTS: Patchouli alcohol treatment increased SH-NP content and CAT activity and significantly protected the gastric mucosa from H. pylori-induced damage.
体外	METHODS: H. pylori infected GES-1 cells were treated with Patchouli alcohol (5-20 µg/mL) for 24 h. Apoptosis was detected by flow cytometry. RESULTS: Patchouli alcohol treatment significantly reduced H. pylori-induced apoptosis. METHODS: H. pylori-infected GES-1 cells were treated with Patchouli alcohol (5-20 µg/mL) for 24 h. Cytokine levels were measured by ELISA. RESULTS: Treatment with 5-20 µg/mL Patchouli alcohol significantly reduced the production of TNF-α and MCP-1.
细胞研究	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 .
动物研究	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 .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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NVP-AUY922; VER-52296

相似产品

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Luminespib mesylate [orb1740720]
CAS 号：
747412-64-2
MW:
479.57
分子式：
C₂₇H₃₃N₃O₅
可选规格： 50 mg, 100 mg, 25 mg
NVP-AUY922 [orb1224082]
纯度：
>98% (HPLC)
CAS 号：
747412-49-3
MW:
465.5414
分子式：
C₂₆H₃₁N₃O₅
可选规格： 5 mg, 25 mg, 50 mg, 100 mg, 200 mg, 10 mg, 500 mg, 1 g

质量保证

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化合物标识

PubChem CID

135539077 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

Mohammed Fulayyih Aloufi et al. Luminespib protects against dexamethasone-induced hepatic, vascular, and metabolic abnormalities in rats Naunyn Schmiedebergs Arch Pharmacol, (2025)

PubMed: 41273382

CAS 号：	747412-64-2
MW:	479.57
分子式：	C₂₇H₃₃N₃O₅

纯度：	>98% (HPLC)
CAS 号：	747412-49-3
MW:	465.5414
分子式：	C₂₆H₃₁N₃O₅

Luminespib

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Luminespib mesylate [orb1740720]

NVP-AUY922 [orb1224082]

质量保证

化合物标识

关键属性

实验方案信息

可选规格