Luminespib (NVP-AUY922)

製品コードS1069 バッチS106910

印刷

化学情報

Chemical Structure Synonyms AUY-922, VER-52296 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H31N3O5
分子量 465.54 CAS No. 747412-49-3
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 93 mg/mL (199.76 mM)
Ethanol 93 mg/mL (199.76 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
in vitro Luminespib (NVP-AUY922) inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. [1] The IC50 values of this compound fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with it does not influence the expression of HSP90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. It increases the binding of HSP70 to HSP90. This compound causes p23 dissociation from the HSP90 complex and can then recruit HSP70 to the HSP90 complex. [1] After the treatment with Luminespib, expression of receptor tyrosine kinases including VEGFR1, 2, 3 and PDGFRɑ is decreased. A decrease is also noticed in the expression of Akt and phospho-Akt. Meanwhile, treatment with it causes decreased expression of HER-2 in NCI-N87 cells. Its treatment results in binding of HSP90 to client proteins and setting them up as targets for degradation by the proteasome. It can influence cell growth by affecting multiple signaling pathways. In addition, treatment with the proteasome inhibitor, MG132, restores expression of thymidylate synthase, which is decreased by this compound. Luminespib increases the expression of cleaved caspase-3 leading to apoptosis in HSC-2 cells.[1]
in vivo Luminespib (NVP-AUY922) causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model. [2] In BT474, it shows complete loss of ERBB2 and substantial depletion of ERα, in addition to reductions in CDK4 and phospho-ERK1/2. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
Luminespib (NVP-AUY922) is dissolved in DMSO at a concentration of 10 mM. It is assessed against HSP90α, HSP90β, GRP94, TRAP-1, HSP72, and topoisomerase II. Profiling against a panel of kinases has been carried out and screening against a panel of additional enzymes and receptors is performed at Cerep.
細胞アッセイ 細胞株 Human gastric cancer cells NCI-N87
濃度 1 μM
反応時間 3 days
実験の流れ Human gastric cancer cells NCI-N87 (5-7 ×103 in 50 μL/well) are seeded in 96-well plates and incubated at 37 °C for 24 hours, followed by treatment with Luminespib (NVP-AUY922) for 1-3 days at 37 °C. After treatment, the cells are assayed by MTT method and analyzed by microplate reader.
動物実験 動物モデル Female NCr athymic mice bearing WM266.4 human melanoma xenografts
投薬量 50 mg/kg
投与方法 Administered via i.v. or i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/21453385/
  • https://pubmed.ncbi.nlm.nih.gov/21508365/
  • https://pubmed.ncbi.nlm.nih.gov/18413753/

カスタマーフィードバック

Data from [J Biol Chem, 2013, 288(23), 16308-20]

, 2011, Dr. Swee Sharp and Professor Paul Workman from Cancer Research UK

Data from [Data independently produced by , , Proc Natl Acad Sci USA, 2014, 111(15): E1528–37 ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
TBK1 is a signaling hub in coordinating stress-adaptive mechanisms in head and neck cancer progression [ Autophagy, 2025, 1-23.] PubMed: 40114316
Targeting HSP90 with Ganetespib to Induce CDK1 Degradation and Promote Cell Death in Hepatoblastoma [ Cancers (Basel), 2025, 17(8)1341] PubMed: 40282517
Individualized Pooled CRISPR/Cas9 Screenings Identify CDK2 as a Druggable Vulnerability in a Canine Mammary Carcinoma Patient [ Vet Sci, 2025, 12(2)183] PubMed: 40005944
Activity-based protein profiling and global proteome analysis reveal MASTL as a potential therapeutic target in gastric cancer [ Cell Commun Signal, 2024, 22(1):397] PubMed: 39138495
HSP90 inhibition suppresses tumor glycolytic flux to potentiate the therapeutic efficacy of radiotherapy for head and neck cancer [ Sci Adv, 2024, 10(8):eadk3663] PubMed: 38394204
The pharmacogenomic assessment of molecular epithelial-mesenchymal transition signatures reveals drug susceptibilities in cancer cell lines [ bioRxiv, 2024, 10.1101/2024.01.16.575190] PubMed: none
HSP90β Impedes STUB1-Induced Ubiquitination of YTHDF2 to Drive Sorafenib Resistance in Hepatocellular Carcinoma [ Adv Sci (Weinh), 2023, 10.1002/advs.202302025] PubMed: 37515378
HSP90β Impedes STUB1-Induced Ubiquitination of YTHDF2 to Drive Sorafenib Resistance in Hepatocellular Carcinoma [ Adv Sci (Weinh), 2023, 10(27):e2302025] PubMed: 37515378
HRS mediates tumor immune evasion by regulating proteostasis-associated interferon pathway activation [ Cell Rep, 2023, 10.1016/j.celrep.2023.113352] PubMed: 37948180

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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