V-9302

製品コードS8818 バッチS881803

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C34H38N2O4
分子量 538.68 CAS No. 1855871-76-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (185.63 mM)
Water 100 mg/mL (185.63 mM)
Ethanol 100 mg/mL (185.63 mM)
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

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生物活性

製品説明 V-9302 is a competitive small molecule antagonist of transmembrane glutamine flux, that selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) with an IC50 value of 9.6 μM for inhibition of glutamine uptake in HEK-293 cells. V-9302 blocks Sodium-neutral AA transporter 2 (SNAT2, SLC38A2) and the large neutral AA transporter 1 (LAT1, SLC7A5) as observed in 143B osteosarcoma cells, HCC1806 breast cancer cells and Xenopus laevis oocytes.Dilution of PBS may cause a clear aqueous solution to turn into a uniform suspension.
in vitro

V-9302 inhibits ASCT2-mediated glutamine uptake in human cells in a concentration-dependent fashion and exhibits a 100-fold improvement in potency (IC50 V-9302 = 9.6 µM) over gamma-L-glutamyl-p-nitroanilide (GPNA; IC50 = 1000 µM)[1].
in vivo

Pharmacological blockade of ASCT2 with V-9302 results in attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress, which collectively, contributes to anti-tumor responses in vitro and in murine models in vivo. The steady-state plasma concentrations are achieved 4 h post-administration, with a half-life of approximately 6 h in healthy mice. Following a single acute V-9302 exposure (4 h), plasma glucose levels are not significantly different than vehicle controls, yet plasma glutamine levels are elevated by approximately 50% in V-9302-treated mice compared to vehicle controls, likely a pharmacodynamic effect. Plasma glucose levels in mice chronically exposed to V-9302 or vehicle over a 21-day regimen are not significantly different, while plasma glutamine levels are slightly decreased[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCC1806 cells
濃度 25 µM
反応時間 48 h
実験の流れ

HCC1806 cells are treated V-9302 (25 µM aqueous, 1% DMSO) for 48 h. Following treatment, cells are fixed with 70% methanol for 5-10 min. LC3B is visualized with 1:100 primary antibody at 37 ºC for 45 min followed by application of 1:600 secondary antibody at 37 ºC for 30 min and DAPI for 4 min.
動物実験 動物モデル cell-line xenograft tumors (propagated in 6-week old, female athymic nude mice)
投薬量 75 mg/kg
投与方法 IP

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：

Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8] PubMed: 38522556
Mesothelioma cancer cells are glutamine addicted and glutamine restriction reduces YAP1 signaling to attenuate tumor formation [ Mol Carcinog, 2023, 62(4):438-449] PubMed: 36562471
Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells [ Nat Commun, 2022, 13(1):3034] PubMed: 35641493
Mapping of functional SARS-CoV-2 receptors in human lungs establishes differences in variant binding and SLC1A5 as a viral entry modulator of hACE2 [ EBioMedicine, 2022, 87:104390] PubMed: 36584595
PET/MR Imaging of a Lung Metastasis Model of Clear Cell Renal Cell Carcinoma with (2S,4R)-4-[18F]Fluoroglutamine [ Mol Imaging Biol, 2022, 10.1007/s11307-022-01747-9] PubMed: 35732988
Targeting of the glutamine transporter SLC1A5 induces cellular senescence in clear cell renal cell carcinoma [ Biochem Biophys Res Commun, 2022, 611:99-106] PubMed: 35487063
Evaluation of Glutaminolysis in T Cells [ Curr Protoc, 2022, 2(9):e540] PubMed: 36111948
Metabolic stress induces GD2+ cancer stem cell-like phenotype in triple-negative breast cancer [ Br J Cancer, 2021, 10.1038/s41416-021-01636-y] PubMed: 34811508
Oncogenic KRAS mutations enhance amino acid uptake by colorectal cancer cells via the hippo signaling effector YAP1 [ Mol Oncol, 2021, 10.1002/1878-0261.12999] PubMed: 34003553
Oncogenic KRAS mutations enhance amino acid uptake by colorectal cancer cells via the hippo signaling effector YAP1 [ Mol Oncol, 2021, 10.1002/1878-0261.12999] PubMed: 34003553

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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