V-9302

製品コードS8818 バッチS881802

化学情報

	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)
* <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	V-9302は、HEK-293細胞におけるグルタミン取り込み阻害のIC50値が9.6 μMである、アミノ酸トランスポーターASCT2（SLC1A5）を選択的かつ強力に標的とする、膜貫通型グルタミンフラックスの競合的低分子アンタゴニストです。V-9302は、143B骨肉腫細胞、HCC1806乳癌細胞、およびアフリカツメガエル卵母細胞で観察されたように、ナトリウム中性AAトランスポーター2（SNAT2、SLC38A2）および大型中性AAトランスポーター1（LAT1、SLC7A5）を阻害します。PBSの希釈により、透明な水溶液が均一な懸濁液に変化する場合があります。
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 of this compound = 9.6 µM) over gamma-L-glutamyl-p-nitroanilide (GPNA; IC50 = 1000 µM).
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 exposure to this compound (4 h), plasma glucose levels are not significantly different than vehicle controls, yet plasma glutamine levels are elevated by approximately 50% in treated mice compared to vehicle controls, likely a pharmacodynamic effect. Plasma glucose levels in mice chronically exposed to this chemical or vehicle over a 21-day regimen are not significantly different, while plasma glutamine levels are slightly decreased.

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

参考

https://pubmed.ncbi.nlm.nih.gov/29334372/
https://pubmed.ncbi.nlm.nih.gov/30072900/

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：

MEBOCOST maps metabolite-mediated intercellular communications using single-cell RNA-seq [ Nucleic Acids Res, 2025, 53(12)gkaf569]	PubMed: 40568942
Predictive role of SLC1A5 in neuroblastoma prognosis and immunotherapy [ BMC Cancer, 2025, 25(1):161]	PubMed: 39875895
PP2A activation drives aberrant macropinocytosis and cell death in pancreatic ductal adenocarcinoma [ bioRxiv, 2025, 2025.07.14.664742]	PubMed: 40791444
Macrophages excite muscle spindles with glutamate to bolster locomotion [ Nature, 2024, 10.1038/s41586-024-08272-5]	PubMed: 39633045
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
Glutamine availability regulates cDC subsets in tissue [ bioRxiv, 2024, 2024.09.17.613574]	PubMed: 39345449
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
Targeting glutamine utilization to block metabolic adaptation of tumor cells under the stress of carboxyamidotriazole-induced nutrients unavailability [ Acta Pharm Sin B, 2022, 12(2):759-773]	PubMed: 35256945
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

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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