AZD3965

製品コードS7339 バッチS733903

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₂₄F₃N₅O₅S
	分子量	515.51	CAS No.	1448671-31-5
Solubility (25°C)*	体外	DMSO	100 mg/mL (193.98 mM)
		Ethanol	100 mg/mL (193.98 mM)
		Water	Insoluble
* <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	AZD3965は、結合親和性が1.6 nMで、MCT2よりも6倍選択的な、強力で選択的かつ経口投与可能なモノカルボン酸トランスポーター1（MCT1）阻害剤です。第1相。
in vitro	In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. This compound inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. In H526, HGC27 cells and DMS114 cells, this chemical increases intracellular lactate and significantly reduces lactate uptake.
in vivo	In nonobese diabetic scid-γ mice bearing COR-L103 xenografts, AZD3965 (100 mg/kg, p.o.) reduces tumor growth and increased intratumor lactate. In mice bearing H526 tumors, this compound (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity.

製品説明

AZD3965は、結合親和性が1.6 nMで、MCT2よりも6倍選択的な、強力で選択的かつ経口投与可能なモノカルボン酸トランスポーター1（MCT1）阻害剤です。第1相。

in vitro

In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth.

This compound inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia.

In H526, HGC27 cells and DMS114 cells, this chemical increases intracellular lactate and significantly reduces lactate uptake.

in vivo

In nonobese diabetic scid-γ mice bearing COR-L103 xenografts, AZD3965 (100 mg/kg, p.o.) reduces tumor growth and increased intratumor lactate.

In mice bearing H526 tumors, this compound (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	DMS114, H526 and HGC27 cells
	濃度	1.6 nM
	反応時間	24 h
	実験の流れ	Cells were incubated in either normoxia, 1% oxygen (hypoxia) or anoxia in complete media supplemented with AZD3965 or DMSO vehicle for 24 hours.
動物実験	動物モデル	Nonobese diabetic scid-γ mice bearing COR-L103 xenografts
	投薬量	100 mg/kg
	投与方法	p.o.

参考

http://cancerres.aacrjournals.org/content/72/8_Supplement/3224
https://pubmed.ncbi.nlm.nih.gov/24277449/
https://pubmed.ncbi.nlm.nih.gov/25281618/

カスタマーフィードバック

: Data from [Data independently produced by , , Cancer Res, 2017, 77(20):5591-5601]

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：

Lactate production by tumor-resident Staphylococcus promotes metastatic colonization in lung adenocarcinoma [ Cell Host Microbe, 2025, 33(7):1089-1105.e7]	PubMed: 40639336
Tumor-associated neutrophil precursors impair homologous DNA repair and promote sensitivity to PARP inhibition [ Nat Commun, 2025, 16(1):6999]	PubMed: 40738898
Lactylation modification of HIF-1α enhances its stability by blocking VHL recognition [ Cell Commun Signal, 2025, 23(1):364]	PubMed: 40760493
CDK1-mediated phosphorylation of LDHA fuels mitosis through LDHB-dependent lactate oxidation [ EMBO Rep, 2025, 10.1038/s44319-025-00573-8]	PubMed: 40940446
Lactate accumulation promotes immunosuppression and fibrotic transformation of bone marrow microenvironment in myelofibrosis [ J Transl Med, 2025, 23(1):69]	PubMed: 39810250
Lactate metabolism in clonal plasma cells and its therapeutic implications in multiple myeloma patients with elevated serum LDH levels [ Cancer Metab, 2025, 13(1):9]	PubMed: 39948621
A375 melanoma-derived lactate controls A375 melanoma phenotypes by inducing macrophage M2 polarization via TCA cycle and TGF-β signaling [ PeerJ, 2025, 13:e18887]	PubMed: 39995996
Deciphering metabolic heterogeneity in retinoblastoma unravels the role of monocarboxylate transporter 1 in tumor progression [ Biomark Res, 2024, 12(1):48]	PubMed: 38730450
H3K9 lactylation in malignant cells facilitates CD8+ T cell dysfunction and poor immunotherapy response [ Cell Rep, 2024, 43(9):114686]	PubMed: 39216002
Lactate promotes myogenesis via activating H3K9 lactylation-dependent up-regulation of Neu2 expression [ J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363]	PubMed: 37919243

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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