AZD3965

製品コードS7339 バッチS733901

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 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.
in vitro	In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. ^[1] AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. ^[2] In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake. ^[3]
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. ^[2] In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity. ^[3]

製品説明

AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM, 6-fold selective over MCT2. Phase 1.

in vitro

In lymphoma cell lines that preferentially express MCT1, AZD3965 potently inhibits lactate transport and cell growth. ^[1]

AZD3965 inhibits MCT1 activity in cells, and shows higher sensitivity in hypoxia. ^[2]

In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake. ^[3]

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. ^[2]

In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity. ^[3]

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

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：

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
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546]	PubMed: 37428012
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546]	PubMed: 37428012
A critical role for heme synthesis and succinate in the regulation of pluripotent states transitions [ Elife, 2023, 12e78546]	PubMed: 37428012
Functional heterogeneity of MCT1 and MCT4 in metabolic reprogramming affects osteosarcoma growth and metastasis [ J Orthop Surg Res, 2023, 18(1):131]	PubMed: 36814318
The lactate-NAD+ axis activates cancer-associated fibroblasts by downregulating p62 [ Cell Rep, 2022, 39(6):110792]	PubMed: 35545049
Succinate uptake by T cells suppresses their effector function via inhibition of mitochondrial glucose oxidation [ Cell Rep, 2022, 40(7):111193]	PubMed: 35977513
A Heme-Binding Transcription Factor BACH1 Regulates Lactate Catabolism Suggesting a Combined Therapy for Triple-Negative Breast Cancer [ Cells, 2022, 11(7)1177]	PubMed: 35406740

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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