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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-Muvadenant fumarate
Muvadenant fumarate

Chemical Structure : Muvadenant fumarate

CAS No.: 3027658-65-4

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Muvadenant fumarate (M1069, M-1069)

货号: PC-28050Not For Human Use, Lab Use Only.

Muvadenant fumarate (M1069) is a potent, orally active dual antagonist of the A2A and A2B adenosine receptors, with selectivity of >100 fold against the A1 and A3 receptors.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Muvadenant fumarate (M1069) is a potent, dual antagonist of the A2A and A2B adenosine receptors, with selectivity of >100 fold against the A1 and A3 receptors.
M1069 caused a dose-dependent suppression of 5′-N-ethylcarboxamide adenosine (stable analog of adenosine)-stimulated cAMP and pCREB induction and rescue of IL-2 production (A2A readout) in assays with primary human T cells.
M1069 also suppressed VEGF production from human macrophages (A2B readout) in adenosine-rich settings.
M1069 exhibited superior suppression of protumorigenic cytokine secretion, including CXCL1, CXCL5 and granulocyte-colony stimulating factor, and the rescue of IL12 secretion from adenosine-differentiated dendritic cells, as compared to an A2Aselective antagonist.
M1069 demonstrated superior T cell activation in adenosine-differentiated dendritic cells.
M1069 reduced tumor growth as a monotherapy and enhanced anti-tumor activity with chemotherapeutic agents in a murine CD73hi/adenosine-rich 4T1 syngeneic breast tumor model.

物理化学性质&存储条件

分子量 546.59
分子式 C25H30N4O8S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxythiazolo[4,5-c]pyridin-2-yl)-7-oxa-2-azaspiro[4.5]decane-2-carboxamide fumarate

参考文献

1. Rinat Zaynagetdinov, et al. Cancer Res (2022) 82 (12_Supplement):3499.

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