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Chemical Structure : M1069
Catalog No.: PC-49354Not For Human Use, Lab Use Only.
M1069 (M-1069) is a potent, dual antagonist of the A2A and A2B adenosine receptors, with selectivity of >100 fold against the A1 and A3 receptors.
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M1069 (M-1069) 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.
| M.Wt | 430.523 | |
| Formula | C21H26N4O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Rinat Zaynagetdinov, et al. Cancer Res (2022) 82 (12_Supplement):3499.
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