For research use only. Not for therapeutic Use.
M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity[1][2][3].
Metabolically stressful conditions, including inflammation and cancer, induces extracellular concentrations of adenosine increase[1].
M1069 dose-dependently suppresses 5’-N-ethylcarboxamide adenosine (stable analog of adenosine)-stimulated cyclic adenosine monophosphate (cAMP) and phosphorylated cAMP- response element binding protein (pCREB) induction, inhibits interleukin (IL)-2 production[1].
M1069 suppresses vascular endothelial growth factor (VEGF) production from human macrophages in adenosine-rich settings[1].
M1069 inhibits protumorigenic cytokine secretion, such as CXCL1, CXCL5 and granulocyte-colony stimulating factor, and reduces IL-12 secretion from adenosine-differentiated dendritic cells[1].
M1069 enhances T-cells activation in adenosine-differentiated dendritic cells[1].
M1069 inhibits breast tumor (CD73hi/adenosine-rich 4T1 syngeneic) growth in vivo in mice and enhances chemotherapeutic agents efficacy[1].
| Catalog Number | I042837 |
| CAS Number | 3027658-65-4 |
| Synonyms | (E)-but-2-enedioic acid;(5S)-N-[7-(3,6-dihydro-2H-pyran-4-yl)-4-methoxy-[1,3]thiazolo[4,5-c]pyridin-2-yl]-7-oxa-2-azaspiro[4.5]decane-2-carboxamide |
| Molecular Formula | C25H30N4O8S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H26N4O4S.C4H4O4/c1-27-18-16-17(15(11-22-18)14-3-9-28-10-4-14)30-19(23-16)24-20(26)25-7-6-21(12-25)5-2-8-29-13-21;5-3(6)1-2-4(7)8/h3,11H,2,4-10,12-13H2,1H3,(H,23,24,26);1-2H,(H,5,6)(H,7,8)/b;2-1+/t21-;/m0./s1 |
| InChIKey | OMDWVJLHHMNGPD-SLISQCDCSA-N |
| SMILES | COC1=NC=C(C2=C1N=C(S2)NC(=O)N3CCC4(C3)CCCOC4)C5=CCOCC5.C(=CC(=O)O)C(=O)O |
| Reference | [1]. Rinat Zaynagetdinov, et al. Abstract 3499: M1069 as dual A2A/A2B adenosine receptor antagonist counteracts immune-suppressive mechanisms of adenosine and reduces tumor growth in vivo. Cancer Res (2022) 82 (12_Supplement):3499. [2]. Lillian L Siu, et al. Abstract CT240: A first-in-human study of the dual A2A/A2B adenosine receptor antagonist M1069 in patients with advanced solid tumors. Cancer Res (2022) 82 (12_Supplement):CT240. [3]. Tanzer Eva-Maria, et al. Preparation of thiazolopyridine derivatives as adenosine receptor antagonists: World Intellectual Property Organization, WO2020152132[P]. 2020-07-30. |
