M1069 |
Catalog No.GC73150
One-Click Copy Product Info
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M1069 es un antagonista del receptor de adenosina A2A/A2B con una selectividad de >100 veces contra los receptores A1 y A3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3027658-65-4
Sample solution is provided at 25 µL, 10mM.
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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.
Metabolically stressful conditions, including inflammation and cancer, induces extracellular concentrations of adenosine increase[1].M1069 dose-dependently suppresses 5’-N-etlcarboxamide 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].
References:
[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.
| Cas No. | 3027658-65-4 | SDF | |
| Formula | C25H30N4O8S | M.Wt | 546.59 |
| Solubility | DMSO : 100 mg/mL (182.95 mM; Need ultrasonic) | Storage | 4°C, sealed storage, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8295 mL | 9.1476 mL | 18.2952 mL |
| 5 mM | 365.9 μL | 1.8295 mL | 3.659 mL |
| 10 mM | 183 μL | 914.8 μL | 1.8295 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)