| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
M1069 free base selectively targets the A2A and A2B adenosine receptors. It displays high selectivity, with a greater than 100-fold preference for A2A/A2B over the A1 and A3 adenosine receptor subtypes. This selectivity profile is crucial for minimizing off-target effects associated with adenosine receptor modulation.
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| ln Vitro |
In vitro studies demonstrate that M1069 free base effectively antagonizes adenosine-mediated signaling at A2A and A2B receptors. By blocking these receptors, it reverses the immune-suppressive effects of adenosine, which is often elevated in the tumor microenvironment. This activity enhances the function of immune effector cells, such as T cells and NK cells, promoting anti-tumor immune responses. Specific IC50 values for receptor blockade and functional cellular assays are available in the primary literature.
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| ln Vivo |
In vivo, M1069 free base has demonstrated anti-tumor efficacy in preclinical animal models. As an orally bioavailable compound, it is typically administered via oral gavage in efficacy studies. The compound's ability to counteract adenosine-mediated immunosuppression in the tumor microenvironment leads to enhanced immune-mediated tumor growth inhibition. Detailed efficacy data, including tumor growth inhibition rates and survival benefits, are described in the patent and subsequent research publications.
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| Enzyme Assay |
The non-cellular enzyme/receptor binding assay for M1069 free base typically involves radioligand binding studies using membrane preparations from cells expressing human adenosine receptor subtypes (A1, A2A, A2B, A3). Compounds are incubated with varying concentrations of the radioligand and test compound to determine binding affinity (Ki values) and selectivity. Data are analyzed using nonlinear regression to calculate IC50 values, which are then converted to Ki using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for M1069 free base utilize immune cells such as T cells or NK cells cultured in the presence of adenosine and the test compound. Functional readouts include measuring cyclic AMP (cAMP) accumulation (as A2A/A2B are Gs-coupled receptors that stimulate cAMP production), assessing cell proliferation, and evaluating cytokine production (e.g., IFN-γ, IL-2). The compound's ability to reverse adenosine-induced suppression of immune cell function is quantified to determine its potency and efficacy.
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| Animal Protocol |
In vivo animal studies for M1069 free base are conducted in syngeneic mouse tumor models. The compound is administered orally once or twice daily at various dose levels. Tumor growth is monitored over time, and endpoints include tumor volume measurements, survival analysis, and immunological assessments (e.g., tumor-infiltrating lymphocyte characterization). Pharmacodynamic markers such as changes in cAMP levels or immune cell activation status in the tumor microenvironment may also be evaluated.
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| ADME/Pharmacokinetics |
As a lipophilic small molecule (molecular weight 430.52), M1069 free base is orally bioavailable. It is typically formulated in vehicles containing DMSO, PEG300, Tween 80, and saline for in vivo administration. The compound is stable as a powder at -20°C for up to 3 years and in solution at -80°C for 1 year. Detailed pharmacokinetic parameters such as half-life, Cmax, and AUC are available from the supplier's data or primary literature.
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| Toxicity/Toxicokinetics |
Standard toxicity assessments for M1069 free base would include acute and sub-chronic toxicity studies in rodents to determine the maximum tolerated dose (MTD) and identify potential target organ toxicities. As an investigational compound, comprehensive toxicology data are typically generated during the preclinical development phase. Researchers should consult the safety data sheet (SDS) and primary literature for specific toxicity information and handle the compound with appropriate laboratory safety precautions.
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| References |
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| Additional Infomation |
M1069 (free base) is a small molecule drug. The international nonproprietary name stem "-adenant" in its name indicates that movadinan is an adenosine receptor antagonist. The monoisotope molecular weight of movadinan is 430.17 Da.
M1069 free base is a research-grade compound supplied for preclinical studies only, not for human therapeutic use. It is identified by the chemical formula C21H26N4O4S. The compound is part of a class of adenosine receptor antagonists being investigated for cancer immunotherapy. Detailed protocols, including in vivo formulation calculators, are available from the supplier. Researchers should consult the patent literature (e.g., references [1][2][3]) for comprehensive biological data. |
| Exact Mass |
430.167
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|---|---|
| CAS # |
2459881-03-7
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| PubChem CID |
154659422
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
679
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=NC=C(C2=C1N=C(S2)NC(=O)N3CC[C@]4(C3)CCCOC4)C5=CCOCC5
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| InChi Key |
CSSAKLQGJYJMNW-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C21H26N4O4S/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/h3,11H,2,4-10,12-13H2,1H3,(H,23,24,26)/t21-/m0/s1
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| Chemical Name |
(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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~232.28 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.81 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.81 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.81 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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