| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
MT-DADMe-ImmA targets 5'-methylthioadenosine phosphorylase (MTAP), an enzyme that catalyzes the reversible phosphorolysis of 5'-methylthioadenosine (MTA) to adenine and 5-methylthioribose-1-phosphate. MTAP is involved in the methionine salvage pathway and polyamine metabolism. The compound is a transition state analogue that binds to MTAP with extraordinarily high affinity, with a Ki of 90 pM. By inhibiting MTAP, MT-DADMe-ImmA increases cellular MTA concentrations, which inhibits polyamine synthesis and induces apoptosis in MTAP-proficient cancer cells.
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| ln Vitro |
Two head and neck squamous cell lines, FaDu and Cal27, underwent cell engraftment after being treated with MT-DADMe-ImmA and MTA. This treatment also decreased polyamine levels, enhanced cellular MTA concentration, and inhibited MTAP. Normal human fibroblast cell lines (CRL2522 and GM02037) and MCF7 (a breast cancer cell line with an MTAP gene deletion) did not respond to the same treatment. No cell line was able to undergo cell hybridization when MT-DADMe-ImmA was used alone, suggesting that MTA is the active ingredient [2].
In vitro studies have demonstrated that MT-DADMe-ImmA is a potent MTAP inhibitor with a Ki of 90 pM. Treatment of cultured cells with MT-DADMe-ImmA and MTA inhibits MTAP, increases cellular MTA concentrations, decreases polyamines, and induces apoptosis in two head and neck squamous cell carcinoma cell lines, FaDu and Cal27. The compound's ability to induce apoptosis in cancer cells makes it a promising anticancer agent. MT-DADMe-ImmA shows promise as an anticancer agent by disrupting adenosine metabolism and inhibiting tumor growth. |
| ln Vivo |
The inhibitory effect of MT-DADMe-ImmA has a half-life of 50 minutes and a total inhibition time of 250 minutes. Sidewall MT-DADMe-ImmA has a biological half-life of 6.3 days and MTAP activity recovers slowly. In immune-deficient mice, the time-dependent growth of FaDu tumors can be inhibited by intraperitoneal or lateral injection of MT-DADMe-ImmA [2].
In vivo, MT-DADMe-ImmA is being studied for its potential therapeutic applications in cancer, including head and neck and prostate cancer. The compound disrupts adenosine metabolism and inhibits tumor growth. However, specific published in vivo efficacy data in animal models are limited. Further research is ongoing to explore its efficacy and safety profile. The compound's high potency and specificity for MTAP make it a promising candidate for further development. |
| Enzyme Assay |
In vitro non-cell enzyme assays for MT-DADMe-ImmA involve measuring MTAP inhibition using purified recombinant MTAP enzyme and a substrate (e.g., MTA or a chromogenic substrate). The compound is incubated with MTAP and substrate, and enzyme activity is measured by detecting product formation (adenine or 5-methylthioribose-1-phosphate) using HPLC, spectrophotometry, or coupled enzyme assays. Ki values are calculated from steady-state kinetic analysis.
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| Cell Assay |
In vitro cell-based assays for MT-DADMe-ImmA use head and neck squamous cell carcinoma cell lines such as FaDu and Cal27. Cells are cultured in appropriate media and treated with MT-DADMe-ImmA (often in combination with MTA) at various concentrations. Parameters assessed include cell viability (MTT or CCK-8 assays), apoptosis (Annexin V/PI staining and flow cytometry), MTA and polyamine levels (HPLC or LC-MS/MS), and markers of apoptosis (caspase activation, PARP cleavage) by Western blotting.
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| Animal Protocol |
In vivo animal studies for MT-DADMe-ImmA would employ xenograft mouse models using FaDu, Cal27, or other MTAP-proficient cancer cell lines. The compound is administered via intraperitoneal or intravenous injection, and parameters assessed include tumor volume measurements, survival analysis, MTA and polyamine levels in tumor tissues, apoptosis markers, and evaluation of systemic toxicity. However, specific published in vivo data for this compound are limited.
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| ADME/Pharmacokinetics |
MT-DADMe-ImmA has a molecular weight of 293.39 g/mol and a molecular formula of C₁₃H₁₉N₅OS. It is also known as Methylthio-DADMe-Immucillin A or MTDIA. The compound is a transition state analogue of MTAP and binds with extraordinary affinity (Ki = 90 pM). It is soluble in DMSO and should be stored at -20°C. Detailed pharmacokinetic parameters have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of MT-DADMe-ImmA has not been comprehensively evaluated in published studies. As a highly potent MTAP inhibitor, the compound is expected to have significant biological activity that requires careful evaluation. The compound is classified as a research reagent and is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies have not been reported.
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| References |
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| Additional Infomation |
MT-DADMe-ImmA is a potent and selective inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. It is also known as Methylthio-DADMe-Immucillin A or MTDIA. The compound increases cellular MTA concentrations, decreases polyamines, and induces apoptosis in head and neck squamous cell carcinoma cells. It is being studied for potential therapeutic applications in cancer, including head and neck and prostate cancer. Not approved for clinical use; intended for research purposes only.
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| Molecular Formula |
C13H19N5OS
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|---|---|
| Molecular Weight |
293.3879
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| Exact Mass |
293.131
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| CAS # |
653592-04-2
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| PubChem CID |
656970
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| Appearance |
White to off-white solid powder
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| LogP |
0
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
334
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S(C([H])([H])[H])C([H])([H])[C@@]1([H])C([H])([H])N(C([H])([H])C2=C([H])N([H])C3C(N([H])[H])=NC([H])=NC2=3)C([H])([H])[C@]1([H])O[H]
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| InChi Key |
NTHMDFGHOCNNOE-ZJUUUORDSA-N
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| InChi Code |
InChI=1S/C13H19N5OS/c1-20-6-9-4-18(5-10(9)19)3-8-2-15-12-11(8)16-7-17-13(12)14/h2,7,9-10,15,19H,3-6H2,1H3,(H2,14,16,17)/t9-,10+/m1/s1
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| Chemical Name |
(3R,4S)-1-[(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]-4-(methylsulfanylmethyl)pyrrolidin-3-ol
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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 (~340.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume 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 (8.52 mM) (saturation unknown) 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. 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 to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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 (8.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4084 mL | 17.0422 mL | 34.0843 mL | |
| 5 mM | 0.6817 mL | 3.4084 mL | 6.8169 mL | |
| 10 mM | 0.3408 mL | 1.7042 mL | 3.4084 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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