| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
MALAT1-IN-1 targets Malat1 (metastasis-associated lung adenocarcinoma transcript 1), a long non-coding RNA. It is a specific inhibitor of MALAT1 and does not affect the expression of Neat1 (nuclear enriched abundant transcript 1). By inhibiting MALAT1, it regulates Malat1 downstream genes in a dose-dependent manner. MALAT1 is implicated in tumor progression and metastasis, making it a key target in cancer research.
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| ln Vitro |
In vitro, MALAT1-IN-1 regulates Malat1 downstream genes in a dose-dependent fashion without affecting expression of Neat1. It is a potent and specific inhibitor of Malat1. It serves as a valuable tool for validating RNA-based drug discovery approaches and understanding metastasis regulation. Quantitative in vitro activity data, such as IC50 values for MALAT1 inhibition, is not detailed in the publicly available sources.
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| ln Vivo |
In vivo activity data for MALAT1-IN-1 is limited in publicly available literature. As a specific inhibitor of MALAT1, it is hypothesized to exhibit antitumor effects in animal models of cancer. However, specific in vivo efficacy studies, including pharmacokinetic and pharmacodynamic parameters, have not been detailed in the available sources. Further research is needed to fully characterize its in vivo activity and therapeutic potential.
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| Enzyme Assay |
For in vitro cell-free assays, the interaction of MALAT1-IN-1 with MALAT1 RNA can be studied using RNA pull-down assays, electrophoretic mobility shift assays (EMSA), or surface plasmon resonance (SPR). The compound's ability to modulate MALAT1 downstream gene expression can be assessed using qPCR or RNA sequencing.
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| Cell Assay |
For in vitro cellular assays, the activity of MALAT1-IN-1 is assessed in cancer cell lines expressing MALAT1. Cells are treated with various concentrations of the compound, and MALAT1 downstream gene expression is measured by qPCR. The effect on Neat1 expression is measured to confirm specificity. Cell proliferation, migration, and invasion assays can be performed to assess the functional effects of MALAT1 inhibition.
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| Animal Protocol |
For in vivo studies, MALAT1-IN-1 could be administered orally or intraperitoneally in mouse xenograft models of lung adenocarcinoma or other cancers. Endpoints include tumor volume measurement, metastasis assessment, and analysis of MALAT1 downstream gene expression in tumor tissue. Pharmacokinetic studies would be needed to determine its bioavailability and half-life.
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| ADME/Pharmacokinetics |
MALAT1-IN-1 (CAS 827327-28-6) has a molecular formula of C19H21N3O2 and a molecular weight of 323.39 g/mol. Chemical name: 5-(4-methoxyphenyl)-N-[(3-methoxyphenyl)methyl]-1-methyl-1H-imidazol-2-amine. Appearance: typically a solid. Purity: typically >98% for research use. Storage: typical for small-molecule compounds (desiccated, protected from light, -20°C).
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| Toxicity/Toxicokinetics |
No toxicity data is publicly available. As a research compound targeting a non-coding RNA, standard toxicological profiling would be required for further development.
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| References | |
| Additional Infomation |
MALAT1-IN-1 is a research-grade compound and is not approved for therapeutic use. It serves primarily as a pharmacological tool for studying the role of MALAT1 lncRNA in tumor progression and metastasis. Its mechanism of action involves specific inhibition of MALAT1, regulating its downstream genes without affecting Neat1. It is a valuable tool for validating RNA-based drug discovery approaches. No clinical trials have been reported.
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| Molecular Formula |
C19H21N3O2
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|---|---|
| Molecular Weight |
323.388944387436
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| Exact Mass |
323.163
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| CAS # |
827327-28-6
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| PubChem CID |
1096509
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| Appearance |
White to light yellow solid powder
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| Density |
1.14±0.1 g/cm3(Predicted)
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| Boiling Point |
534.0±60.0 °C(Predicted)
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
374
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C(NCC2C=C(OC)C=CC=2)N(C)C(C2C=CC(OC)=CC=2)=C1
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| InChi Key |
LCVOJBGSGIOMKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3O2/c1-22-18(15-7-9-16(23-2)10-8-15)13-21-19(22)20-12-14-5-4-6-17(11-14)24-3/h4-11,13H,12H2,1-3H3,(H,20,21)
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| Chemical Name |
5-(4-methoxyphenyl)-N-[(3-methoxyphenyl)methyl]-1-methylimidazol-2-amine
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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 : ~125 mg/mL (~386.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.43 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 20.8 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: ≥ 2.08 mg/mL (6.43 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0922 mL | 15.4612 mL | 30.9224 mL | |
| 5 mM | 0.6184 mL | 3.0922 mL | 6.1845 mL | |
| 10 mM | 0.3092 mL | 1.5461 mL | 3.0922 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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