MRT-83
Based on 1 Customer Validation
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
For research use only. We do not sell to patients.
- Purity: 99.27%
- CAS No.: 1263131-92-5
- Formula: C31H30N4O5
- Molecular Weight:538.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Anti-Pancreatic Cancer Compound Library
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Anti-Liver Cancer Compound Library
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Anti-Colorectal Cancer Compound Library
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Cancer Stem Cells Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
Smo[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C3H 10T1/2 | IC50 |
0.011 μM
Compound: 86
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Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
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[PMID: 22268551] |
| HEK293 | IC50 |
5 nM
Compound: 86
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Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
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[PMID: 22268551] |
| Shh Light II | IC50 |
0.015 μM
Compound: 86
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Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
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[PMID: 22268551] |
MRT-83 displays full antagonist properties with an IC50 (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC50 ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC50 of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC50 of 14 nM, which is in good correlation with its IC50 in the Shh-light2 and alkaline phosphatase assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1263131-92-5
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Appearance Solid
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Molecular Weight 538.59
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Formula C31H30N4O5
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Color White to light yellow
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SMILES
COC1=C(OC)C(OC)=CC(C(NC(NC2=CC(NC(C3=CC=C(C4=CC=CC=C4)C=C3)=O)=C(C)C=C2)=N)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 250 mg/mL (464.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mice[1] MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Four groups of six animals received 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin PBS solution containing 0.9 μg of ShhN alone or in the presence of MRT-83 (200 ng) or MRT-36 (110 ng). A control group receive 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin solution alone. All groups are analyzed 48 h after the injection[1]
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8567 mL | 9.2835 mL | 18.5670 mL | 46.4175 mL |
| 5 mM | 0.3713 mL | 1.8567 mL | 3.7134 mL | 9.2835 mL | |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8567 mL | 4.6417 mL | |
| 15 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL | 3.0945 mL | |
| 20 mM | 0.0928 mL | 0.4642 mL | 0.9283 mL | 2.3209 mL | |
| 25 mM | 0.0743 mL | 0.3713 mL | 0.7427 mL | 1.8567 mL | |
| 30 mM | 0.0619 mL | 0.3094 mL | 0.6189 mL | 1.5472 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4642 mL | 1.1604 mL | |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9283 mL | |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 80 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4642 mL |
MRT-83 Related Classifications
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