MCT1-IN-2
Based on 2 publication(s) in Google Scholar
MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 227321-12-2
- Formula: C25H29N3O2S
- Molecular Weight:435.58
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) MCT1-IN-2
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Biological Activity
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MCT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | EC50 |
>10 μM
Compound: 1
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Growth inhibition of human MCF7 cells overexpressing MCT4 after 4 days by MTT assay
Growth inhibition of human MCF7 cells overexpressing MCT4 after 4 days by MTT assay
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[PMID: 25068893] |
| MCF7 | EC50 |
21 nM
Compound: 1
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Growth inhibition of human MCF7 cells overexpressing MCT1 after 4 days by MTT assay
Growth inhibition of human MCF7 cells overexpressing MCT1 after 4 days by MTT assay
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[PMID: 25068893] |
| MCF7 | IC50 |
105 nM
Compound: 1
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Inhibition of MCT1 (unknown origin) overexpressed in human MCF7 cells assessed as inhibition of transporter-mediated [14C]lactate transport after 10 mins by scintillation counting
Inhibition of MCT1 (unknown origin) overexpressed in human MCF7 cells assessed as inhibition of transporter-mediated [14C]lactate transport after 10 mins by scintillation counting
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[PMID: 25068893] |
| Raji | EC50 |
0.5 nM
Compound: 1
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Growth inhibition of human Raji cells after 96 hrs by MTT assay
Growth inhibition of human Raji cells after 96 hrs by MTT assay
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[PMID: 25068893] |
| Raji | EC50 |
5 nM
Compound: 5
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Inhibition of MCT1 in human Raji cells assessed as inhibition of cell proliferation after 96 hrs by MTT assay
Inhibition of MCT1 in human Raji cells assessed as inhibition of cell proliferation after 96 hrs by MTT assay
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[PMID: 27347360] |
| Raji | EC50 |
5 nM
Compound: Table 4; R1C1
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Cytotoxicity against human Raji cells
Cytotoxicity against human Raji cells
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[PMID: 34517305] |
MCT1-IN-2 (compound 3) has a pKi of 9.48 for Jurkat T-cells and inhibits human peripheral blood mononuclear cells (PBMC) proliferation (pIC50=8.61)[1].
MCT1-IN-2 (compound 1) has an EC50 of 5.5 nM (MTT assay) and an IC50 of 105 nM (lactate transport inhibition assay) in human Raji lymphoma cell proliferation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 227321-12-2
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Appearance Solid
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Molecular Weight 435.58
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Formula C25H29N3O2S
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Color White to off-white
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SMILES
O=C1C2=C(SCCCO)N(CC3=C4C=CC=CC4=CC=C3)C=C2C(CC(C)C)=NN1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
Solvent & Solubility
DMSO : 100 mg/mL (229.58 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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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-
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Clare M Murray, et al. Monocarboxylate transporter MCT1 is a target for immunosuppression. Nat Chem Biol. 2005 Dec;1(7):371-6. [Content Brief]
[2]. Hui Wang, et al. Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors. J Med Chem. 2014 Sep 11;57(17):7317-24. [Content Brief]
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 (sealed storage, away from moisture). 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 | 2.2958 mL | 11.4789 mL | 22.9579 mL | 57.3947 mL |
| 5 mM | 0.4592 mL | 2.2958 mL | 4.5916 mL | 11.4789 mL | |
| 10 mM | 0.2296 mL | 1.1479 mL | 2.2958 mL | 5.7395 mL | |
| 15 mM | 0.1531 mL | 0.7653 mL | 1.5305 mL | 3.8263 mL | |
| 20 mM | 0.1148 mL | 0.5739 mL | 1.1479 mL | 2.8697 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9183 mL | 2.2958 mL | |
| 30 mM | 0.0765 mL | 0.3826 mL | 0.7653 mL | 1.9132 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5739 mL | 1.4349 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1479 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3826 mL | 0.9566 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7174 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL | 0.5739 mL |