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MTHFD1/2-IN-1
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Catalog No. T218595 Copy Product Info
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MTHFD1/2-IN-1 is an orally active dual inhibitor of MTHFD1 and MTHFD2, exhibiting IC50 values of 0.26 μM and 0.031 μM for human MTHFD1 and MTHFD2, respectively. It disrupts one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 and both the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby impairing nucleotide biosynthesis and redox homeostasis in cancer cells. This compound demonstrates good Caco-2 permeability and hepatic microsome metabolic stability. Furthermore, MTHFD1/2-IN-1 shows significant anti-leukemia activity, reducing the viability of various leukemia cells and inhibiting tumor growth in mouse models of acute myeloid leukemia (AML).
MTHFD1/2-IN-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Storage & Solubility Information
| Description | MTHFD1/2-IN-1 is an orally active dual inhibitor of MTHFD1 and MTHFD2, exhibiting IC50 values of 0.26 μM and 0.031 μM for human MTHFD1 and MTHFD2, respectively. It disrupts one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 and both the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby impairing nucleotide biosynthesis and redox homeostasis in cancer cells. This compound demonstrates good Caco-2 permeability and hepatic microsome metabolic stability. Furthermore, MTHFD1/2-IN-1 shows significant anti-leukemia activity, reducing the viability of various leukemia cells and inhibiting tumor growth in mouse models of acute myeloid leukemia (AML). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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