MTHFD1/2-IN-1
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models.
For research use only. We do not sell to patients.
- CAS No.: 3125953-25-2
- Formula: C30H36F3N5O6S
- Molecular Weight:651.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
MTHFD1/2-IN-1 (compound 34) potently inhibits the proliferation of human acute myeloid leukemia (AML) cell lines MOLM-13 (IC50=0.25 μM) and THP-1 (IC50=0.06 μM), and exhibits only moderate activity against K562, NALM-6 and MOLT-4 cells[1].
MTHFD1/2-IN-1 (0.1-10 μM; 1 h+15 min) directly interacts with human MTHFD1 and MTHFD2 proteins, which is confirmed by its dose-dependent protective effect against proteolytic degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human AML cell lines MOLM-13, THP-1; human CML cell line K562; human ALL cell lines NALM-6, MOLT-4
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Concentration:Serial dilutions
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Incubation Time:72 h
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Result:Inhibited proliferation of MOLM-13 cells with an IC50 of 0.25 μM.
Inhibited proliferation of THP-1 cells with an IC50 of 0.06 μM.
Inhibited proliferation of K562 cells with an IC50 of 0.40 μM.
Inhibited proliferation of NALM-6 cells with an IC50 of 1.26 μM.
Inhibited proliferation of MOLT-4 cells with an IC50 of 1.78 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft model)[1]
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Dosage:100 mg/kg; 300 mg/kg
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Administration:p.o.; once daily
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Result:Induced tumor growth inhibition at 100 mg/kg.
Induced 79% tumor growth inhibition (TGI) at 300 mg/kg.
Maintained stable body weight across treatment period, indicating no significant treatment-related toxicity.
Chemical Information
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CAS No. 3125953-25-2
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Molecular Weight 651.70
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Formula C30H36F3N5O6S
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SMILES
CC1=C(C=CC(C2=C3CN(CC2)C(C4=CC(OC(F)(F)F)=C(C=C4)NS(N(C)CC)(=O)=O)=O)=C1OC3=O)N5C[C@@H](N(CC5)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTHFD1/2-IN-1 Related Classifications
HY-182356 Related Classifications
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