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.
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- CAS No.: 3125953-25-2
- 화학식: C30H36F3N5O6S
- 분자량:651.70
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
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.
In Vivo
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.
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Xenograft (PDX)
- Transepithelial/transendothelial electrical resistance assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3125953-25-2
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분자량 651.70
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTHFD1/2-IN-1 Related Classifications
HY-182356 Related Classifications
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