MTHFD2-IN-7
MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research.
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- Formule: C28H32F3N5O6S
- Masse moléculaire:623.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
MTHFD2-IN-7 (compound 31) inhibits the proliferation of human leukemia cell lines[1].
MTHFD2-IN-7 (0.1-10 μM; 1 h+15 min) binds to and protects purified human MTHFD2 and MTHFD1 from pronase degradation in a dose-dependent manner, with such effects observed at concentrations of 0.1, 1.0 and 10 μM, which confirms its direct binding to the targets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human leukemia cell lines: MOLM-13, THP-1, K562, NALM-6 and MOLT-4
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Concentration:IC50
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Incubation Time:72 h
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Result:Inhibited the proliferation of human leukemia cell lines, with IC50 values of 0.72 μM (MOLM-13), 0.25 μM (THP-1), 0.84 μM (K562), 2.45 μM (NALM-6) and 4.75 μM (MOLT-4).
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 mice with Acute myeloid leukemia (female, 6−8 weeks old)[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:Achieved 37% tumor growth inhibition at 100 mg/kg.
Achieved 67% tumor growth inhibition at 300 mg/kg.
Showed no significant body weight loss, indicating well tolerated treatment.
Chemical Information
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Masse moléculaire 623.64
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Formule C28H32F3N5O6S
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SMILES
CC1=C(C=CC(C2=C3CN(CC2)C(C4=CC(OC(F)(F)F)=C(C=C4)NS(NC)(=O)=O)=O)=C1OC3=O)N5C[C@@H](N(CC5)C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTHFD2-IN-7 Related Classifications
HY-182355 Related Classifications
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