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製品番号: HY-182355

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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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₂₈H₃₂F₃N₅O₆S
分子量:623.64

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

MTHFD2-IN-7 構造式

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

体外実験

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.

Cell Proliferation Assay^[1]

Cell Line:

Human leukemia cell lines: MOLM-13, THP-1, K562, NALM-6 and MOLT-4
Concentration:

IC₅₀
Incubation Time:

72 h
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).

体内実験

MTHFD2-IN-7 (compound 31) (100-300 mg/kg; p.o.; once daily) induces dose-dependent tumor growth inhibition in MOLM-13 AML xenografts, with no significant toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude mice with Acute myeloid leukemia (female, 6−8 weeks old)^[1]
Dosage:

100 mg/kg; 300 mg/kg
Administration:

p.o.; once daily
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.

化学情報

分子量 623.64
分子式 C₂₈H₃₂F₃N₅O₆S
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Lin H, et al. Discovery of 1,2,3,4-Tetrahydrochromeno[3,4-c]pyridin-5-one Derivatives as Novel MTHFD Inhibitors for the Treatment of Acute Myeloid Leukemia. J Med Chem. Published online March 20, 2026. [Content Brief]

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モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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希釈計算機

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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