MAT2A-IN-26
MAT2A-IN-26 is an orally active MAT2A inhibitor with a human IC50 of 17.53 nM. MAT2A-IN-26 inhibits the enzymatic activity of MAT2A, thereby reducing the levels of S-adenosylmethionine (SAM) and symmetric dimethylarginine (sDMA). MAT2A-IN-26 inhibits the proliferation of MTAP-deficient cancer cells and induces anti-tumor efficacy in xenograft models. MAT2A-IN-26 can be used in non-small cell lung cancer research.
For research use only. We do not sell to patients.
- Formula: C23H21F2N5O2
- Molecular Weight:437.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
MAT2A-IN-26 (Compound 33) (0.01-1 μM; 72 h) potently and selectively inhibits proliferation of HCT116 MTAP KO cells with a GI50 of 0.76 μM, reduces intracellular SAM and sDMA levels in HCT116 MTAP KO cells, and suppresses proliferation of multiple MTAP-null cancer cell lines including MCF-7, H4, and NCI-H838[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (female)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; daily
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Result:Exhibited slightly stronger antitumor efficacy than IDE-397 at 1 mg/kg.
Induced tumor regression with mean tumor volumes returning to baseline levels and a tumor growth inhibition (TGI) value of approximately 90% at 10 mg/kg after continuous administration for 8 days.
Caused only a slight decrease in body weight at 10 mg/kg.
Showed dose-dependent reduction in SAM levels in both plasma and tumor tissue, with the most pronounced reduction at 10 mg/kg.
Induced substantial decrease in tumor sDMA levels.
Chemical Information
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Molecular Weight 437.44
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Formula C23H21F2N5O2
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SMILES
CN1C=C2C=C(C=CC2=N1)N3N=CC(NCC4CC4)=C(C3=O)C5=CC=C(C=C5)OC(F)F
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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)