1. Epigenetics Metabolic Enzyme/Protease
  2. Methionine Adenosyltransferase (MAT)
  3. MAT2A-IN-10

MAT2A-IN-10 (Compound 28) is an orally active MAT2A inhibitor with an IC50 of 26 nM. MAT2A-IN-10 can be used for the research of cancer.

For research use only. We do not sell to patients.

MAT2A-IN-10 Chemical Structure

MAT2A-IN-10 Chemical Structure

CAS No. : 2924825-23-8

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Description

MAT2A-IN-10 (Compound 28) is an orally active MAT2A inhibitor with an IC50 of 26 nM. MAT2A-IN-10 can be used for the research of cancer[1].

IC50 & Target

IC50: 26 nM (MAT2A)[1]

In Vitro

MAT2A-IN-10 (Compound 28; 0.1 nM-10 μM; 4 days) inhibits HCT-116 (MTAP-/-) cell proliferation with an IC50 of 75 ± 5 nM but not inhibits HCT-116 (WT) proliferation[1].

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

Cell Proliferation Assay[1]

Cell Line: HCT-116 (WT) and HCT-116 (MTAP-/-)
Concentration: 0.1 nM-10 μM
Incubation Time: 4 days
Result: Inhibited cell proliferation with IC50s of 75 ± 5 nM and >10000 nM against HCT-116 (MTAP-/-) and HCT-116 (WT) cells, respectively.
In Vivo

MAT2A-IN-10 (Compound 28; p.o.; once daily for 6 days) results in tumor regression in the HCT-116 (MTAP-/-) xenograft tumor model in BALB/c mice[1].

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

Animal Model: BALB/c mice, HCT-116(MTAP-/-) xenograft mouse tumor model[1]
Dosage: 50 mg/kg
Administration: PO, once daily for 6 days
Result: Resulted in tumor regression. Induced a continuous decrease in tumor volume after day 6, and the tumor regression reached -52% at the end of treatment (day 18).
Animal Model: Male ICR Mice[1]
Dosage: 10 mg/kg
Administration: Oral (Pharmacokinetic Analysis)
Result: Pharmacokinetic Properties of MAT2A-IN-10 (Compound 28) in Male ICR Mice (n = 3)a
route dose [mg/kg] Tmax [h] T1/2 [h] MRT [h] Cmax [ng/mL] AUC [ng•h/mL]
po 10 0.67 2.98 4.71 6733 41192

aTmax, time for maximum plasma concentration; T1/2, elimination half-life; MRT, mean residue time; Cmax, maximum plasma concentration; AUC, area under drug time curve.
Molecular Weight

534.51

Formula

C27H24F2N6O4

CAS No.
SMILES

CCOC1=NC2=C(C(N(C(N2C3=CC=C(C=C3)OC(F)F)=O)C4=CC=C5N=C6CN(CCN6C5=C4)C)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MAT2A-IN-10
Cat. No.:
HY-149915
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