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.
- CAS No.: 2924825-23-8
- Formula: C27H24F2N6O4
- Molecular Weight:534.51
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 26 nM (MAT2A)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
75 nM
Compound: 28
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Antiproliferative activity against human HCT-116 cells expressing MTAP-/- assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
Antiproliferative activity against human HCT-116 cells expressing MTAP-/- assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
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[PMID: 36961373] |
| HCT-116 | IC50 |
>10000 nM
Compound: 28
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
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[PMID: 36961373] |
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.
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Cell Line:HCT-116 (WT) and HCT-116 (MTAP-/-)
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Concentration:0.1 nM-10 μM
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Incubation Time:4 days
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Result:Inhibited cell proliferation with IC50s of 75 ± 5 nM and >10000 nM against HCT-116 (MTAP-/-) and HCT-116 (WT) cells, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice, HCT-116(MTAP-/-) xenograft mouse tumor model[1]
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Dosage:50 mg/kg
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Administration:PO, once daily for 6 days
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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).
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Animal Model:Male ICR Mice[1]
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Dosage:10 mg/kg
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Administration:Oral (Pharmacokinetic Analysis)
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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.
Chemical Information
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CAS No. 2924825-23-8
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Molecular Weight 534.51
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Formula C27H24F2N6O4
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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
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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)
MAT2A-IN-10 Related Classifications
HY-149915 Related Classifications
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