| Identification | Back Directory | [Name]
Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, 1-[4-(difluoromethoxy)phenyl]-7-ethoxy-3-(1,2,3,4-tetrahydro-2-methylpyrazino[1,2-a]benzimidazol-7-yl)- | [CAS]
2924825-23-8 | [Synonyms]
MAT2A-IN-10
Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, 1-[4-(difluoromethoxy)phenyl]-7-ethoxy-3-(1,2,3,4-tetrahydro-2-methylpyrazino[1,2-a]benzimidazol-7-yl)- | [Molecular Formula]
C27H24F2N6O4 | [MOL File]
2924825-23-8.mol | [Molecular Weight]
534.52 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | 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.
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| [References]
[1] Zhang S, et al. Design and Structural Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High In Vivo Potency and Oral Bioavailability. J Med Chem. 2023 Apr 13;66(7):4849-4867. DOI:10.1021/acs.jmedchem.2c02006 |
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