产品
编 号:F756952
分子式:C27H24F2N6O4
分子量:534.51
产品类型
结构图
CAS No: 2924825-23-8
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生物活性:
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.
体内研究:
MAT2A-IN-10 (Compound 28; p.o.; once daily for 6 days) 在小鼠 HCT-116 (MTAP-/-) 移植模型中导致肿瘤消退。Animal Model:BALB/c mice, HCT-116(MTAP-/-) xenograft mouse tumor model
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
Dosage:10 mg/kg
Administration:Oral (Pharmacokinetic Analysis)
Result:Pharmacokinetic Properties of MAT2A-IN-10 (Compound 28) in Male ICR Mice (n = 3)aroutedose [mg/kg] Tmax [h] T1/2 [h] MRT [h] Cmax [ng/mL] AUC [ng?h/mL]
po100.672.984.71673341192
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.
体外研究:
MAT2A-IN-10 (Compound 28; 0.1 nM-10 μM; 4 days) 抑制 HCT-116 (MTAP-/-) 细胞增殖,IC50 为 75 ± 5 nM。不抑制 HCT-116 (WT) 细胞增殖。