iGOT1-01 是一种天冬氨酸转氨酶 1 (谷氨酸草酰乙酸转氨酶 1；GOT1) 抑制剂，在 GOT1/GLOX/HRP 测定中IC50为 11.3 μM，在 MDH 偶联 GOT1 酶法测定中IC50为 85 μM。它显示出抗癌活性。

iGOT1-01 is an effective inhibitor of glutamate oxaloacetate transaminase 1(GOT1) . iGOT1-01 has IC50s of 84.6 μM and 11.3 μM in GOT1/MDH1 assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 can be used in anti-cancer studies.

iGOT1-01 (3.125-200 μM; for 3 h) reveals little to no toxicity using two readouts of cell viability in PaTu8902 pancreatic and DLD1 colon cancer cells. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM[1].

In female CD1 mice, iGOT1-01 (20 mg/kg; oral) has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour ng/mL)[2].

882256-55-5

C19H20N4O

320.39

iGOT1-01

DMSO:98 mg/mL (305.88 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years