iGOT1-01是有效的天冬氨酸转氨酶1(谷氨酸草酰乙酸转氨酶1；GOT1)抑制剂，在MDH偶联GOT1酶法测定中IC50为85μM，在GOT1/GLOX/HRP测定中IC50为11.3μM。iGOT1-01具有抗癌活性。
货号:ajcx30798
CAS:882256-55-5
分子式:C19H20N4O
分子量：320.39
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC50s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity[1][2].

iGOT1-01 has an IC50 of 84.6 μM in the GOT1/MDH1 assay. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM[2]. 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[2].

iGOT1-01 (compound 1a; 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)[1]. Animal Model: Female CD1 mice with 9 weeks old[1]

[1]. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678. [2]. Melissa C Holt, et al. Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors. Biochemistry. 2018 Nov 27;57(47):6604-6614.