• 产品描述：

  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

• 靶点： IC50: 85 μM (MDH coupled GOT1 enzymatic assay) and 11.3 μM (GOT1/GLOX/HRP assay)

• 体外研究：
  iGOT1-01 has an IC50 of 11.3 μM in the GOT1/GLOX/HRP assay and 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.
  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.

• 体内研究：
  iGOT1-01 (compound 1a; 20 mg/kg; oral) has reasonable bioavailability and exposure properties in the female CD1 mice with 9 weeks old (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0–24 hours)=11734 hour•ng/mL). Animal Model: Female CD1 mice with 9 weeks old Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: Oral Result: Has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour•ng/mL).

• 参考文献：
  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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.121 ml	15.606 ml	31.212 ml
  5 mM	0.624 ml	3.121 ml	6.242 ml
  10 mM	0.312 ml	1.561 ml	3.121 ml
  50 mM	0.062 ml	0.312 ml	0.624 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *