| 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: |
-80℃(运输条件:冰袋低温运输) |
| 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 |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |