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iGOT1-01

    
10mM in DMSO

源叶(MedMol)
T28919 一键复制产品信息
882256-55-5
C19H20N4O
320.39
iGOT101; iGOT1 01; iGOT1-01
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T28919-1ml
10mM in DMSO

¥780.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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
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参考文献

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摩尔浓度计算器

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