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GSK 2837808A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK 2837808A图片
CAS NO:1445879-21-9
包装:10mg
规格:98%
市场价:2552元
分子量:649.62

产品介绍
Potent, selective lactate dehydrogenase A (LDHA) inhibitor
CAS:1445879-21-9
分子式:C31H25F2N5O7S
分子量:649.62
纯度:98%
存储:Store at -20°C

Background:

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 1.9 and 14 nM for LDHA and LDHB, respectively.


GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR with EC50=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells[1].


Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is shown to be 69 mL/minute/kg in rats, which exceeds the animal liver blood flow. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL[1].


参考文献:
[1]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.