GSK2837808A MedChemExpress (MCE)

Product Name	GSK2837808A
Synonyms	GSK2837808A GSK 2837808A(GSK2837808A) 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid 3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid Synonyms GSK2837808A GSK 2837808A(GSK2837808A) 3-((3-(N-Cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid 3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid Benzoic acid, 3-[[3-[(cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)-
CAS	1445879-21-9
EINECS
Chemical Formula	C31H25F2N5O7S
Molecular Weight	649.62
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg
Price	Email to quote
Descriptions	GSK2837808A GSK2837808A MedChemExpress (MCE) HY-100681 1445879-21-9 99.0% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions GSK2837808A GSK2837808A MedChemExpress (MCE) HY-100681 1445879-21-9 99.0% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, 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]. Mice: GSK2837808A is administered to male CD mice or male Sprague-Dawley rats orally or by intravenous (IV) infusion over 120 minutes into a femoral vein. Arterial blood samples are collected over time and GSK2837808A concentration is determined by liquid chromatography (LC)/MS/MS analysis[1]. Sixty thousand Snu398 cells per well are plated in 6-well tissue culture plates in RPMI-1640 medium supplemented with 2.5% charcoal-stripped FBS. Cells are allowed to attach overnight and then DMSO control or the indicated doses of LDHA inhibitor dissolved in DMSO are added directly to the wells. After 4 to 8 days of incubation in the indicated oxygen conditions, adherent cells are trypsinized, counted, and had their viability assessed by the trypan-blue exclusion method using the Vi-Cell XR Cell Viability Analyzer[1]. IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [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. [Content Brief]
Supplier Website	http://www.medchemexpress.com/GSK2837808A.html
Last Update	2025-10-14 16:03:33

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