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GSK2837808A

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.

Catalog No. T15435Cas No. 1445879-21-9

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Purity:99.78%

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COA HNMR HPLC

GSK2837808A

Catalog No. T15435Cas No. 1445879-21-9

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.

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Pack Size	Price	Availability
1 mg	$40	In Stock
5 mg	$113	In Stock
10 mg	$179	In Stock
25 mg	$347	In Stock
50 mg	$479	In Stock
100 mg	$679	In Stock
1 mL x 10 mM (in DMSO)	$177	In Stock

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Product Introduction

Bioactivity

Description	GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.
Targets&IC50	LDHB:1.9 nM, LDHA:1.9 nM
In vitro	GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR (EC50=10 μM). LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels range from 400 nM to no effect (EC50 reported as 30 μM).
In vivo	GSK2837808A (p.o.; 50 mg/kg in rats; 100 mg/kg in mice) treatment, causes blood compound levels at or below the detection limit of 2.5 ng/mL. Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is displayed to be 69 mL/minute/kg in rats and it exceeds the animal liver blood flow.

Chemical Properties

Molecular Weight	649.62
Formula	C₃₁H₂₅F₂N₅O₇S
Cas No.	1445879-21-9

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 95 mg/mL (146.24 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5394 mL	7.6968 mL	15.3936 mL	76.9681 mL
5 mM	0.3079 mL	1.5394 mL	3.0787 mL	15.3936 mL
10 mM	0.1539 mL	0.7697 mL	1.5394 mL	7.6968 mL
20 mM	0.0770 mL	0.3848 mL	0.7697 mL	3.8484 mL
50 mM	0.0308 mL	0.1539 mL	0.3079 mL	1.5394 mL
100 mM	0.0154 mL	0.0770 mL	0.1539 mL	0.7697 mL

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In Vivo Formulation Calculator (Clear solution)

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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