GSK2837808A

Name: GSK2837808A
Brand: MedChemExpress
SKU: HY-100681
Rating: 5.0 (24 reviews)

Cat. No.: HY-100681 Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC₅₀s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.

For research use only. We do not sell to patients.

GSK2837808A Chemical Structure

CAS No. : 1445879-21-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 197	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 197	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 138	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 820	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 24 publication(s) in Google Scholar

23 Publications Citing Use of MCE GSK2837808A

: GSK2837808A purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2023 May 23.; The conditioned media (CM) from hypoxia-treated NRK-52 E cells reduce the expression of FN, COL-Ⅰ, α-SMA and PCNA proteins in NRK-49 F cells after SSR (Shen Shuai II Recipe) and (or) GSK (GSK2837808A) treatment.

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Biological Activity
Protocol
Purity & Documentation
References
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Description

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC₅₀s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.

IC₅₀ & Target

IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A673	IC₅₀	> 57 μM Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
A673	IC₅₀	0.84 μM Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
MIA PaCa-2	IC₅₀	1.37 μM Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
MIA PaCa-2	IC₅₀	28.4 μM Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

649.62

Formula

C₃₁H₂₅F₂N₅O₇S

CAS No.

1445879-21-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)C1=CC(OC2=CC(F)=CC(F)=C2)=CC(NC3=C(S(=O)(NC4CC4)=O)C=NC5=CC(C6=CN=C(OC)N=C6OC)=CC=C35)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (76.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5394 mL	7.6968 mL	15.3936 mL
5 mM	0.3079 mL	1.5394 mL	3.0787 mL
10 mM	0.1539 mL	0.7697 mL	1.5394 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (257 KB)

Handling Instructions (2659 KB)

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]

Cell Assay ^[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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5394 mL	7.6968 mL	15.3936 mL	38.4840 mL
	5 mM	0.3079 mL	1.5394 mL	3.0787 mL	7.6968 mL
	10 mM	0.1539 mL	0.7697 mL	1.5394 mL	3.8484 mL
	15 mM	0.1026 mL	0.5131 mL	1.0262 mL	2.5656 mL
	20 mM	0.0770 mL	0.3848 mL	0.7697 mL	1.9242 mL
	25 mM	0.0616 mL	0.3079 mL	0.6157 mL	1.5394 mL
	30 mM	0.0513 mL	0.2566 mL	0.5131 mL	1.2828 mL
	40 mM	0.0385 mL	0.1924 mL	0.3848 mL	0.9621 mL
	50 mM	0.0308 mL	0.1539 mL	0.3079 mL	0.7697 mL
	60 mM	0.0257 mL	0.1283 mL	0.2566 mL	0.6414 mL

GSK2837808A Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK2837808A1445879-21-9Lactate DehydrogenaseLDHInhibitorinhibitorinhibit

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GSK2837808A

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GSK2837808A Related Antibodies

23 Publications Citing Use of MCE GSK2837808A

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Complete Stock Solution Preparation Table

GSK2837808A Related Classifications

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