GSK 2837808A

Tocris Bioscience | Catalog # 5189

Potent and selective LDHA inhibitor
Tocris Bioscience
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Key Product Details

Description

Potent and selective LDHA inhibitor

Product Description

GSK 2837808A is a potent and selective lactate dehydrogenase A and B (LDHA and LDHB) inhibitor (IC50 values are 2.6 and 43 nM for LDHA and LDHB respectively). Inhibits lactate production in selected cancer cell lines. Reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells. Inhibits proliferation and induces apoptosis in Snu398 cells. Inhibits transcription of histone 2B (H2B) gene in HCT116 and NCM460 cells. Cell permeable.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Product Specifications for GSK 2837808A

Molecular Weight

649.62

Formula

C31H25F2N5O7S

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid

CAS Number

1445879-21-9

PubChem ID

71533725

InChI Key

RZBCPMYJIARMGV-UHFFFAOYSA-N

SMILES

O=S(C2=C(NC3=CC(OC5=CC(F)=CC(F)=C5)=CC(C(O)=O)=C3)C1=CC=C(C6=CN=C(OC)N=C6OC)C=C1N=C2)(NC4CC4)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 64.96 100

Preparing Stock Solutions for GSK 2837808A

The following data is based on the product molecular weight 649.62.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.54 mL 7.70 mL 15.39 mL
5 mM 0.31 mL 1.54 mL 3.08 mL
10 mM 0.15 mL 0.77 mL 1.54 mL
50 mM 0.03 mL 0.15 mL 0.31 mL

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 42 publications citing the usage of this product.

Product Documents for GSK 2837808A

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for GSK 2837808A

For research use only

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  • Mouse oocytes lactate uptake
    Name: Anonymous
    Species: Mouse
    Assay Type: In Vitro
    Cell Line/Tissue: Oocytes
    Verified Customer | Posted 11/13/2023
    GSK 2837808A inhibitor titrations were performed at pH 6 with oocytes preincubated for 45 min in a different uptake buffer (75 mM NaCl, 2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Mes, pH 6) containing the required concentration of GSK 2837808A prior to measuring the uptake of L-[14C]lactate (0.5 mM).
    GSK 2837808A 5189

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