An MCT4 inhibitor
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MSC4381

Item No. 41135

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[2-[5-chloro-2-[[(5-ethoxy-8-quinolinyl)sulfonyl]amino]phenyl]ethynyl]-4-methoxy-2-pyridinecarboxylic acid
CAS Number
2445185-57-7
Molecular Formula
C26H20ClN3O6S
Formula Weight
538.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlMethanol: Slightly soluble: 0.1-1 mg/ml
SMILES
COC1=CC(C(O)=O)=NC=C1C#CC2=CC(Cl)=CC=C2NS(C3=CC=C(OCC)C4=CC=CN=C34)(=O)=O
InChi Code
InChI=1S/C26H20ClN3O6S/c1-3-36-22-10-11-24(25-19(22)5-4-12-28-25)37(33,34)30-20-9-8-18(27)13-16(20)6-7-17-15-29-21(26(31)32)14-23(17)35-2/h4-5,8-15,30H,3H2,1-2H3,(H,31,32)
InChi Key
FNBUZGRPJLEIMO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $120

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    10 mg

    $249

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    25 mg

    $524

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    100 mg

    $1,048

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    Cayman Chemical
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    Product Description

    MSC4381 is an inhibitor of monocarboxylate transporter 4 (MCT4; Ki = 0.011 µM).1 It selectively inhibits lactate efflux in MDA-MB-231 cells, which endogenously express high levels of MCT4, over SNU-398 cells, which endogenously express high levels of MCT1, and RT4 cells, which endogenously express MCT2 and MCT3 (IC50s = 0.001, >4, and 0.638 µM, respectively). MSC4381 (30 mg/kg) increases survival and reduces tumor volume in an MC-38 murine colorectal carcinoma model when administered in combination with an antibody targeting programmed cell death ligand 1 (PD-L1).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Heinrich, T., Sala-Hojman, A., Ferretti, R., et al. Discovery of 5-{2-[5-chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic acid, a highly selective in vivo useable chemical probe to dissect MCT4 biology. J. Med. Chem. 64(16), 11904-11933 (2021).

    2. Babl, N., Decking, S.-M., Voll, F., et al. MCT4 blockade increases the efficacy of immune checkpoint blockade. J. Immunother. Cancer 11(10), e007349 (2023).