An inhibitor of MCT1 and 2
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AR-C 155858

Item No. 14884

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[[(4S)-4-hydroxy-2-isoxazolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
CAS Number
496791-37-8
Molecular Formula
C21H27N5O5S
Formula Weight
461.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mM
SMILES
CN(C(C(C(C(N1OC[C@@H](O)C1)=O)=C(CC2=C(C)NN=C2C)S3)=C3N4CC(C)C)=O)C4=O
InChi Code
InChI=1S/C21H27N5O5S/c1-10(2)7-25-20-17(18(28)24(5)21(25)30)16(19(29)26-8-13(27)9-31-26)15(32-20)6-14-11(3)22-23-12(14)4/h10,13,27H,6-9H2,1-5H3,(H,22,23)/t13-/m0/s1
InChi Key
ISIVOJWVBJIOFM-ZDUSSCGKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $267

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    Product Description

    AR-C 155858 is an inhibitor of monocarboxylate transporter 1 (MCT1) and MCT2 (Kis = 2.3 and <10 nM, respectively, in Xenopus oocytes expressing the human receptors).1 It is selective for MCT1 and MCT2 over MCT4 (Ki = >10 μM). AR-C 155858 inhibits L-lactate uptake in and proliferation of murine 4T1 breast cancer cells (IC50s = 25 and 20.2 nM, respectively).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ovens, M.J., Davies, A.J., Wilson, M.C., et al. AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem. J. 425(3), 523-530 (2010).

    2. Guan, X., Bryniarski, M.A., and Morris, M.E. In vitro and in vivo efficacy of the monocarboxylate transporter 1 inhibitor AR-C155858 in the murine 4T1 breast cancer tumor model. AAPS J. 21(1), 3 (2018).