An inhibitor of ASCT2
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V-9302

Item No. 27688

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-2-amino-4-[bis[[2-[(3-methylphenyl)methoxy]phenyl]methyl]amino]-butanoic acid
CAS Number
1855871-76-9
Molecular Formula
C34H38N2O4
Formula Weight
538.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 20 mg/ml
SMILES
CC1=CC=CC(COC2=C(CN(CC3=C(OCC4=CC(C)=CC=C4)C=CC=C3)CC[C@H](N)C(O)=O)C=CC=C2)=C1
InChi Code
InChI=1S/C34H38N2O4/c1-25-9-7-11-27(19-25)23-39-32-15-5-3-13-29(32)21-36(18-17-31(35)34(37)38)22-30-14-4-6-16-33(30)40-24-28-12-8-10-26(2)20-28/h3-16,19-20,31H,17-18,21-24,35H2,1-2H3,(H,37,38)/t31-/m0/s1
InChi Key
YGKNVAAMULVFNN-HKBQPEDESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $209

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    10 mg

    $341

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    25 mg

    $653

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    Cayman Chemical
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    Product Description

    V-9302 is an inhibitor of amino acid transporter 2 (ASCT2).1 It inhibits glutamine uptake with IC50 values of 9 and 9.6 µM for the rat and human transporters, respectively. V-9302 also inhibits glutamine uptake in HEK293 cells and reduces cell viability of a variety of cancer cell lines, including HCT116, HT-29, COLO 205, and RKO cells (EC50s = 8.9, 9.4, 14.5, and 8.3 µM, respectively).2 It reduces glutamine uptake into tumor tissue and prevents tumor growth in HCT116 and HT-29 mouse xenograft models expressing K-RasG13D and BRAFV600E mutations, respectively, when administered at a dose of 75 mg/kg per day for 21 days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schulte, M.L., Khodadadi, A.B., Cuthbertson, M.L., et al. 2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport. Bioorg. Med. Chem. Lett. 26(3), 1044-1047 (2016).

    2. Schulte, M.L., Fu, A., Zhao, P., et al. Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical models. Nat. Med. 24(2), 194-202 (2018).