A dual inhibitor of IDO1 and STAT3 activation
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CAY10763

Item No. 30593

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR)-α-[[1,4-dihydro-4-(hydroxyimino)-1-oxo-2-naphthalenyl]amino]-N-(3,5-dimethoxyphenyl)-benzenepropanamide
CAS Number
2364458-49-9
Molecular Formula
C27H25N3O5
Formula Weight
471.5
Purity
≥98%
Formulation (Request formulation change)
A solid
λmax
242 nm
SMILES
O=C(C1=C/2C=CC=C1)C(N[C@H](CC3=CC=CC=C3)C(NC4=CC(OC)=CC(OC)=C4)=O)=CC2=N/O
InChi Code
InChI=1S/C27H25N3O5/c1-34-19-13-18(14-20(15-19)35-2)28-27(32)25(12-17-8-4-3-5-9-17)29-24-16-23(30-33)21-10-6-7-11-22(21)26(24)31/h3-11,13-16,25,29,33H,12H2,1-2H3,(H,28,32)/b30-23+/t25-/m1/s1
InChi Key
BTNMSAUAXSTYIU-RLOMCBGXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $90

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    1 mg

    $168

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    5 mg

    $653

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    Cayman Chemical
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    Product Description

    CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50 = 46 nM) and STAT3 activation.1 It binds to STAT3 (Kd = 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in a B16/F10 murine melanoma model and a HepG2 mouse xenograft model when administered at doses of 100 and 10 mg/kg, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, R., Jing, X., Huang, X., et al. Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3. J. Med. Chem. 63(4), 1544-1563 (2020).