A multi-kinase inhibitor
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CEP-40783

Item No. 25749

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-1,2,3,4-tetrahydro-1-(1-methylethyl)-2,4-dioxo-5-pyrimidinecarboxamide
CAS Number
1437321-24-8
Synonyms
  • RXDX-106
Molecular Formula
C31H26F2N4O6
Formula Weight
588.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 5 mg/mlEthanol: 2 mg/ml
λmax
232, 240, 299 nm
SMILES
COC(C(OC)=C1)=CC2=C1C(OC3=C(F)C=C(NC(C4=CN(C(C)C)C(N(C5=CC=C(F)C=C5)C4=O)=O)=O)C=C3)=CC=N2
InChi Code
InChI=1S/C31H26F2N4O6/c1-17(2)36-16-22(30(39)37(31(36)40)20-8-5-18(32)6-9-20)29(38)35-19-7-10-26(23(33)13-19)43-25-11-12-34-24-15-28(42-4)27(41-3)14-21(24)25/h5-17H,1-4H3,(H,35,38)
InChi Key
FKCWHHYUMFGOPY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $312

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    25 mg

    $680

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    Product Description

    CEP-40783 is an inhibitor of the receptor tyrosine kinases Axl and c-MET (IC50s = 7 and 12 nM, respectively).1 It inhibits Axl in 293GT cells expressing Axl and c-MET in NCI H1299 non-small cell lung cancer (NSCLC) cells with IC50 values of 0.26 and 6 nM, respectively. It also inhibits the receptor tyrosine kinases TYRO3 and MER (IC50s = 3.5 and 1.89 nM, respectively).2 CEP-40783 (0.3 mg/kg) induces complete regression of tumors in an Axl/NIH3T3 mouse xenograft model and reduces the metastatic tumor burden in mouse orthotopic breast cancer models. It also induces tumor stasis and regression in an EBC-1 NSCLC mouse xenograft model when administered at doses of 3 and 10 mg/kg, respectively. CEP-40783 reduces tumor growth in an MC38 mouse syngeneic model concomitantly with an increase in leukocyte infiltration into tumors, the production of IFN-γ in natural killer cells, and the percentage of CD8+ T cells in tumor tissue.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miknyoczki, S.J., Cheng, M., Hudkins, R., et al. CEP-40783: A potent and selective AXL/c-Met inhibitor for use in breast, non-small cell lung (NSCLC), and pancreatic cancers. Mol. Cancer Ther. 12(11 Suppl), C275 (2013).

    2. Yokoyama, Y., Lew, E.D., Seelige, R., et al. Immuno-oncological efficacy of RXDX-106, a novel TAM (TYRO3, AXL, MER) family small-molecule kinase inhibitor. Cancer Res. 79(8), 1996-2008 (2019).