A TAM family kinase inhibitor
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LDC-1267

Item No. 29459

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide
CAS Number
1361030-48-9
Molecular Formula
C30H26F2N4O5
Formula Weight
560.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 1 mg/mlEthanol: Partially soluble
λmax
236, 294, 322 nm
SMILES
COC(C(OC)=C1)=CC2=C1N=CC=C2OC3=CC=C(NC(C4=NN(C5=C(C)C=C(F)C=C5)C=C4OCC)=O)C=C3F
InChi Code
InChI=1S/C30H26F2N4O5/c1-5-40-28-16-36(23-8-6-18(31)12-17(23)2)35-29(28)30(37)34-19-7-9-25(21(32)13-19)41-24-10-11-33-22-15-27(39-4)26(38-3)14-20(22)24/h6-16H,5H2,1-4H3,(H,34,37)
InChi Key
ISPBCAXOSOLFME-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $76

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    10 mg

    $138

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    25 mg

    $275

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    Product Description

    LDC-1267 is a TAM family kinase inhibitor (IC50s = 5, 8, and 29 nM for Mer, Tyro3, and Axl, respectively).1 It is selective for TAM family kinases over a panel of 456 kinases at 1 μM, but does inhibit Met, Aurora B, LCK, and Src (IC50s = 35, 36, 51, and 338 nM, respectively). It inhibits suppression of proliferation and IFN-γ production induced by growth arrest-specific protein 6 (GAS6) in C-type lectin-like receptor NKG2D-activated natural killer (NK) cells. Adoptive transfer of NK cells pre-incubated with LDC-1267 decreases tumor growth but not metastasis in a B16/F10 murine melanoma model. LDC-1267 (20 mg/kg, i.p.) reduces the number of metastases in B16/F10 murine melanoma and 4T1 murine mammary carcinoma models in an NK cell-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Paolino, M., Choidas, A., Wallner, S., et al. The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature 507(7493), 508-512 (2014).