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    LDC1267
    LDC1267

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0638
    CAS #: 1361030-48-9Purity ≥98%

    Description: LDC1267 (LDC-1267) is a novel, highly potent and selective TAM (Tyro3, Axl and Mer) kinase inhibitor with potential antitumor activity. It inhibits Mer, Tyro3, and Axl with IC50s of<5 nM, 8 nM, and 29 nM respectively, and shows less effects against other kinases such as Met, Aurora B, Lck, Src, and CDK8. It showsexcellent in vivo antitumor efficacy in mouse B16F10 metastatic melanoma model.

    References: Nature. 2014 Mar 27;507(7493):508-12.

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    Molecular Weight (MW)560.55
    FormulaC30H26F2N4O5
    CAS No.1361030-48-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (178.4 mM)
    Water: <1 mg/mL
    Ethanol: 2 mg/mL (3.6 mM)
    Other ifo

    Chemical Name: N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide

    InChi Key: ISPBCAXOSOLFME-UHFFFAOYSA-N

    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)

    SMILES Code: O=C(C1=NN(C2=CC=C(F)C=C2C)C=C1OCC)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C(F)=C3

    SynonymsLDC-1267; LDC1267; LDC 1267.


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    In Vitro

    In vitro activity: LDC1267 moderately affects cell proliferation in 11 of 95 different cell lines with IC50 of >5μM. In NKG2D-activated NK cells, LDC1267 abolishes the inhibitory effects of Gas6 stimulation.


    Kinase Assay: For optimization of Axl/TAM receptor inhibitors, an Axl binding assay is established (HTRF method; Kinase tracer 236). This assay is based on the binding and displacement of the Alexa Fluor 647-labelled Kinase tracer 236 to each glutathione S-transferase (GST)-tagged kinase used in the binding assay. Binding of the tracer to the kinase was detected by using europium (Eu)-labelled anti-GST antibodies. Simultaneous binding of both the fluorescent tracer and the Eu-labelled antibodies to the GST-tagged kinase generates a fluorescence resonance energy transfer (FRET) signal. Binding of inhibitor to the kinase competes for binding with the tracer, resulting in a loss of the FRET signal. For the assay, the compound is diluted in 20 mM HEPES, pH 8.0, 1 mM DTT, 10 mM MgCl2 and 0.01% Brij35. Then, the kinase of interest (5 nM final concentration), fluorescent tracer (15 nM final concentration) and LanthaScreen Eu-anti-GST antibody (2 nM final concentration) are mixed with the respective compound dilutions (from 5 nM to 10 μM) and incubated for 1 h. The FRET signal is quantified using an EnVision Multilabellreader 2104. 


    Cell Assay:  After incubation for 72 hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control. Cell lines: A panel of 93 cancer cell lines and two primary cells (x axis, IMR90 and human peripheral blood mononuclear cells).

    In VivoIn B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, i.p.) efficiently enhances anti-metastatic NK cell activity, and rejects tumor metastases without serious cytotoxicity.
    Animal modelMouse B16F10 metastatic melanoma model
    Formulation & DosageDissolved in 90% PEG400:10% DMSO; 20 mg/kg; i.p.
    References

    Nature. 2014 Mar 27;507(7493):508-12.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    LDC1267

    a, TC-1 tumour growth in Cbl-b+/+ Rag2−/− and Cbl-b−/− Rag2−/− mice (mean ± s.e.m., n = 10 each). ***P < 0.001 (two-way analysis of variance (ANOVA), Bonferroni’s post-hoc test). b, Cbl-b and β-actin protein expression in Cbl-b+/+, Cbl-…Nature. 2014 Mar 27;507(7493):508-12.

    LDC1267

    a, In vitro Cbl-b-dependent ubiquitylation of Tyro3, Axl and Mer (anti-Ub). Control, no TAM receptors. Loading controls are shown. b, IFN-γ+ Cbl-b+/− and Cbl-b−/− NK cells (%) stimulated with anti-NKG2D antibodies in the presence of sol…Nature. 2014 Mar 27;507(7493):508-12.

    LDC1267

    a, Kinetics of primary 4T1 tumour cell growth in the mammary fat pad of control and anti-asialo GM1-treated mice that received LDC1267 or vehicle (mean ± s.e.m., n = 6–9 mice per group). NS, not significant (one-way ANOVA). Nature. 2014 Mar 27;507(7493):508-12.


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