2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor FLT3
  4. LDC1267

LDC1267 is a AXL/TAM/FLT3 inhibitor with IC50 values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia.

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CAS No. : 1361030-48-9

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Based on 10 publication(s) in Google Scholar

LDC1267 Related Antibodies

Top Publications Citing Use of Products

    LDC1267 purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    LDC1267 purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

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    Axl Mer Tyro3

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LDC1267 is a AXL/TAM/FLT3 inhibitor with IC50 values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia[1][2][3].

    IC50 & Target[1]

    Axl

    42 nM (IC50)

    MERTK

    130 nM (IC50)

    Tyro3

    63 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    Hs-578T IC50
    19 nM
    Compound: 7; LDC1267
    Inhibition of AXL in human Hs578t cells by homogeneous time-resolved fluorescence assay
    Inhibition of AXL in human Hs578t cells by homogeneous time-resolved fluorescence assay
    		[PMID: 26555154]
    In Vitro

    LDC1267 inhibits purified AXL, MERTK, and TYRO3 kinases with IC50 values of 42 nM, 130 nM, and 63 nM, respectively, and weakly inhibits purified FLT3 kinase with an IC50 of 2500 nM[1].
    LDC1267 (0.005-1 μmol/L; 30 min pre-incubation) potently and specifically inhibits GAS6-mediated AXL, AKT, and ERK1/2 phosphorylation in glioblastoma LN229 cells with IC50 values of 26, 25, and 48 nmol/L, respectively[2].
    LDC1267 (up to 10 μmol/L; 72 h) does not impair the viability of glioblastoma LN229 cells at concentrations up to 10 μmol/L[2].
    LDC1267 (1-2.5 μmol/L; 4 days) specifically inhibits GAS6-induced invasion of glioblastoma LN229 spheroids at 1 and 2.5 μmol/L without reducing 2D cell viability[2].
    LDC1267 (2.5 μmol/L; 24 h) does not disrupt the endo-lysosomal compartment in wild-type or AXL KO glioblastoma LN229 cells at 2.5 μmol/L[2].
    LDC1267 (2.5 μmol/L; 24 h) does not impair autophagic flux in wild-type or AXL KO glioblastoma LN229 cells at 2.5 μmol/L[2].
    LDC1267 (1-5 μM; 72 h) potently inhibits proliferation of K562-S and K562-R cells with IC50 values of 5 μM and 3 μM, respectively, in a dose-dependent manner[3].
    LDC1267 (4 μM for K562-S, 3 μM for K562-R, 4 μM combined with 0.25 μM Imatinib for K562-S; 72 h) interferes with the Wnt/β-catenin pathway in K562-S and K562-R cells by downregulating pathway regulators AXL-RTK and EYA3, and downstream targets c-Myc and Axin2, with enhanced effects when combined with Imatinib in K562-S cells[3].
    LDC1267 (4 μM; 72 h) does not induce apoptosis in K562-S or K562-R cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    LDC1267 Related Antibodies

    Western Blot Analysis[2]

    Cell Line: glioblastoma LN229 cells
    Concentration: 0.005-1 μmol/L (30-minute pre-incubation); 400 ng/mL GAS6 (10-minute stimulation)
    Incubation Time: 30 min (pre-incubation with LDC1267); 10 min (stimulation with GAS6)
    Result: Potently blocked GAS6-induced phosphorylation of AXL, AKT, and ERK1/2.
    Displayed IC50 values of 26 nmol/L for inhibition of AXL phosphorylation, 25 nmol/L for inhibition of AKT phosphorylation, and 48 nmol/L for inhibition of ERK1/2 phosphorylation.
    Inhibited phosphorylation of AXL, AKT, and ERK1/2 at closely matched concentrations, indicating specificity for AXL-mediated signaling.

    Cell Invasion Assay[2]

    Cell Line: glioblastoma LN229 cells grown as spheroids
    Concentration: 1-2.5 μmol/L
    Incubation Time: 4 days (with GAS6)
    Result: Blocked GAS6-induced invasion of LN229 spheroids at both tested concentrations.
    Did not affect the viability of 2D monolayer cultures of LN229 cells at these concentrations.

    Immunofluorescence[2]

    Cell Line: wild-type and AXL KO glioblastoma LN229 cells
    Concentration: 2.5 μmol/L
    Incubation Time: 24 h
    Result: Did not trigger changes in the distribution, number, or area of EEA1-positive early endosomes or LAMP1-positive late endosomes/lysosomes in either wild-type or AXL KO LN229 cells.

    Cell Proliferation Assay[3]

    Cell Line: Imatinib-sensitive K562 (K562-S), Imatinib-resistant K562 (K562-R)
    Concentration: 1-5 μM
    Incubation Time: 72 h
    Result: Exhibited a significant dose-dependent antiproliferative effect in both K562-S and K562-R cells.
    Reached an IC50 of 5 μM in K562-S cells and 3 μM in K562-R cells.

    RT-PCR[3]

    Cell Line: Imatinib-sensitive K562 (K562-S), Imatinib-resistant K562 (K562-R)
    Concentration: 4 μM (K562-S cells); 3 μM (K562-R cells); 4 μM LDC1267 combined with 0.25 μM Imatinib (K562-S cells)
    Incubation Time: 72 h
    Result: Significantly downregulated AXL-RTK (p-value 0.0005), EYA3 (p-value <0.0001), c-Myc (p-value <0.0001), and Axin2 (p-value <0.0001) in K562-S cells when used alone.
    Caused further significant downregulation of AXL-RTK, EYA3, c-Myc, and Axin2 (p-values <0.0001) in K562-S cells when combined with Imatinib.
    Significantly downregulated AXL-RTK (p-value <0.0001), EYA3 (p-value 0.0001), c-Myc (p-value <0.05), and Axin2 (p-value <0.0001) in K562-R cells.
    In Vivo
    Animal Model: C57BL/6J wild type mice (8-12 weeks old syngeneic bearing B16F10 cells)[1]
    Dosage: 20mg/kg
    Administration: Intraperitoneal injection; every 12 hours for 14 days
    Result: Markedly reduced metastatic spreading of melanomas.
    Molecular Weight

    560.55

    Formula

    C30H26F2N4O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC1=CC(NC(C2=NN(C3=CC=C(F)C=C3C)C=C2OCC)=O)=CC=C1OC4=CC=NC5=CC(OC)=C(OC)C=C54
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (89.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7840 mL 8.9198 mL 17.8396 mL
    5 mM 0.3568 mL 1.7840 mL 3.5679 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (17.84 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7840 mL 8.9198 mL 17.8396 mL 44.5991 mL
    5 mM 0.3568 mL 1.7840 mL 3.5679 mL 8.9198 mL
    10 mM 0.1784 mL 0.8920 mL 1.7840 mL 4.4599 mL
    15 mM 0.1189 mL 0.5947 mL 1.1893 mL 2.9733 mL
    20 mM 0.0892 mL 0.4460 mL 0.8920 mL 2.2300 mL
    25 mM 0.0714 mL 0.3568 mL 0.7136 mL 1.7840 mL
    30 mM 0.0595 mL 0.2973 mL 0.5947 mL 1.4866 mL
    40 mM 0.0446 mL 0.2230 mL 0.4460 mL 1.1150 mL
    50 mM 0.0357 mL 0.1784 mL 0.3568 mL 0.8920 mL
    60 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7433 mL
    80 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5575 mL
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    LDC1267 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    LDC12671361030-48-9LDC 1267LDC-1267TAM ReceptorFLT3Tyro3AxlMerCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3K562-S cellsAXLWnt/β-catenin signalingchronic myeloid leukemiaTYRO3MERTKK562-R cellsglioblastomaLN229 cellsInhibitorinhibitorinhibit

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