LDC1267

Catalog No.S7638 Batch:S763801

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Technical Data

Formula

C30H26F2N4O5
Molecular Weight 560.55 CAS No. 1361030-48-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (178.39 mM)
Ethanol 2 mg/mL (3.56 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
Targets
Mer [1]
(Cell-free assay)		 Tyro3 [1]
(Cell-free assay)		 Axl [1]
(Cell-free assay)
<5 nM 8 nM 29 nM
In vitro 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. [1]
In vivo In B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, i.p.) efficiently enhances anti-metastatic NK cell activity, and rejects tumor metastases without serious cytotoxicity. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Kinase binding assays

    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:[1]
  • Cell lines

    A panel of 93 cancer cell lines and two primary cells (x axis, IMR90 and human peripheral blood mononuclear cells)

  • Concentrations

    ~30 μM

  • Incubation Time

    72 hours

  • Method

    After incubation for 72 hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control.
Animal Study:[1]
  • Animal Models

    Mouse B16F10 metastatic melanoma model

  • Dosages

    20 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2018, 9(5): 6402-6415]

Selleck's LDC1267 has been cited by 10 publications

Isthmin-1 is an adipokine that promotes glucose uptake and improves glucose tolerance and hepatic steatosis [ Cell Metab, 2021, S1550-4131(21)00326-0] PubMed: 34348115
TYRO3 induces anti-PD-1/PD-L1 therapy resistance by limiting innate immunity and tumoral ferroptosis [ J Clin Invest, 2021, 131(8)e139434 139434] PubMed: 33855973
TYRO3 induces anti-PD-1/PD-L1 therapy resistance by limiting innate immunity and tumoral ferroptosis [ J Clin Invest, 2021, 131(8)139434] PubMed: 33855973
Roles of Sialic Acid, AXL, and MER Receptor Tyrosine Kinases in Mumps Virus Infection of Mouse Sertoli and Leydig Cells [ Front Microbiol, 2020, 11:1292] PubMed: 32695074
Tyrosine Kinase Receptors Axl and MerTK Mediate the Beneficial Effect of Electroacupuncture in a Cuprizone-Induced Demyelinating Model [ Evid Based Complement Alternat Med, 2020, 2020:3205176] PubMed: 32714402
TAM Kinases Promote Necroptosis by Regulating Oligomerization of MLKL [ Mol Cell, 2019, 10.1016/j.molcel.2019.05.022] PubMed: 31230815
Serotonin receptors 2A and 1A modulate anxiety-like behavior in post-traumatic stress disordered mice [ Am J Transl Res, 2019, 11(4):2288-2303] PubMed: 31105836
RAS-MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade [ Mol Cancer Ther, 2018, 17(7):1526-1539] PubMed: 29654068
DAPK and CIP2A are involved in GAS6/AXL-mediated Schwann cell proliferation in a rat model of bilateral cavernous nerve injury. [ Oncotarget, 2018, 9(5):6402-6415] PubMed: 29464081
Axl inhibitor R428 induces apoptosis of cancer cells by blocking lysosomal acidification and recycling independent of Axl inhibition [Chen F Am J Cancer Res, 2018, 8(8):1466-1482] PubMed: 30210917

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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