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LDC1267

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Catalog No. T2311Cas No. 1361030-48-9

LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM).

LDC1267

LDC1267

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🥰Excellent
Purity: 99.88%
Catalog No. T2311Cas No. 1361030-48-9
LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$70In StockIn Stock
10 mg$107In StockIn Stock
25 mg$173In StockIn Stock
50 mg$261In StockIn Stock
100 mg$396In StockIn Stock
1 mL x 10 mM (in DMSO)$85In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.88%
Color:White
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Product Introduction

Bioactivity
Description
LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM).
Targets&IC50
Axl:29 nM, Tyro3:8 nM, Mer:<5 nM
In vitro
In mice bearing B16F10 melanoma, intraperitoneal injection of LDC1267 (20 mg/kg) exhibits high safety and is capable of inhibiting tumor metabolism and enhancing the activity of anti-metastatic NK cells.
In vivo
In various cell lines, LDC1267 exhibits inhibition of cellular proliferation with an IC50 >5 μM. Moreover, in NKG2D-activated NK cells, LDC1267 can block the inhibitory effect induced by Gas6 stimulation.
Kinase Assay
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 Research
After incubation for 72?hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control.(Only for Reference)
Chemical Properties
Molecular Weight560.55
FormulaC30H26F2N4O5
Cas No.1361030-48-9
SmilesCCOc1cn(nc1C(=O)Nc1ccc(Oc2ccnc3cc(OC)c(OC)cc23)c(F)c1)-c1ccc(F)cc1C
Relative Density.1.32 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45.4 mg/mL (80.99 mM), Sonication is recommended.
Ethanol: 2 mg/mL (3.57 mM), Heating is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.89 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.7840 mL8.9198 mL17.8396 mL89.1981 mL
DMSO
1mg5mg10mg50mg
5 mM0.3568 mL1.7840 mL3.5679 mL17.8396 mL
10 mM0.1784 mL0.8920 mL1.7840 mL8.9198 mL
20 mM0.0892 mL0.4460 mL0.8920 mL4.4599 mL
50 mM0.0357 mL0.1784 mL0.3568 mL1.7840 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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