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FGFR1/DDR2 inhibitor 1

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Catalog No. T11279Cas No. 2308497-58-5

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

FGFR1/DDR2 inhibitor 1

FGFR1/DDR2 inhibitor 1

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Purity: 99.43%
Catalog No. T11279Cas No. 2308497-58-5
FGFR1/DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$93In StockIn Stock
5 mg$228In StockIn Stock
10 mg$372In StockIn Stock
25 mg$612In StockIn Stock
50 mg$845In StockIn Stock
100 mg$1,230In StockIn Stock
1 mL x 10 mM (in DMSO)$253In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.43%
Appearance:Solid
Color:White
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Product Introduction

FGFR1/DDR2 inhibitor 1 AI Summary
FGFR1/DDR2 inhibitor 1 exhibits a wide range of bioactivities, including antiproliferative effects against various cell lines such as human KG1, NCI-H2286, FGFR1-fused human KG1, FGFR2-amplified human SNU16, NCI-H716, UM-UC-14 with FGFR3 mutation, and NCI-H2286 with DDR2 mutation, with differing IC50 values. It also inhibits several kinases like FGFR1, DDR2, ABL, ALK, AXL, BTK, c-Met, c-Src, CSF-1R, and CDK1. The compound demonstrates antitumor activity in NCI-H1581 cells xenografted in nude mice at different doses and exhibits reversible and time-dependent irreversible inhibition of several CYP enzymes in human liver microsomes. Moreover, it inhibits human ERG and shows specific pharmacokinetic parameters in mice, such as Tmax, Cmax, AUC, and MRT..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
FGFR1/DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
Targets&IC50
KG-1:108.4 nM , DDR2:3.2 nM, FGFR1:31.1 nM
Chemical Properties
Molecular Weight501.5
FormulaC28H22F3N5O
Cas No.2308497-58-5
SmilesCc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F
Relative Density.1.42 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: 250 mg/mL (498.5 mM), Sonication is recommended.
H2O: < 0.1 mg/mL (insoluble)
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (6.58 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
DMSO
1mg5mg10mg50mg
1 mM1.9940 mL9.9701 mL19.9402 mL99.7009 mL
5 mM0.3988 mL1.9940 mL3.9880 mL19.9402 mL
10 mM0.1994 mL0.9970 mL1.9940 mL9.9701 mL
20 mM0.0997 mL0.4985 mL0.9970 mL4.9850 mL
50 mM0.0399 mL0.1994 mL0.3988 mL1.9940 mL
100 mM0.0199 mL0.0997 mL0.1994 mL0.9970 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:
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2 Enter the in vivo formulation:
% DMSO
%
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% Saline/PBS/ddH2O

Dose Conversion

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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

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