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DDR1-IN-5 is a potent and selective inhibitor of the Discoidin Domain Receptor family, member 1 (DDR1). It effectively inhibits the phosphorylation of DDR1b (Y513) with an IC 50 value of 4.1 nM. Furthermore, DDR1-IN-5 demonstrates remarkable anti-cancer activity. Its inhibitory potency against DDR1 (IC 50 = 7.36 nM) makes it a promising compound for targeted therapy in cancer treatment.


| Description | DDR1-IN-5 is a potent and selective inhibitor of the Discoidin Domain Receptor family, member 1 (DDR1). It effectively inhibits the phosphorylation of DDR1b (Y513) with an IC 50 value of 4.1 nM. Furthermore, DDR1-IN-5 demonstrates remarkable anti-cancer activity. Its inhibitory potency against DDR1 (IC 50 = 7.36 nM) makes it a promising compound for targeted therapy in cancer treatment. |
| Targets&IC50 | DDR1:7.36 nM (IC50) |
| In vitro | DDR1-IN-5 (compound 121), when administered for 24 hours, hampers the production of collagen in human hepatic stellate LX-2 cells, demonstrating an inhibitory concentration (IC 50) of 62 nM[1]. A prolonged exposure of 72 hours to DDR1-IN-5 reveals cytotoxic effects on LX-2 cells, with a cytotoxic concentration (CC 50) exceeding 40 μM[1]. |
| Synonyms | DDR1-IN-5 |
| Molecular Weight | 434.382 |
| Formula | C22H13F3N6O |
| Cas No. | 2416022-90-5 |
| Smiles | Cc1ccc2c(Nc3cncc(c3)C(F)(F)F)noc2c1C#Cc1cnc2cccnn12 |
| Relative Density. | 1.45 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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