Molecular Formula | C30H31F3N4O3 |
Molar Mass | 552.59 |
Solubility | DMSO: ≥ 41 mg/mL |
Storage Condition | -20℃ |
In vitro study | In U2OS cells, DDR1-IN-1 inhibited basal DDR1 autophosphorylation with an EC50 of 86 nM and a stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines with gain-of-function mutations and/or overexpression of DDR1, DDR1-IN-1 did not inhibit cell proliferation at concentrations below 10 μm, while GSK2126458 will enhance the antiproliferative activity of DDR1-IN-1. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.81 ml | 9.048 ml | 18.097 ml |
5 mM | 0.362 ml | 1.81 ml | 3.619 ml |
10 mM | 0.181 ml | 0.905 ml | 1.81 ml |
5 mM | 0.036 ml | 0.181 ml | 0.362 ml |
biological activity | DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor, with an IC50 of 105 nM, the selectivity is approximately 3-fold higher than for DDR2. |
Target | Value |
DDR1 (Cell-free assay) | 105 nM |
DDR2 (Cell-free assay) | 413 nM |