DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
| Molecular Weight | 417.44 |
| Formula | C23H20FN5O2 |
| CAS Number | 1644069-80-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 65 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Joseph S Baxter, et al. Mol Oncol. Resistance to DNA repair inhibitors in cancer
| Related Discoidin Domain Receptor Products |
|---|
| DDR1/2 inhibitor-2
DDR1/2 inhibitor-2 is a DDR1/DDR2 inhibitor, with IC50 values less than 100 nM. |
| WRG-28
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice. |
| BAY-826
BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively. |
| DDR1-IN-4
DDR1-IN-4 is an effective and selective inhibitor of disk peptide domain receptor 1 (DDR1) autophosphorylation, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively. |
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