[CAS NO. 2125676-13-1] DDR1-IN-4
PRODUCTS SPECIFICATIONS [2125676-13-1]
DESCRIPTION [2125676-13-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 565.34 |
| Molecular Formula | C23H20BrF3N6O3 |
| SMILES | O=C(NCC(F)(F)F)CN1C(C2(CCN(C(C3=CC=C(NN=C4)C4=N3)=O)CC2)C5=C1C=CC=C5Br)=O |
Summary
DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC 50 values of 29 nM and 1.9 μM for DDR1 and DDR2 , respectively [1] .
IC50 & Target
|
DDR1 29 nM (IC 50 ) |
DDR2 1900 nM (IC 50 ) |
In Vitro
DDR1-IN-4 (Compound 2.45) shows a clear dose-dependent inhibition of DDR1 phosphorylation in HT1080 cells overexpressing DDR1, with greater than 70% inhibition of phosphorylation at a concentration of 1 μM, and retaining selectivity over inhibition of DDR2 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) preserves renal function and reduces tissue damage in Col4a3 –/– mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Col4a3 –/– mice, a mouse model phenocopying Alport syndrome [1] . |
| Dosage: | 90 mg/kg. |
| Administration: | Injected intraperitoneally daily. |
| Result: |
Resulted in a significant reduction of fibrosis evaluated by Picro Sirius Red, smooth muscle actin staining, and collagen I accumulation.
Significantly reduces the levels of pDDR1 in Col4a3 knockout mice compared to controls. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 442.21 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7688 mL | 8.8442 mL | 17.6885 mL |
| 5 mM | 0.3538 mL | 1.7688 mL | 3.5377 mL |
| 10 mM | 0.1769 mL | 0.8844 mL | 1.7688 mL |