DDR1/2 IN-4
DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis.
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- No. CAS: 3027967-95-6
- Fòrmula: C23H20F3N7O
- Peso molecular:467.45
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
DDR1 8.6 (pKi) |
DDR2 8.2 (pKi) |
In Vitro
DDR1/2 IN-4 potently binds to DDR1 (pKi=8.6) and DDR2 (pKi=8.2)[1].
DDR1/2 IN-4 potently inhibits DDR1 activity in U2OS cells, with a pIC50 of 8.0[1].
DDR1/2 IN-4 (1-30 μM; 48 h) shows no cytotoxicity against A549 cells at concentrations up to 10 μM, and only exhibits mild cytotoxicity after 48 h treatment at 30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:1-30 μM
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Incubation Time:48 h
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Result:Showed no cytotoxicity at concentrations up to 10 μM; reduced cell viability to 84.9% at 30 μM.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax (Plasma) | T1/2 | AUClast |
|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.n. | 117 (plasma) ng/g | 0.083 (plasma) h | 2 (plasma) h | 141 (plasma) ng·h/mL |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (male)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
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Administration:intranasal; single dose
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Result:Showed dose-dependent inhibition of pulmonary MCP-1 levels.
Caused a significant 39% reduction in pulmonary MCP-1 levels compared to the vehicle-treated, collagen-challenged group (p < 0.05) at 1 mg/kg.
Chemical Information
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No. CAS 3027967-95-6
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Peso molecular 467.45
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Fòrmula C23H20F3N7O
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SMILES
O=C(NC1=CC(C(F)(F)F)=CN=C1)C2=CC=C(C)C(NC3CN(C4=C5C=NC=CN5N=C4)C3)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DDR1/2 IN-4 Related Classifications
HY-181839 Related Classifications
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