1. Protein Tyrosine Kinase/RTK
  2. Discoidin Domain Receptor
  3. DDR1-IN-4

DDR1-IN-4 

Cat. No.: HY-114173
Handling Instructions

DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.

For research use only. We do not sell to patients.

DDR1-IN-4 Chemical Structure

DDR1-IN-4 Chemical Structure

CAS No. : 2125676-13-1

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Description

DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively[1].

IC50 & Target[1].

DDR1

29 nM (IC50)

DDR2

1900 nM (IC50)

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].

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].

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.
Molecular Weight

565.34

Formula

C₂₃H₂₀BrF₃N₆O₃

CAS No.

2125676-13-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

DDR1-IN-4Discoidin Domain ReceptorAlportsyndromefibrosisInhibitorinhibitorinhibit

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DDR1-IN-4
Cat. No.:
HY-114173
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