DDR1-IN-4

SKU: orb1691212

Description

DDR1-IN-4 is a potent and selective inhibitor of discoidin domain receptor 1 (DDR1), blocking its autophosphorylation and that of DDR2. This compound is a valuable research tool for investigating DDR1's role in cancer biology and chronic kidney disease, with utility in both in vitro and in vivo experimental models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2125676-13-1
• MW: 565.34
• Purity: 97.25% (May vary between batches)
• Formula: C₂₃H₂₀BrF₃N₆O₃
• SMILES: O=C(NCC(F)(F)F)CN1C(=O)C2(C=3C(Br)=CC=CC31)CCN(C(=O)C4=NC=5C=NNC5C=C4)CC2
• Target: Discoidin Domain Receptor (DDR)
• Solubility: DMSO:200 mg/mL (353.77 mM)

Bioactivity

• Target IC50:
  DDR2:1900 nM|DDR1:29 nM
• In Vivo:
  DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) maintains renal function and mitigates tissue damage in Col4a3 –/– mice, a preclinical model for Alport syndrome, through DDR1 phosphorylation inhibition. In this model, daily 90 mg/kg intraperitoneal injections reduced fibrosis, indicated by Picro Sirius Red, smooth muscle actin staining, collagen I levels, and decreased pDDR1 levels, demonstrating efficacy.
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• In Vitro:
  DDR1-IN-4 (Compound 2.45) exhibits dose-dependent inhibition of DDR1 phosphorylation in DDR1-overexpressing HT1080 cells, achieving over 70% inhibition at a 1 μM concentration, while maintaining selectivity against DDR2 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DDR1 IN 4, DDR1, DDR1IN4, DDR-1-IN-4, DDR1-IN-4, DDR2, DDR, DiscoidinDomainReceptor, DiscoidinDomainReceptor(DDR), Discoidin Domain Receptor, Discoidin Domain Receptor (DDR)

Compound Identifiers

PubChem CID

130301864