Ddr1-In-1

SKU: orb1304310

Description

DDR1-IN-1 is a potent and selective small molecule inhibitor of the DDR1 kinase, demonstrating an IC50 of 105 nM and approximately 3-fold selectivity against DDR2. This tool compound is useful for investigating the role of DDR1 in fibrotic diseases and cancer progression in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1449685-96-4
• MW: 552.59
• Purity: 99.93%
• Formula: C₃₀H₃₁F₃N₄O₃
• SMILES: CCN1CCN(Cc2ccc(cc2C(F)(F)F)C(=O)Nc2ccc(C)c(Oc3ccc4NC(=O)Cc4c3)c2)CC1
• Target: Discoidin Domain Receptor (DDR)
• Solubility: Ethanol:4 mg/mL (7.24 mM);DMSO:26.67 mg/mL (48.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.97 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  DDR1:105 nM
• In Vitro:
  In U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger Inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiate the ant Proliferative activity of DDR1-IN-1.
• Cell Research:
  Cells are plated in triplicate at a density of 3000 cells per well in 96-well plates and 1500 cells per well in 384-well plates. Compounds of various concentration are added into plates for 48 hours. Cell viability is determined usin the CellTiter-Glo and CCK-8. Both assays are performed according to the manufacturer's instructions. For CellTiter-Glo assay, luminescence is determined in a multi-label reader. For CCK-8 assay, absorbance is measured in a microplate reader at 450 nM. Data are normalized to control group (DMSO) and represented b the mean of at least two independent measurement with s andard error < 0%. GI50 were calculated using Prism 5.0.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Discoidin Domain Receptor, Discoidin Domain Receptor (DDR), DiscoidinDomainReceptor, DiscoidinDomainReceptor(DDR), Ddr1 In 1, DDR1, DDR, Ddr1In1, Ddr-1-In-1, Ddr1-In-1, DDR2

Compound Identifiers

PubChem CID

72836888