| Name | Ddr1-In-1 |
| Description | DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2. |
| 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 concentrations are added into plates for 48 hours. Cell viability is determined using 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 by the mean of at least two independent measurement with standard error <20%. GI50 were calculated using Prism 5.0.(Only for Reference) |
| Kinase Assay | General procedure for the EC50 test: DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na3VO4, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513). |
| 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 potentiates the antiproliferative activity of DDR1-IN-1. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 93 mg/mL (168.3 mM)
Ethanol : 4 mg/mL (7.23 mM), Heating is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Discoidin Domain Receptor | inhibit | Ddr-1-In-1 | Inhibitor | Ddr1 In 1 | Ddr1In1 | Ddr1-In-1 |
| Inhibitors Related | DDR-TRK-1 | DDR Inhibitor | VU6015929 | DDR1-IN-4 | FGFR1/DDR2 inhibitor 1 | WRG-28 | Sitravatinib | LCB 03-0110 | DDR1-IN-2 | Merestinib | (S)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-2-(pyrimidin-5-yl)-1,2,3,4-tetrahydroisoquinoline-7-carboxamide |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-COVID-19 Compound Library |
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