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Ddr1-In-1

Catalog No. T3337   CAS 1449685-96-4

DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2.

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Ddr1-In-1 Chemical Structure
Ddr1-In-1, CAS 1449685-96-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 77.00
10 mg In stock $ 117.00
25 mg In stock $ 180.00
50 mg In stock $ 288.00
100 mg In stock $ 450.00
1 mL * 10 mM (in DMSO) In stock $ 92.00
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Purity: 99.83%
Purity: 99.34%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2.
Targets&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 potentiates the antiproliferative activity of DDR1-IN-1. [1]
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).
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)
Molecular Weight 552.59
Formula C30H31F3N4O3
CAS No. 1449685-96-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (168.3 mM)

Ethanol: 4 mg/mL(7.23 mM), warming

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Kim HG, et al. ACS Chem Biol. 2013, 8(10), 2145-2150.

TargetMolCitations

1. Wang J, Xie S, Li N, et al. Matrix stiffness exacerbates the proinflammatory responses of vascular smooth muscle cell through the DDR1-DNMT1 mechanotransduction axis. Bioactive Materials. 2022 2. Liu G, Jin X, Wang H, et al.Downregulation of CYRI-B promotes migration, invasion and EMT by activating the Rac1-STAT3 pathway in gastric cancer.Experimental Cell Research.2022: 113453.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library NO PAINS Compound Library Fluorochemical Library Kinase Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Inhibitor Library Anti-COVID-19 Compound Library

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Keywords

Ddr1-In-1 1449685-96-4 Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) Discoidin Domain Receptor inhibit Ddr-1-In-1 Inhibitor Ddr1 In 1 Ddr1In1 inhibitor

 

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