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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, CAS 1449685-96-4

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Purity: 98%

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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	552.598
Formula	C30H31F3N4O3
CAS No.	1449685-96-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 93 mg/mL (168.3 mM)

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

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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

Citations

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Inhibitor Library Fluorochemical Library Anti-COVID-19 Compound Library Kinase Inhibitor Library Neuronal Signaling Compound Library Bioactive Compound Library Tyrosine Kinase Inhibitor Library

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Related compounds with same targets

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Keywords

Ddr1-In-1 1449685-96-4 蛋白酪氨酸激酶 Discoidin Domain Receptor (DDR) Discoidin Domain Receptor inhibit Ddr-1-In-1 Inhibitor Ddr1 In 1 Ddr1In1 inhibitor

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