Product Name :
DDR1-IN-1
Description:
DDR1-IN-1 is a potent and selective DDR1 inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2. DDR1-IN-1 binds to DDR1 in the ‘DFG-out’ conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity as assessed against a panel of 451 kinases measured. DDR1-IN-1 provides a useful pharmacological probe for DDR1-dependent signal transduction. The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion.
CAS:
1449685-96-4
Molecular Weight:
552.59
Formula:
C30H31F3N4O3
Chemical Name:
4-((4-ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)benzamide
Smiles :
CC1=CC=C(C=C1OC1=CC2CC(=O)NC=2C=C1)NC(=O)C1=CC(=C(CN2CCN(CC2)CC)C=C1)C(F)(F)F
InChiKey:
AOZPVMOOEJAZGK-UHFFFAOYSA-N
InChi :
InChI=1S/C30H31F3N4O3/c1-3-36-10-12-37(13-11-36)18-21-6-5-20(15-25(21)30(31,32)33)29(39)34-23-7-4-19(2)27(17-23)40-24-8-9-26-22(14-24)16-28(38)35-26/h4-9,14-15,17H,3,10-13,16,18H2,1-2H3,(H,34,39)(H,35,38)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Pentagastrin} web|{Pentagastrin} Neuronal Signaling|{Pentagastrin} NF-κB|{Pentagastrin} Protocol|{Pentagastrin} References|{Pentagastrin} manufacturer}
Shelf Life:
≥360 days if stored properly.{{Irbesartan} site|{Irbesartan} Apoptosis|{Irbesartan} Technical Information|{Irbesartan} In Vitro|{Irbesartan} manufacturer|{Irbesartan} Autophagy}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:23880095
Additional information:
DDR1-IN-1 is a potent and selective DDR1 inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2. DDR1-IN-1 binds to DDR1 in the ‘DFG-out’ conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity as assessed against a panel of 451 kinases measured. DDR1-IN-1 provides a useful pharmacological probe for DDR1-dependent signal transduction. The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion.|Product information|CAS Number: 1449685-96-4|Molecular Weight: 552.59|Formula: C30H31F3N4O3|Synonym:|DDR1-IN1|DDR1-IN-1|DDR1-IN 1|DDR1-IN1.|Chemical Name: 4-((4-ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)benzamide|Smiles: CC1=CC=C(C=C1OC1=CC2CC(=O)NC=2C=C1)NC(=O)C1=CC(=C(CN2CCN(CC2)CC)C=C1)C(F)(F)F|InChiKey: AOZPVMOOEJAZGK-UHFFFAOYSA-N|InChi: InChI=1S/C30H31F3N4O3/c1-3-36-10-12-37(13-11-36)18-21-6-5-20(15-25(21)30(31,32)33)29(39)34-23-7-4-19(2)27(17-23)40-24-8-9-26-22(14-24)16-28(38)35-26/h4-9,14-15,17H,3,10-13,16,18H2,1-2H3,(H,34,39)(H,35,38)|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO, not in water|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥360 days if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 References:|Canning P, Tan L, Chu K, Lee SW, Gray NS, Bullock AN. Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors. J Mol Biol. 2014 Jun 26;426(13):2457-70. doi: 10.1016/j.jmb.2014.04.014. Epub 2014 Apr 23. PubMed PMID: 24768818; PubMed Central PMCID: PMC4058747.Products are for research use only. Not for human use.|