Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
D421663-1ml | 1ml | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $667.90 |
DDR Inhibitors
Synonyms | DDR1-IN-1|1449685-96-4|4-[(4-Ethylpiperazin-1-Yl)methyl]-N-{4-Methyl-3-[(2-Oxo-2,3-Dihydro-1h-Indol-5-Yl)oxy]phenyl}-3-(Trifluoromethyl)benzamide|DDR-IN-1|4-((4-Ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)ben |
---|---|
Specifications & Purity | Moligand™, 10mM in DMSO |
Biochemical and Physiological Mechanisms | DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2. |
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | Information DDR1-IN-1 DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2. Targets DDR1 (Cell-free assay); DDR2 (Cell-free assay) 105 nM; 413 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. Cell Research(from reference) Cell lines:U2OSWT, U2OSOWT and U2OSG707A cell lines Concentrations:~20 μM Incubation Time:48 h |
ALogP | 4.972 |
---|---|
HBD Count | 2 |
Rotatable Bond | 8 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
IUPAC Name | 4-[(4-ethylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(2-oxo-1,3-dihydroindol-5-yl)oxy]phenyl]-3-(trifluoromethyl)benzamide |
---|---|
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) |
InChi Key | AOZPVMOOEJAZGK-UHFFFAOYSA-N |
Canonical SMILES | CCN1CCN(CC1)CC2=C(C=C(C=C2)C(=O)NC3=CC(=C(C=C3)C)OC4=CC5=C(C=C4)NC(=O)C5)C(F)(F)F |
Isomeric SMILES | CCN1CCN(CC1)CC2=C(C=C(C=C2)C(=O)NC3=CC(=C(C=C3)C)OC4=CC5=C(C=C4)NC(=O)C5)C(F)(F)F |
PubChem CID | 72836888 |
Molecular Weight | 552.59 |
Enter Lot Number to search for COA:
DMSO(mg / mL) Max Solubility | 100 |
---|---|
DMSO(mM) Max Solubility | 180.9659965 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
---|---|
Signal | Warning |
Hazard Statements | H413:May cause long lasting harmful effects to aquatic life H302:Harmful if swallowed |
Precautionary Statements | P273:Avoid release to the environment. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |