| Identification | Back Directory | [Name]
DDR1-IN-1 | [CAS]
1449685-96-4 | [Synonyms]
TL4-44
CS-1427
DDR-IN-1
DDR1-IN-1
DDR1 inhibitor 1
4-((4-ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-((2-oxoindolin-5-yl)oxy)phenyl)-3-(trifluoromethyl)benzamide
N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide
Benzamide, N-[3-[(2,3-dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)- | [Molecular Formula]
C30H31F3N4O3 | [MDL Number]
MFCD28144507 | [MOL File]
1449685-96-4.mol | [Molecular Weight]
552.59 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (180.97 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | [form ]
Powder | [color ]
Light yellow to yellow | [InChIKey]
AOZPVMOOEJAZGK-UHFFFAOYSA-N | [SMILES]
CC(C=CC(NC(C1=CC(C(F)(F)F)=C(CN2CCN(CC)CC2)C=C1)=O)=C3)=C3OC4=CC(CC(N5)=O)=C5C=C4 |
| Hazard Information | Back Directory | [Uses]
DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM)[1]. | [Definition]
ChEBI: DDR1-IN-1 is a secondary carboxamide resulting from the formal condensation of the carboxy group of 4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzoic acid with the amino group of 5-(5-amino-2-methylphenoxy)-1,3-dihydro-2H-indol-2-one. It is a potent inhibitor of discoidin domain receptor tyrosine kinase 1 and 2 (DDR1/2) with IC50 = 105 nM and 413 nM, respectively. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a N-alkylpiperazine, a member of benzamides, a member of (trifluoromethyl)benzenes, a secondary carboxamide, an aromatic ether and a member of oxindoles. | [Biochem/physiol Actions]
DDR1-IN-1 is a type II, subtype-selective discoidin domain receptor (DDR) tyrosine kinase inhibitor (DDR1/2 IC50 = 105 nM/413 nM) that 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 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture (123%, 70%, 50% of control, respectively, post 48-hr 250 nM DDR1-IN-1, 82.5 nM GSK2126458, or combined treatment). ent). ned treatment). | [References]
[1] Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. DOI:10.1021/cb400430t |
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| Company Name: |
Acesys Pharmatech
|
| Telephone: |
18860950986 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15849/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
|