- DDR1-IN-1
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- $1.00 / 1KG
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2019-12-27
- CAS:1449685-96-4
- Min. Order: 1KG
- Purity: 97%-99.9%
- Supply Ability: 100kg
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| | DDR1-IN-1 Basic information |
| Product Name: | DDR1-IN-1 | | Synonyms: | TL4-44;DDR-IN-1;DDR1-IN-1;N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide;4-((4-ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-((2-oxoindolin-5-yl)oxy)phenyl)-3-(trifluoromethyl)benzamide;CS-1427;DDR1 inhibitor 1;Benzamide, N-[3-[(2,3-dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)- | | CAS: | 1449685-96-4 | | MF: | C30H31F3N4O3 | | MW: | 552.59 | | EINECS: | | | Product Categories: | | | Mol File: | 1449685-96-4.mol |  |
| | DDR1-IN-1 Chemical Properties |
| 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 |
| | DDR1-IN-1 Usage And Synthesis |
| 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). |
| | DDR1-IN-1 Preparation Products And Raw materials |
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