Ki23057: K-samII/FGF-R2 phosphorylation inhibitor for treatment of scirrhous gastric cancer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9850161 |
| CHEMBL ID | 352308 |
| SCHEMBL ID | 1249550 |
| MeSH ID | M0504674 |
| Synonym |
|---|
| bdbm50141809 |
| 2-(2-{4-[4-(4-tert-butyl-phenylamino)-phenoxy]-6-methoxy-quinolin-7-yloxy}-ethylamino)-ethanol |
| CHEMBL352308 , |
| SCHEMBL1249550 |
| 516523-31-2 |
| ki23057 |
| ki-23057 |
| FT-0745070 |
| 2-((2-((4-(4-((4-(tert-butyl)phenyl)amino)phenoxy)-6-methoxyquinolin-7-yl)oxy)ethyl)amino)ethanol |
| ki 23057 |
| unii-5zh5na7zmf |
| 5zh5na7zmf , |
| 2-((2-((4-(4-((4-(1,1-dimethylethyl)phenyl)amino)phenoxy)-6-methoxy-7-quinolinyl)oxy)ethyl)amino)ethanol |
| ethanol, 2-((2-((4-(4-((4-(1,1-dimethylethyl)phenyl)amino)phenoxy)-6-methoxy-7-quinolinyl)oxy)ethyl)amino)- |
| 2-[2-[4-[4-(4-tert-butylanilino)phenoxy]-6-methoxyquinolin-7-yl]oxyethylamino]ethanol |
Ki23057 is a small synthetic tyrosine kinase inhibitor. It blocks autophosphorylation of the VEGF receptor2 (VEGFR2)
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ki23057 is a new, small synthetic tyrosine kinase inhibitor that blocks autophosphorylation of the VEGF receptor2 (VEGFR2). " | ( A novel angiogenesis inhibitor, Ki23057, is useful for preventing the progression of colon cancer and the spreading of cancer cells to the liver. Hirakawa, K; Komatsu, M; Matsuzaki, T; Miwa, A; Ohira, M; Sakurai, K; Yamada, N; Yashiro, M, 2007) | 2.07 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.5369 | 10.0000 | AID67292 |
| Insulin-like growth factor 1 receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0003 | 0.4308 | 8.0000 | AID93464 |
| Hepatocyte growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 0.3722 | 10.0000 | AID219503 |
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.2745 | 0.0006 | 0.8007 | 8.5000 | AID155191; AID710557 |
| Mast/stem cell growth factor receptor Kit | Homo sapiens (human) | IC50 (µMol) | 0.0845 | 0.0007 | 0.4708 | 10.0000 | AID219501; AID710627 |
| Platelet-derived growth factor receptor alpha | Homo sapiens (human) | IC50 (µMol) | 0.4800 | 0.0001 | 0.4912 | 10.0000 | AID155191 |
| Fibroblast growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0785 | 0.0004 | 0.3276 | 8.6200 | AID710626; AID73463 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0760 | 0.0000 | 0.4830 | 8.8000 | AID216787; AID710632 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID15623 | Solubility after at pH 1.2 | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID67291 | Inhibition of EGF-receptor autophosphorylation in intact cells at 10 uM (inactive) | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID710557 | Inhibition of PDGFRbeta | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
| AID710632 | Inhibition of VEGFR2 | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
| AID219503 | Inhibition of c-Met autophosphorylation of in intact cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID89952 | Percent remaining after incubation with human liver microsomes for 10 min | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID710627 | Inhibition of c-Kit | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
| AID67292 | Inhibition of EGF-receptor autophosphorylation in intact cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID187078 | Percent remaining after incubation with rat liver microsomes for 40 min | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID89953 | Percent remaining after incubation with human liver microsomes for 40 min | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID710626 | Inhibition of FGFR2 | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
| AID15624 | Solubility after injection of water | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID219501 | Inhibition of c-Kit autophosphorylation in intact cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID93464 | Inhibition of IGF-receptor 1 autophosphorylation in intact cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID187077 | Percent remaining after incubation with rat liver microsomes for 10 min | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID73463 | In vitro inhibition against autophosphorylation of Fibroblast growth factor receptor 2 in the human scirrhous gastric carcinoma cell line | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID155191 | Inhibition of PDGF-receptor autophosphorylation in intact cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID93463 | Inhibition of IGF-receptor 1 autophosphorylation in intact cells at 10 uM (inactive) | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID216787 | Inhibition of vascular endothelial growth factor receptor 2 autophosphorylation in intact cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| AID219502 | Inhibition of c-Met autophosphorylation in intact cells at 10 uM (inactive) | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (57.14) | 29.6817 |
| 2010's | 3 (42.86) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.26) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||