2,4-Thiazolidinedione, 3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]-
S49076
CAS: 1265965-22-7
Molecular Formula: C22H22N4O4S
2,4-Thiazolidinedione, 3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]- - Names and Identifiers
| Name | S49076 |
| Synonyms | S49076 CS-2684 S4 9076 S4-9076 2,4-Thiazolidinedione, 3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]- |
| CAS | 1265965-22-7 |
2,4-Thiazolidinedione, 3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]- - Physico-chemical Properties
| Molecular Formula | C22H22N4O4S |
| Molar Mass | 438.5 |
| Solubility | DMSO: ≥ 31 mg/mL |
| Storage Condition | -20℃ |
| In vitro study | S49076 effectively inhibits the phosphorylation of MET, AXL and FGFRs in cells and inhibits their downstream signaling in in vitro and in vivo experiments. In a cell model, S49076 inhibits MET-and FGFR2-dependent gastric cancer cells, prevents MET-driven migration of lung cancer cells, and inhibits colony formation of liver cancer cells expressing FGFR1/2 and AXL. S49076 inhibits cell viability, motility, three-dimensional colony formation of cancer cells expressing MET, AXL or FGFRs. |
| In vivo study | S49076 has significant anti-tumor activity in MET and FGFR dependent tumor grafts. S49076 has a high distribution in tumors, with a half-life of about 7 hours in tumors and less than 2 hours in blood at a dose of 3.125 mg/kg. At doses above 6.25 mg/kg, more than 50% of MET phosphorylation was inhibited for 16 hours. S49076 is also active in a model that is resistant to bevacizumab and is used in combination with bevacizumab to completely inhibit the growth of colon cancer xenografts. |
2,4-Thiazolidinedione, 3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.281 ml | 11.403 ml | 22.805 ml |
| 5 mM | 0.456 ml | 2.281 ml | 4.561 ml |
| 10 mM | 0.228 ml | 1.14 ml | 2.281 ml |
| 5 mM | 0.046 ml | 0.228 ml | 0.456 ml |
Last Update：2024-01-02 23:10:35
2,4-Thiazolidinedione, 3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]- - Reference Information
| biological activity | S49076 is a new and effective Met (c-Met), AXL/MER and FGFR1/2/3 inhibitor with IC50 lower than 20 nM. |
| target | TargetValue met (cell-free assay) 1 nm mer (cell-free assay) 2 nm axl (cell-free assay) 7 nm fgfr3 (cell-free assay) 15 nm fgfr2 (cell-free assay) 17 nm |
| Target | Value |
| Met (Cell-free assay) | 1 nM |
| Mer (Cell-free assay) | 2 nM |
| Axl (Cell-free assay) | 7 nM |
| FGFR3 (Cell-free assay) | 15 nM |
| FGFR2 (Cell-free assay) | 17 nM |
| in vitro study | S49076 effectively inhibited the phosphorylation of intracellular MET, AXL and FGFRs, and inhibited their downstream signals in vivo and in vitro experiments. In the cell model, S49076 inhibits MET-and FGFR2-dependent gastric cancer cells, prevents MET-driven migration of lung cancer cells, and inhibits colony formation of liver cancer cells expressing FGFR1/2 and AXL. S49076 inhibits three-dimensional colony formation in cell viability, motility, MET, AXL, or FGFRs-expressing cancer cells. |
| in vivo study | S49076 has significant anti-tumor activity in MET and FGFR dependent tumor grafts. S49076 has a high distribution in the tumor. When the dose is 3.125 mg/kg, its half-life in the tumor is about 7 hours, and it is less than 2 hours in the blood. At doses above 6.25 mg/kg, MET phosphorylation in excess of 50% was inhibited for a duration of 16 h. S49076 is also active in bevacizumab tolerant models. when used in combination with bevacizumab, it completely inhibits the growth of colon cancer xenografts. |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: S49076 Visit Supplier Webpage Request for quotationCAS: 1265965-22-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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