Information S49076 is a novel, potent inhibitor ofMet (c-Met),AXL/MER, andFGFR1/2/3with IC50 values below 20 nmol/L. Targets Met (Cell-free assay); Mer (Cell-free assay); Axl (Cell-free assay); FGFR3 (Cell-free assay); FGFR2 (Cell-free assay) 16457,1 nM; 2 nM; 7 nM; 15 nM; 17 nM In vitro S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling in vitro and in vivo. In cell models, S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. S49076 inhibits viability, motility, and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs. In vivo S49076 shows marked antitumor activity in MET- and FGFR-dependent tumor xenografts at well-tolerated doses. S49076 has high distribution to tumors, in which the half-life for the dose of 3.125 mg/kg is approximately 7 hours versus less than 2 hours in the blood. At doses of 6.25 mg/kg and higher, more than 50% inhibition of MET phosphorylation is retained at 16 hours. S49076 is also active in a bevacizumab-resistant model and totally inhibits the growth of colon carcinoma xenografts in association with bevacizumab. Cell Research(from reference) Cell lines：GTL-16 and SNU-16 cell lines Incubation Time：96 h or 120 h
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S49076
Dangerous GoodsCAS number：1265965-22-7 molecular formula：C22H22N4O4S
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| Chinese alias | - | ||
| English alias | 1265965-22-7 | s8404 | 65ZUU7MATU | HY-12965 | CID 49870909 | S-49076(Free base) | 3-((3-((4-((4-Morpholinyl)methyl)-1H-pyrrol-2-yl)methylene)-2-oxo-2,3-dihydro-1H-indol-5-yl)methyl)-1,3-thiazolidine-2,4-dione | BS-14862 | BDBM50172080 | CCG-269111 | 2,4- | ||
| CAS number | 1265965-22-7 | molecular formula | C22H22N4O4S |
| molecular weight | 438.5 g/mol | Exact mass | ≥97% |
| PSA | 120.000 Ų | logp | 1.882 |
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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