S49076

Catalog No.S8404 Batch:S840401

Technical Data

Formula	C₂₂H₂₂N₄O₄S
Molecular Weight	438.50	CAS No.	1265965-22-7
Solubility (25°C)*	In vitro	DMSO	87 mg/mL (198.4 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.

Targets

Met ^[1] (Cell-free assay)	Mer ^[1] (Cell-free assay)	Axl ^[1] (Cell-free assay)	FGFR3 ^[1] (Cell-free assay)	FGFR2 ^[1] (Cell-free assay)	View More
1 nM	2 nM	7 nM	15 nM	17 nM	View More

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^[1].

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^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines GTL-16 and SNU-16 cell lines Concentrations -- Incubation Time 96 h or 120 h Method For GTL-16 and SNU-16 viability assays, cells are seeded in 96-well microplates at the appropriate density in media containing 10% FCS and supplemented 48 hours later with serial dilutions of S49076 in a final volume of 150 μL per well. After 96 hours (GTL-16) or 120 hours (SNU-16) incubation, 15 μL of a solution of 5 mg/mL MTT is added to each well and the plates are incubated for 4 hours at 37℃. The formazan metabolite is solubilized in SDS for SNU-16 and, following removal of the MTT solution, in DMSO for GTL-16. Global cell viability is estimated by measurement of optical density at 540 nm.
Animal Study:^{^[1]}	Animal Models Female balb/c and swiss nu/nu mice Dosages 50 or 100 mg/kg Administration oral administration

Cell Assay:^{^[1]}

Cell lines
GTL-16 and SNU-16 cell lines
Concentrations
--
Incubation Time
96 h or 120 h
Method
For GTL-16 and SNU-16 viability assays, cells are seeded in 96-well microplates at the appropriate density in media containing 10% FCS and supplemented 48 hours later with serial dilutions of S49076 in a final volume of 150 μL per well. After 96 hours (GTL-16) or 120 hours (SNU-16) incubation, 15 μL of a solution of 5 mg/mL MTT is added to each well and the plates are incubated for 4 hours at 37℃. The formazan metabolite is solubilized in SDS for SNU-16 and, following removal of the MTT solution, in DMSO for GTL-16. Global cell viability is estimated by measurement of optical density at 540 nm.

Animal Study:^{^[1]}

Animal Models
Female balb/c and swiss nu/nu mice
Dosages
50 or 100 mg/kg
Administration
oral administration

References

[1] Burbridge MF, et al. Mol Cancer Ther. 2013, 12(9):1749-62.

Selleck's S49076 has been cited by 1 publication

Axl receptor tyrosine kinase is a regulator of apolipoprotein E. [ Mol Brain, 2020, 4;13(1):66]	PubMed: 32366277

Axl receptor tyrosine kinase is a regulator of apolipoprotein E. [ Mol Brain, 2020, 4;13(1):66]

PubMed: 32366277

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.