1. Protein Tyrosine Kinase/RTK
  2. FGFR
    c-Met/HGFR
  3. S49076

S49076 

Cat. No.: HY-12965 Purity: 98.99%
Handling Instructions

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.

For research use only. We do not sell to patients.

S49076 Chemical Structure

S49076 Chemical Structure

CAS No. : 1265965-22-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 116 In-stock
Estimated Time of Arrival: December 31
2 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 972 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

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Description

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.

IC50 & Target[1]

METD1246N

8 nM (IC50)

METY1248C

16 nM (IC50)

METD1246H

11 nM (IC50)

METY1248D

17 nM (IC50)

METY1248H

1 nM (IC50)

METM1268T

1 nM (IC50)

MET

1 nM (IC50)

FGFR1

18 nM (IC50)

FGFR1V561M

23 nM (IC50)

FGFR2

17 nM (IC50)

FGFR2N549H

19 nM (IC50)

FGFR3

15 nM (IC50)

AXL

7 nM (IC50)

MER

2 nM (IC50)

In Vitro

S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling. 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. Total inhibition of MET phosphorylation is seen after 2 hours of incubation with 10 nM S49076 and an with an IC50 of 2 nM. S49076 inhibits MET phosphorylation on this site in GTL-16 gastric carcinoma cells with an IC50 value of 3 nM. The IC50 for AXL inhibition by S49076 is 56 nM. S49076 inhibits AXL signaling via AKT with an IC50 of 33 nM[1].

In Vivo

In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 is established and correlated well with impact on tumor growth. MET, AXL, and the FGFRs have all been implicated in resistance to VEGF/VEGFR inhibitors such as bevacizumab. Combination of S49076 with bevacizumab in colon carcinoma xenograft models leads to near total inhibition of tumor growth. S49076 alone caused tumor growth arrest in bevacizumab-resistant tumors[1].

Molecular Weight

438.50

Formula

C₂₂H₂₂N₄O₄S

CAS No.

1265965-22-7

SMILES

O=C(N1CC2=CC3=C(NC(/C3=C\C4=CC(CN5CCOCC5)=CN4)=O)C=C2)SCC1=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (70.70 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2805 mL 11.4025 mL 22.8050 mL
5 mM 0.4561 mL 2.2805 mL 4.5610 mL
10 mM 0.2281 mL 1.1403 mL 2.2805 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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 (corresponding to 4 doubling times), 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°C. 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Female balb/c and swiss nu/nu mice are used in the study. The hydrochloride salt of S49076 is administered orally to mice in 1% (w/v) hydroxyethylcellulose in ammonium acetate buffer pH 4.5 in a volume of 200 μL per 20 g body weight. The maximal tolerated dose of S49076 in these mice is determined to be 100 mg/kg/d (5 days a week for at least 3 weeks). Bevacizumab is dissolved in PBS and administered intraperitoneally in a volume of 200 μL per 20 g body weight[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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S49076
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