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SGX523

Cat. No. M1777
SGX523 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 180 In stock
25mg USD 320 In stock
50mg USD 580 In stock
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Quality Control
Biological Activity

SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. SGX523, a novel, ATP-competitive kinase inhibitor remarkablefor its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. SGX523 is the most selective inhibitor of MET catalytic activity described to date and is thus a useful tool to investigate the role of MET kinase in cancer without the confounding effects of promiscuous protein kinase inhibition.

Protocol
Cell Experiment
Cell lines MDCK cells and A549 cells line (migration)
Preparation method Scatter and Migration Assays
To measure the effect of SGX523 on HGF-induced cell scatter, MDCK cells were plated at 1 × 103 per well in a 24-well plate and incubated at 37°C in 5% CO2 for 1 week in MEM and 10% fetal bovine serum. HGF (90 ng/mL) and various concentrations of SGX523 were added, and the cells were incubated for 18 h (37°C, 5% CO2 humidified incubator) and visualized. To investigate cell migration, A549 cells were plated in 12-well plates (6 × 104 per well) and incubated to confluence. A channel was introduced into the monolayers by scratching with a pipette tip. Various dilutions of compound were added in starve medium in the presence and absence of HGF (90 ng/mL). Twenty-four hours later, wells were checked for cell migration. Cells were stained and visualized as described.
Concentrations 0, 0.04, 0.12, 0.36 and 3 μ M
Incubation time 18h or 24h
Animal Experiment
Animal models Human GTL16 tumor xenografts in mice / U87MG tumor xenografts in mice
Formulation 20% isopropanol, 200 mmol/L ammonium acetate, and 100 mmol/L Tris-HCl (pH 7.5); 25% (v/v) glycerol
Dosages 10, 20, 30, and 100 mg/kg twice daily or 60 mg/kg daily starting at day 4 for 14 d / 10 or 60 mg/kg twice daily starting at day 5 for 22 d
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 359.41
Formula C18H13N7S
CAS Number 1022150-57-7
Purity 99.43%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2009). Figure 3. SGX523
Method immunoblot
Cell Lines GTL16 cells
Concentrations 10 μmol/L
Incubation Time 1 h
Results In the gastric cancer cell line GTL16, MET gene amplification leads to constitutive signaling, which is abolished by SGX523
Rating
References

MET kinase inhibitor SGX523 synergizes with epidermal growth factor receptor inhibitor erlotinib in a hepatocyte growth factor-dependent fashion to suppress carcinoma growth.
Zhang YW, et al. Cancer Res. 2010 Sep 1;70(17):6880-90. PMID: 20643778.

Species-specific metabolism of SGX523 by aldehyde oxidase and the toxicological implications.
Diamond S, et al. Drug Metab Dispos. 2010 Aug;38(8):1277-85. PMID: 20421447.

SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
Buchanan SG, et al. Mol Cancer Ther. 2009 Dec;8(12):3181-90. PMID: 19934279.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SGX523 supplier, c-Met, inhibitors

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