SGX-523

Catalog No.S1112

SGX-523 Chemical Structure

Molecular Weight(MW): 359.41

SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.

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2 Customer Reviews

  • Association of c-Met phosphorylation and s-Met generation in EBC-1 xenograft tumor. Mice were treated with SGX523 at 10 mg/kg, 3 mg/kg, 0.1 mg/kg, at 0 h and 8 h point, respectively. Plasma and tumor lysates were collected using the method described in "Materials and methods"section at 24 h time point. The bar and line in the figure represents the average phosphorylation rate of c-Met and s-Met in subgroups, respectively. Each subgroup consists of four mice with tumor volume around 600 mm3.

    Biomarkers 2013 18(2), 126-35. SGX-523 purchased from Selleck.

    After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of SGX-523 for 3h,followed by 15-minute stimolation of 100ng/ml HGF.

     

     

    Dr. Zhang of Tianjin Medical University. SGX-523 purchased from Selleck.

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Choose Selective c-Met Inhibitors

Biological Activity

Description SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.
Targets
c-Met [1] B-Raf (V599E) [1] C-Raf [1] Abl [1] p38α [1]
4 nM >7 μM >7 μM >7 μM >7 μM
In vitro

SGX-523 belongs to the class of c-Met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors. SGX-523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for its selectivity. SGX523 potently inhibits the purified MET catalytic domain but not the closely related receptor tyrosine kinase RON. SGX523 indicates ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), with a Ki of 2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), with a Ki of 23 nM], a phenomenon consistent with preferential binding to an inactive enzyme conformation. SGX523 inhibits MET-mediated signaling, cell proliferation and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations.[1]

In vivo SGX523 significantly retards the growth of preestablished GTL16 tumors when administered orally at doses of ≥10 mg/kg twice daily. SGX523 potently inhibits U87MG tumor growth; at 30 mg/kg dosed twice daily, SGX523 leads to clear regression of U87MG tumors. SGX523, dosed twice daily at 30 mg/kg, also retards the growth of H441 tumors with concomitant reduction in tumor MET autophosphorylation levels. SGX523 inhibition of MET in vivo is associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma, lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity. [1]

Protocol

Kinase Assay:[1]
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Kinase assays:

Initial rate constants are measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) are quenched with 20 μL Kinase-Glo detection buffer. Luminescence is detected in a plate-reading luminometer and the results are analyzed by nonlinear regression.
Cell Research:[1]
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  • Cell lines: MDCK cells
  • Concentrations: 200 nM
  • Incubation Time: 18 hours
  • Method: MDCK cells are seeded 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 are added and the cells are incubated for another 18 hours (37 °C, 5% CO2 humidified incubator) and visualized. A549 cells are plated in 12-well plates (6 × 104 per well) and incubated to confluence to investigate cell migration. A channel is introduced into the monolayers by scratching with a pipette tip. Various dilutions of compound are added in starve medium in the presence and absence of HGF (90 ng/mL).The wells are checked for cell migration after twenty-fou
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: GTL16, U87, or H441 xenografts in Harlan nude mice
  • Formulation: 0.5% MC 400 with 0.05% Tween 80
  • Dosages: 60 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL warmed (8.34 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% methylcellulose+0.2% Tween 80 30 mg/mL

* 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.

Chemical Information

Molecular Weight 359.41
Formula

C18H13N7S

CAS No. 1022150-57-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00606879 Terminated Advanced Cancer SGX Pharmaceuticals, Inc. January 2008 Phase 1
NCT00607399 Terminated Advanced Cancer SGX Pharmaceuticals, Inc. January 2008 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID