1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. SGX-523

SGX-523 

Cat. No.: HY-12019 Purity: >98.0%
Handling Instructions

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

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

SGX-523 Chemical Structure

SGX-523 Chemical Structure

CAS No. : 1022150-57-7

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10 mM * 1 mL in DMSO USD 95 In-stock
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2 mg USD 72 In-stock
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5 mg USD 120 In-stock
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10 mg USD 180 In-stock
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50 mg USD 540 In-stock
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100 mg USD 840 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SGX-523 purchased from MCE. Usage Cited in: Cancer Res. 2015 Nov 1;75(21):4548-59.

    c-Myc downregulation is essential for c-Met inhibition caused by growth arrest in MET-addicted cells. EBC-1, NCI-H1993, SNU-5, MKN-45, and HCC827 cells are treated with SGX-523 at 1 μM for 24 or 48 hours followed by immunoblotting analysis of cell-cycle regulators.
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    Description

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

    Clinical Trial
    Molecular Weight

    359.41

    Formula

    C₁₈H₁₃N₇S

    CAS No.

    1022150-57-7

    SMILES

    CN1N=CC(C2=NN3C(SC4=CC5=C(N=CC=C5)C=C4)=NN=C3C=C2)=C1

    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 : ≥ 3.6 mg/mL (10.02 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7823 mL 13.9117 mL 27.8234 mL
    5 mM 0.5565 mL 2.7823 mL 5.5647 mL
    10 mM 0.2782 mL 1.3912 mL 2.7823 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      SGX-523 is prepared in 0.5% sodium carboxymethyl cellulose[2].

    References

    Purity: >98.0%

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    Keywords:

    SGX-523SGX523SGX 523c-Met/HGFRInhibitorinhibitorinhibit

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    Product name:
    SGX-523
    Cat. No.:
    HY-12019
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