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

SGX-523 

Cat. No.: HY-12019 Purity: 99.28%
Handling Instructions

SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity.

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

SGX-523 Chemical Structure

SGX-523 Chemical Structure

CAS No. : 1022150-57-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 95 In-stock
Estimated Time of Arrival: December 31
Solid
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 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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.
    • Biological Activity

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    • References

    • Customer Review

    Description

    SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity[1].

    In Vitro

    SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), Ki=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), Ki=23 nM][1].
    SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC50s of 0.02, 0.113, and 0.035 µM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively[1].
    The IC50 value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells[1].
    SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM; 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells[1].

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

    Cell Viability Assay[1]

    Cell Line: Gastric cancer cell line GTL16
    Concentration: 4.6, 14, 40, 120, 370, 1100, 3300, 10000 nM
    Incubation Time: 1 hours
    Result: Abolished constitutive signaling induced by MET gene amplification.
    In Vivo

    SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth[2].

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

    Animal Model: Female Harlan nude mice (athymic nu/nu) were s.c. implanted with U87 cells[2]
    Dosage: 10 or 30 mg/kg
    Administration: Oral gavage; twice daily starting at day 5 for 22 days
    Result: Potently inhibited U87MG tumor growth at a dose of 10 mg/kg administered twice daily.
    Led to clear regression of U87MG tumors at 30 mg/kg dosed twice daily.
    Clinical Trial
    Molecular Weight

    359.41

    Formula

    C₁₈H₁₃N₇S

    CAS No.
    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 : 30 mg/mL (83.47 mM; Need ultrasonic)

    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: 99.28%

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