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

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
2 mg USD 79 In-stock
5 mg USD 100 In-stock
10 mg USD 150 In-stock
25 mg USD 295 In-stock
50 mg USD 470 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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

    • Purity & Documentation

    • 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].

    MedChemExpress (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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 30 mg/mL (83.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: ≥99.0%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7823 mL 13.9117 mL 27.8234 mL 69.5584 mL
    5 mM 0.5565 mL 2.7823 mL 5.5647 mL 13.9117 mL
    10 mM 0.2782 mL 1.3912 mL 2.7823 mL 6.9558 mL
    15 mM 0.1855 mL 0.9274 mL 1.8549 mL 4.6372 mL
    20 mM 0.1391 mL 0.6956 mL 1.3912 mL 3.4779 mL
    25 mM 0.1113 mL 0.5565 mL 1.1129 mL 2.7823 mL
    30 mM 0.0927 mL 0.4637 mL 0.9274 mL 2.3186 mL
    40 mM 0.0696 mL 0.3478 mL 0.6956 mL 1.7390 mL
    50 mM 0.0556 mL 0.2782 mL 0.5565 mL 1.3912 mL
    60 mM 0.0464 mL 0.2319 mL 0.4637 mL 1.1593 mL
    80 mM 0.0348 mL 0.1739 mL 0.3478 mL 0.8695 mL
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    SGX-523 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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