Home Tools

SGX-523

Catalog No. T2293 CAS 1022150-57-7

SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SGX-523, CAS 1022150-57-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 44.00
2 mg	In stock	$ 61.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 143.00
25 mg	In stock	$ 293.00
50 mg	In stock	$ 473.00
100 mg	In stock	$ 693.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 99.6%

Purity: 99%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
Targets&IC50	MET:4 nM
In vitro	SGX523, administered orally twice daily at a dose of ≥10 mg/kg, significantly delays the anticipated growth of GTL16 tumors. At a higher concentration of 30 mg/kg, SGX523 not only markedly inhibits the growth of U87 mg tumors but also delays the growth of H441 tumors, while reducing the levels of MET autophosphorylation.
In vivo	SGX523, at nanomolar concentrations, inhibits MET-regulated signaling, cell proliferation, and migration without affecting signals dependent on other protein kinases, such as RON, even at micromolar levels. In vivo, SGX523 dose-dependently inhibits the growth of xenografts derived from human malignant gliomas, lung cancer, and gastric cancer, indicating these tumors' reliance on MET's catalytic activity. SGX-523 acts as a c-Met/hepatocyte growth factor receptor tyrosine kinase inhibitor, deactivating MET and preventing its interaction with other protein kinases. It significantly inhibits the catalytic domain of purified MET while having no effect on closely related RON. As an ATP-competitive inhibitor, SGX523 shows a higher affinity for low-activity and non-phosphorylated MET (MET-KD(0P), Ki: 2.7 nM).
Kinase Assay	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	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)

Molecular Weight	359.41
Formula	C18H13N7S
CAS No.	1022150-57-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.59 mg/mL (10 mM)

References and Literature

1. Buchanan SG, et al. Mol Cancer Ther, 2009, 8(12), 3181-3190.

Citations

1. Huang Y, Guo Y, Zhou Y, et al.Tivantinib alleviates inflammatory diseases by directly targeting NLRP3.iScience.2023

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library

Related Products

Related compounds with same targets

LY3009120 Sulindac sulfide AD80 PLX8394 SB-590885 PROTAC B-Raf degrader 1 K-Ras(G12C) Inhibitor 6 RAF265

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SGX-523 1022150-57-7 Angiogenesis Cytoskeletal Signaling MAPK Tyrosine Kinase/Adaptors Raf p38 MAPK c-Met/HGFR Bcr-Abl inhibit Inhibitor antitumor selective exquisitely MET SGX523 SGX 523 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.