Art. -Nr.: HY-12019

SGX-523

9 Cited Publications

Kundenbewertung

Based on 9 publication(s) in Google Scholar

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.51%
CAS. Nr.: 1022150-57-7
Formel: C₁₈H₁₃N₇S
Molecular Weight:359.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SGX-523 Chemical Structure

CAS. Nr.: 1022150-57-7

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10000 nM Compound: 1; SGX-523	Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
HCCLM3	IC₅₀	24 nM Compound: 1; SGX-523	Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
Huh-7	IC₅₀	>10000 nM Compound: 1; SGX-523	Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
MHCC97H	IC₅₀	11 nM Compound: 1; SGX-523	Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
MKN-45	IC₅₀	15 nM Compound: 1; SGX-523	Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-H1975	IC₅₀	>10000 nM Compound: 1; SGX-523	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-H1993	IC₅₀	25 nM Compound: 1; SGX-523	Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-N87	IC₅₀	>10000 nM Compound: 1; SGX-523	Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
SNU-5	IC₅₀	3.9 nM Compound: 1; SGX-523	Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]

In Vitro

SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), K_i=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), K_i=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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1022150-57-7
Appearance Solid
Molecular Weight 359.41
Formel C₁₈H₁₃N₇S
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All WB

Sort by:

Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Cancer Res

c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. [Abstract]

2015 Nov 1;75(21):4548-59. PMID: 26483207

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.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer. [Abstract]

2024 Feb 20;5(2):101388. PMID: 38262412
EMBO Mol Med

PlexinD1 is a driver and a therapeutic target in advanced prostate cancer. [Abstract]

2025 Feb;17(2):336-364. PMID: 39748059
Invest Ophthalmol Vis Sci

Hepatocyte Growth Factor Confers Trabecular Meshwork Stem Cell Resilience and Paracrine Protection of Trabecular Meshwork Cells in Glaucoma. [Abstract]

2026 Apr 1;67(4):1. PMID: 41920145
Toxicol Lett

SGX523 causes renal toxicity through aldehyde oxidase-mediated less-soluble metabolite formation in chimeric mice with humanized livers. [Abstract]

2023 Oct 1:388:48-55. PMID: 37806366
Biochem Biophys Res Commun

FAXC depletion contributes to tumor progression via the c-MET pathway in renal cell carcinoma. [Abstract]

2025 Sep 8:778:152388. PMID: 40706244
bioRxiv

Met regulates endoderm migration in zebrafish. [Abstract]

2026 May 5:2026.05.01.722050. PMID: 42146489

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Buchanan SG, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther, 2009, 8(12), 3181-3190. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SGX-523

9 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

SGX-523

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SGX-523

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SGX-523

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SGX-523

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SGX-523 Related Classifications

HY-12019 Related Classifications