GS-493
Based on 1 publication(s) in Google Scholar
GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1710337-31-7
- Formel: C21H14N6O8S
- Molecular Weight:510.44
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) GS-493
More
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 71 nM (SHP2); 2.08 μM (SHP1); 3.17 μM (PTP1B)[1]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HPAF-II | IC50 |
3.4 μM
Compound: 3; GS493
|
Inhibition of HGF-induced cell scattering in human HPAF-II cells incubated for 1 hr by Hoechst staining based assay
Inhibition of HGF-induced cell scattering in human HPAF-II cells incubated for 1 hr by Hoechst staining based assay
|
[PMID: 33210922] |
In Vitro
GS-493 (0.0625-10 μM) blocks hepatocyte growth factor (HGF)-stimulated epithelial-mesenchymal transition of human pancreatic adenocarcinoma (HPAF) cells[1].
GS-493 (40 μM, a couple of days) blocks growth of the human NSCL cancer cell line LXFA 526L in soft agar and decreases the number of tumor cell colonies to 32%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Nude mouse xenograft model (strain NMRI nu/nu mice)
-
Dosage:46 mg/kg (45.93 mg in 3 mL DMSO per kg)
-
Administration:i.p.; daily for 27 days
-
Result:Inhibited tumor growth significantly.
Chemical Information
-
CAS. Nr. 1710337-31-7
-
Molecular Weight 510.44
-
Formel C21H14N6O8S
-
SMILES
O=S(C1=CC=C(N/N=C2C(C3=CC=C([N+]([O-])=O)C=C3)=NN(C4=CC=C([N+]([O-])=O)C=C4)C/2=O)C=C1)(O)=O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Int Immunopharmacol
Clarithromycin-treated chronic spontaneous urticaria with the negative regulation of FcεRΙ and MRGPRX2 activation via CD300f. [Abstract]2022 Sep:110:109063. PMID: 35853276
Protokoll
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)