GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC 50 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.

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].

GS-493 (46 mg/kg; i.p.; daily for 27 days) inhibits tumor growth significantly in a murine xenograft model[1]. 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.

1710337-31-7

C21H14N6O8S

510.44

GS-493

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years