GS-493

Name: GS-493
Brand: TargetMol
SKU: T39167
Price: -1 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T39167Cas号 1710337-31-7

GS-493, a highly specific protein tyrosine phosphatase SHP2 (PTPN11) inhibitor, exhibits remarkable potency with an IC50 of 71 nM. It displays 29- and 45-fold greater affinity towards SHP2 compared to its related counterparts, SHP1 and PTP1B, respectively. In addition, GS-493 impedes both cellular motility and growth of cancer cells, portraying promising antitumor effects.

GS-493

还可以

产品编号 T39167Cas号 1710337-31-7

规格	价格	库存	数量
25 mg	¥ 10,600	6-8周

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生物活性

产品描述	GS-493, a highly specific protein tyrosine phosphatase SHP2 (PTPN11) inhibitor, exhibits remarkable potency with an IC50 of 71 nM. It displays 29- and 45-fold greater affinity towards SHP2 compared to its related counterparts, SHP1 and PTP1B, respectively. In addition, GS-493 impedes both cellular motility and growth of cancer cells, portraying promising antitumor effects.
靶点活性	SHP1:2.08 μM (IC50), PTP1B:3.17 μM (IC50), SHP2:71 nM (IC50)
体外活性	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].
体内活性	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.