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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, 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.
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 25 mg | ¥ 10,600 | 6-8周 |
GS-493 相关产品
| 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. |
| 分子量 | 510.44 |
| 分子式 | C21H14N6O8S |
| CAS No. | 1710337-31-7 |
| 密度 | 1.66 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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