Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GS-493 1710337-31-7 GS493 GS 493 Inhibitor inhibitor inhibit