GS-493

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GS-493 

GS-493 是一种选择性的酪氨酸磷酸酶 SHP2 (PTPN11) 抑制剂，IC50 为 71 nM，对 SHP2 的活性比 SHP1 和 PTP1B 高 29 倍和 45 倍。 GS-493 抑制细胞运动和癌细胞生长。GS-493 具有抗肿瘤活性。

GS-493

GS-493 Chemical Structure

CAS No. : 1710337-31-7

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生物活性

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[1].

IC50 & Target

IC50: 71 nM (SHP2); 2.08 μM (SHP1); 3.17 μM (PTP1B)[1]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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

上海金畔生物科技有限公司 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.

分子量

510.44

Formula

C21H14N6O8S
CAS 号

1710337-31-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Grosskopf S, et al. Selective inhibitors of the protein tyrosine phosphatase SHP2 block cellular motility and growth of cancer cells in vitro and in vivo. ChemMedChem. 2015;10(5):815-826.

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