Name: GS-493
Brand: TargetMol
SKU: T39167
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

25 mg

¥ 10,600

6-8周

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	SHP2:71 nM (IC50), PTP1B:3.17 μM (IC50), SHP1:2.08 μM (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.

化学信息

分子量	510.44
分子式	C₂₁H₁₄N₆O₈S
CAS No.	1710337-31-7
Smiles	OS(=O)(=O)c1ccc(N\N=C2/C(=O)N(N=C2c2ccc(cc2)N(=O)=O)c2ccc(cc2)N(=O)=O)cc1 \|c:14\|
密度	1.66 g/cm3 (Predicted)