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编 号:F747148
分子式:C17H21Cl2N5S
分子量:398.35
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生物活性:
SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells.

体外研究:
SHP2-IN-8 (compound TK-453) (0-100 μM; 48 hours) has moderate inhibitory effects on the proliferation of KYSE-70, Hela and THP-1 cells.SHP2-IN-8 (0-30 μM; 24 hours) induces the apoptosis of Hela cells in a concentration-dependent manner.SHP2-IN-8 (0-30 μM; 0-2 hour)concentration- and time-dependently inhibits the phosphorylation of AKT in Hela and KYSE-70 cell lines.
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