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编 号:F756125
分子式:C28H28BF5N2O5S
分子量:610.4
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1mg
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5mg
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10mg
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生物活性:
STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.

体内研究:
STAT3-SH2 domain inhibitor 1 (compound 7; 5 and 15 mg/kg; i.p.; daily, for 20 d) exhibits superior antitumor activity in BALB/c male nude mice with gastric tumor xenografts.Animal Model:BALB/c male nude mice with gastric tumor xenografts
Dosage:5 and 15 mg/kg
Administration:Intraperitoneal injection; daily, for 20 days
Result:Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) of65.14% at 5 mg/kg and 79.13% at 15 mg/kg, respectively.

体外研究:
STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway.STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC50 values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively.STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells.
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