SC144

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SC144 是一种口服活性小分子 gp130 抑制剂。

SC144 is an orally active small-molecule gp130 inhibitor.

SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM).The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 μM) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer.SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells.SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner.SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis. Apoptosis Analysis Cell Line:OVCAR-8 and Caov-3 cells Concentration:2 μM Incubation Time:24 hours Result:Significantly caused cell death in OVCAR-8 and Caov-3 cells.Western Blot Analysis Cell Line:OVCAR-8, Caov-3 cells Concentration:0.5-2 μM Incubation Time:0-6 hours Result:Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.

SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts.SC144 (100 mg/kg;p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group. Animal Model:Athymic mice (human ovarian cancer xenograft)Dosage:10 mg/kg Administration:I.p; daily for 58 days Result:Significantly inhibited tumor growth by about 73%.

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Cell Cycle/DNA Damage

DNA/RNA Synthesis

gp130

Cancer

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895158-95-9

322.3

C16H11FN6O

>98% (HPLC)

DMSO : 19.5 mg/mL. 60.50 mM;

Fc1cc2c(cc1)n1cccc1c(NNC(=O)c1cnccn1)n2

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(-20℃)

With Ice Pack

≥ 2 years