产品说明书

SC144

Print
Chemical Structure| 895158-95-9 同义名 : -
CAS号 : 895158-95-9
货号 : A172019
分子式 : C16H11FN6O
纯度 : 99%+
分子量 : 322.297
MDL号 : MFCD25976763
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(49.64 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

生物活性
靶点

  • P-gp
描述 Drug resistance is caused by various cellular mechanism. One of the most important factors is the expression of a group of genes encoding ATP-dependent transporters of particular importance in drug resistance. SC144 showed its function through both exhibiting potent cytotoxicity, by itself or synergism with other compounds, against a panel of drug-sensitive and drug-resistant cancer cell lines, and targeting to gp130. Treatment with SC144 induced p-gp130-S782 in a time (2μM, 5min-6h)- and dose (0.5-2μM)-dependent manner in both OVCAR-8 and Caov-3 cells, suggesting the downregulation of cell surface expression of gp130. Consistent with the induced phosphorylation, the suppression on Stat3 signaling pathway, a downstream signaling cascade of gp130, and its target gene expression, including decrease of constitutive phosphorylation of Stat3, Survivin, MMP-7, D1, Bcl-XL, Bcl-2 and Ape1/Ref-1, can be observed after treatment with SC144 both in vitro and in vivo. For Gp130 is part of the receptor signaling complexes for at least 8 cytokines, suppression of gp130 by SC144 can inhibit downstream signaling induced by gp130 cytokines, including p-Stat3, p-Stat1 and p-Akt induced by LIF or Il-6. Daily intraperitoneal injection of SC144 at 10 mg/kg 5 days on and 2 days off for 58 days significantly inhibited OVCAR-8 tumor growth in mice[1]. Treatment with SC144 alone can cause growth inhibition of HT29 colon cancer cells with IC50 value of 0.9μM. Combined treatment with SC144 significantly enhanced the cytotoxicity of oxaliplatin in oxaliplatin-resistant HTOXAR3 cells. Co-treatment of SC144 with oxaliplatin in HT29 cells caused cell cycle arrest halting at S-phase[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells expressing p53 gene after 72 hrs by MTT assay, IC50=0.6 μM 17085054
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by MTT assay, IC50=0.9 μM 17085054
HT29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT29 cells after 72 hrs by MTT assay, IC50=0.9 μM 17085054
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.03mL

6.21mL

3.10mL
参考文献

[1]Xu S, Grande F, et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49.

[2]Oshima T, Cao X, et al. Combination effects of SC144 and cytotoxic anticancer agents. Anticancer Drugs. 2009 Jun;20(5):312-20.

[3]Zhao D, Han DF, et al. Roles of tumor necrosis factor-α and interleukin-6 in regulating bone cancer pain via TRPA1 signal pathway and beneficial effects of inhibition of neuro-inflammation and TRPA1. Mol Pain. 2019 Jan-Dec;15:1744806919857981.