895158-95-9|SC144|CsnPharm

CAS No.: 895158-95-9

SC144 Catalog No. CSN16588

Synonyms: SC144

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.

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400-920-2911

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tech@csnpharm.cn

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究

剂量

Mice: 100 mg/kg23536726} (p.o.), min = 0.3 mg/kg{{19221468 (i.p.), max = 100 mg/kg^[2] (i.p.); rat^[3] (i.p.): 5 mg/kg - 20 mg/kg

给药途径

p.o., i.p.

动物药代数据

Animal	Mice^[2]
Dose	25 mg/kg
Administration	i.p. p.o.
T_1/2	2.275 ± 1.77 h (i.p.) 1.643 h (p.o.)
T_max	1 h (i.p.) 1 h (p.o.)
C_max	3345 ± 926 ng/ml (i.p.) 312 g/ml (p.o.)
AUC	6684 ± 169 ng/ml·h (i.p.) 999 ng/ml·h (p.o.)

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1027 mL
- 15.5137 mL
- 31.0273 mL
- 5 mM
- 0.6205 mL
- 3.1027 mL
- 6.2055 mL
- 10 mM
- 0.3103 mL
- 1.5514 mL
- 3.1027 mL

技术信息

CAS号

895158-95-9

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H11FN6O

运输

蓝冰

分子量

322.30

别名

SC144

溶解度

DMSO	60.0 mg/mL (186.2 mM)
Water	insoluble

动物实验配方

30% propylene glycol+5% Tween 80+65% water

30 mg/mL

suspension

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