3-(6-Methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide, sodium salt

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A 83-01 Sodium Salt 3-(6-甲基吡啶-2-基)-N-苯基-4-(喹啉-4-基)-1H-吡唑-1-硫代甲酰胺钠盐 Cat No. FB15714Cas No. N/A

A 83-01 Sodium Salt is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50 values of 12, 45 and 7.5 nM, respectively.

规格	价格	促销价格	库存

18817579266

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18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2548 mL
- 11.2740 mL
- 22.5480 mL
- 5 mM
- 0.4510 mL
- 2.2548 mL
- 4.5096 mL
- 10 mM
- 0.2255 mL
- 1.1274 mL
- 2.2548 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号	N/A	储存条件	粉末 -20°C 3 年液体 -80°C 12 月
分子式	C25H18N5NaS	运输	蓝冰
分子量	443.50	别名

靶点数据

生物活性

描述Transforming growth factor (TGF)-beta signaling facilitates tumor growth and metastasis in advanced cancer. Use of inhibitors of TGF-beta signaling may thus be a novel strategy for the treatment of patients with such cancer. A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC₅₀s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively. A 83-01 sodium salt (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells. A 83-01 sodium salt (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation. A 83-01 sodium salt (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 sodium salt (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells.