A 83-01 sodium是一种选择性的 TGF-β 类型 I 受体 ALK5 激酶、类型 I 活化素/结节受体 ALK4 和类型 I 结节受体 ALK7 抑制剂,IC50 值分别为 12、45 和 7.5 nM。


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| 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[1]. 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[1]. 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[1]. 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[2]. 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[2]. A 83-01 sodium salt (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.23mL |
11.27mL 2.25mL 1.13mL |
22.55mL 4.51mL 2.25mL |
|
| CAS号 | 2828431-89-4 |
| 分子式 | C25H18N5NaS |
| 分子量 | 443.5 |
| SMILES Code | S=C(N1N=C(C2=NC(C)=CC=C2)C(C3=CC=NC4=CC=CC=C34)=C1)[N-]C5=CC=CC=C5.[Na+] |
| MDL No. | MFCD31630814 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(236.75 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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