3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺
中文名称 | 3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 |
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中文同义词 | 3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺;化合物ALK5 INHIBITOR IV;83-01(DMSO溶液;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;A 83-01,ALK4、5和7激酶抑制剂 |
英文名称 | A-83-01 |
英文同义词 | A 83-01;A83-01;TGF inhibitor A-83-01;3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide;TGF-β RI Kinase Inhibitor IV;A 83-01, >=98%;3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide;A-83-01AB142092);ALK5 Inhibitor IV |
CAS号 | 909910-43-6 |
分子式 | C25H19N5S |
分子量 | 421.52 |
EINECS号 | |
相关类别 | 小分子抑制剂;TGF-β抑制剂;抑制剂;小分子抑制剂,天然产物;Inhibitors;Protein Kinase;TGF-beta/Smad |
Mol文件 | 909910-43-6.mol |
结构式 |
3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 性质
熔点 | 111℃ |
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沸点 | 590.0±60.0 °C(Predicted) |
密度 | 1.27±0.1 g/cm3(Predicted) |
储存条件 | -20°C |
溶解度 | DMSO:可溶5mg/mL,澄清(加热) |
酸度系数(pKa) | 8.77±0.70(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
稳定性 | 可在-20°下的DMSO中的溶液保存长达2个月。 |
Target | Value |
ALK7
(Cell-free assay) | 7.5 nM |
ALK5
(Cell-free assay) | 12 nM |
ALK4
(Cell-free assay) | 45 nM |
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC 50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC 50 s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (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 (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 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells.
安全信息
危险品标志 | Xn |
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危险类别码 | 22-36/37/38 |
安全说明 | 26-36 |
WGK Germany | 3 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/16 | S7692 | A-83-01 | 909910-43-6 | 1mg*5 | 794.43元 |
2024/01/16 | S7692 | 3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 A-83-01 | 909910-43-6 | 5mg | 843.13元 |