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909910-43-6

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
英文名称 A-83-01
CAS 909910-43-6
分子式 C25H19N5S
分子量 421.52
MOL 文件 909910-43-6.mol
更新日期 2024/04/28 11:56:10
909910-43-6 结构式 909910-43-6 结构式

基本信息

中文别名
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
英文别名
CS-578
A 83-01, >=98%
A 83-01
A83-01
A-83-01AB142092)
ALK5 Inhibitor IV
TGF inhibitor A-83-01
TGF-β RI Kinase Inhibitor IV
A83-01
A-83-01
A8301
A-8301
A 8301
TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide

物理化学性质

熔点111℃
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。

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335
危险品标志Xn
危险类别码22-36/37/38
安全说明26-36
WGK Germany3
3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/01/16S7692A-83-01909910-43-61mg*5794.43元
2024/01/16S76923-(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
909910-43-65mg843.13元
2024/01/16S76923-(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
909910-43-625mg2583.54元

常见问题列表

生物活性
A-83-01 是一种有效的 TGF-β type I receptor (ALK5-TD) 的抑制剂,其IC50值为12 nM。A-83-01 还抑制由 activin/nodal type I receptor (ALK4-TD) 和 nodal type I receptor (ALK7-TD) 诱导的转录,对应的IC50值分别为45 nM和7.5 nM。现配现用。
靶点
TargetValue
ALK7
(Cell-free assay)
7.5 nM
ALK5
(Cell-free assay)
12 nM
ALK4
(Cell-free assay)
45 nM
体外研究

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.

体内研究

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.

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