中文名 | A 83-01 |
英文名 | A 83-01 |
别名 | 化合物ALK5 INHIBITOR IV 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 | A83-01 A-83-01 A 83-01 A-83-01AB142092) ALK5 Inhibitor IV TGF inhibitor A-83-01 TGF-β RI Kinase Inhibitor IV 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide |
CAS | 909910-43-6 |
化学式 | C25H19N5S |
分子量 | 421.52 |
密度 | 1.27±0.1 g/cm3(Predicted) |
熔点 | 111℃ |
沸点 | 590.0±60.0 °C(Predicted) |
溶解度 | DMSO: 可溶5mg/mL,澄清 (温热) |
酸度系数 | 8.77±0.70(Predicted) |
存储条件 | -20°C |
稳定性 | 从提供的购买之日起稳定2年。在DMSO中的溶液可以在-20 ° 储存长达2个月。 |
外观 | 粉末 |
颜色 | white to beige |
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. |
危险品标志 | Xn - 有害物品 |
风险术语 | R22 - 吞食有害。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.372 ml | 11.862 ml | 23.724 ml |
5 mM | 0.474 ml | 2.372 ml | 4.745 ml |
10 mM | 0.237 ml | 1.186 ml | 2.372 ml |
5 mM | 0.047 ml | 0.237 ml | 0.474 ml |
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