中文名称: | A 83-01 促销 | ||||
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英文名称: | A 83-01 | ||||
别名: | 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide | ||||
CAS No: | 909910-43-6 | 分子式: | C25H19N5S | 分子量: | 421.52 |
CAS No: | 909910-43-6 | ||||
分子式: | C25H19N5S | ||||
分子量: | 421.52 |
基本信息
产品编号:A10095 |
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产品名称:A 83-01 |
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CAS: |
909910-43-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
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分子量 |
421.52 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
21mg/mL (49.81mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.3724mL |
11.8618mL |
23.7237mL |
5mM |
0.4745mL |
2.3724mL |
4.7447mL |
10mM |
0.2372mL |
1.1862mL |
2.3724mL |
生物活性
产品描述 |
一种ALK抑制剂,能抑制TGF-βⅠ型受体ALK-5和活化素IB型受体ALK-4及结节型受体ALK-7诱导的转录活性,其激酶结构域与ALK-5结构域高度相关, IC50分别为 12nM、45nM和7.5nM。 |
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靶点/IC50 |
ALK5 12nM (IC50) |
ALK4 45nM (IC50) |
ALK7 7.5nM(IC50) |
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 IC50 of 12nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45nM and 7.5nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83- 01 (1-10µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation. |
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体内研究 |
A 83-01 (50, 150 and 500μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells. |
推荐实验方法(仅供参考)
细胞实验: |
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HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay. |
动物实验: |
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Mice |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )