中文名 | AM580 |
英文名 | 4-[(5,6,7,8-Tetrahydro-5,5,8,8-Tetramethyl-2-Naphthalenyl)Carboxamido]Benzoic Acid |
别名 | 化合物AM580 RARΑ激动剂(AM580) 4-(5,5,8,8-四甲基-5,6,7,8-四氢化萘-2-甲酰氨基)苯甲酸 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 |
英文别名 | AM580 AM 580 AM580 AM580 4-(1,1,4,4-Tetramethyltetralin-6-ylcarbonylamino)benzoic acid 4-((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbonyl)aminobenz 2-Naphthalenecarboxamide,5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-N-3-quinolinyl- 4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)benzoic acid 4-[(5,6,7,8-Tetrahydro-5,5,8,8-Tetramethyl-2-Naphthalenyl)Carboxamido]Benzoic Acid 4-[(5,6,7,8-TETRAHYDRO-5,5,8,8-TETRAMETHYL-2-NAPHTHALENYL)CARBOXAMIDO]BENZOIC ACID 4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydronaphthalene-2-ylcarbonylamino)benzoic acid Benzoic acid,4-[[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbonyl]amino]- |
CAS | 102121-60-8 |
化学式 | C22H25NO3 |
分子量 | 351.44 |
密度 | 1.154 |
熔点 | 265-267℃ |
沸点 | 485.24°C (rough estimate) |
溶解度 | 溶于DMSO (20mg/ml) 或乙醇 (10mg/ml)。 |
折射率 | 1.5614 (estimate) |
酸度系数 | 4.28±0.10(Predicted) |
存储条件 | -20°C |
稳定性 | 从提供的购买之日起稳定2年。DMSO中的溶液可以在-20 °C下储存长达3个月。 |
外观 | 白色至灰白色固体。 |
颜色 | Off-white |
体外研究 | In the presence of G-CSF, AM580 (at 10 -8 M) produces a remarkable induction in LAP mRNA of NB4 cells. At a concentration of 10 -5 M, AM580 and ATRA, in combination with G-CSF, induce almost the same level of LAP transcript. AM580 (at 10 -8 M) leads to an approximately sixfold increase in the steady-state levels of the transcript coding for the G-CSF receptor in NB4 cells. AM580 (50 nM) increases caspase-3 expression in all of the colonies, and in 30% of the colonies induce acinar-like cavitation. Knockdown of RARγ1 in primary Myc cells using shRARγ1 followed by Am580 treatment results in an even higher level of CRBP1 expression, showing that in these cells RARγ has a repressive effect on the RARα target gene CRBP1 . Am580 (200 nM) enhances the anti-proliferative effect exhibited by RARγ knockdown in the MCF-10A and MCF-7 cell lines but not in the MDA-MB-231 cells. |
体内研究 | Am580 (0.3 mg/kg/day) treatment has a more profound effect on tumor-free survival of MMTV-wnt1 mice, the effect being noticeable even in early appearing tumors, and no overt toxicity is found in liver, lungs, kidney, and spleen. Am580 treatment reduces substantially and equally the level of hyperplasia in both transgenic glands. Treatment of MMTV-Myc mice with the RARα-selective agonist Am580 leads to significant inhibition of mammary tumor growth, lung metastasis and extends tumor latency in 63% of mice. |
WGK Germany | 3 |
RTECS | DH6834890 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.845 ml | 14.227 ml | 28.454 ml |
5 mM | 0.569 ml | 2.845 ml | 5.691 ml |
10 mM | 0.285 ml | 1.423 ml | 2.845 ml |
5 mM | 0.057 ml | 0.285 ml | 0.569 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!