4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸
中文名称 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 |
---|---|
中文同义词 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸;4-(5,5,8,8-四甲基-5,6,7,8-四氢化萘-2-甲酰氨基)苯甲酸;RARΑ激动剂(AM580);AM580 AM580;化合物AM580;AM580,RARΑ激动剂 |
英文名称 | 4-[(5,6,7,8-TETRAHYDRO-5,5,8,8-TETRAMETHYL-2-NAPHTHALENYL)CARBOXAMIDO]BENZOIC ACID |
英文同义词 | 4-[[(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbonyl]amino]benzoic acid;NSC 608001;4-{[(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbonyl]amino}benzoic acid;benzoicacid,4-((5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbony;cd336;l)amino-;ro40-6055;AM 580 |
CAS号 | 102121-60-8 |
分子式 | C22H25NO3 |
分子量 | 351.44 |
EINECS号 | |
相关类别 | 信号转导通路激酶抑制剂;细胞生物学试剂;Intracellular receptor |
Mol文件 | 102121-60-8.mol |
结构式 |
4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 性质
熔点 | 265-267℃ |
---|---|
沸点 | 485.24°C (rough estimate) |
密度 | 1.154 |
折射率 | 1.5614 (estimate) |
储存条件 | -20°C |
溶解度 | 溶于DMSO(20mg/ml)或乙醇(10mg/ml)。 |
形态 | 白色至类白色固体。 |
酸度系数(pKa) | 4.28±0.10(Predicted) |
颜色 | 米白色 |
稳定性 | 可在-20°C下的DMSO中的溶液储存长达3个月。 |
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.
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.
安全信息
WGK Germany | 3 |
---|---|
RTECS号 | DH6834890 |
海关编码 | 2924.29.7790 |
提供商 | 语言 |
---|---|
英文
|
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-10475 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 AM580 | 102121-60-8 | 5mg | 600元 |
2024/08/19 | HY-10475 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 AM580 | 102121-60-8 | 10mM * 1mLin DMSO | 660元 |