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4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸

4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸

中文名稱4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸
中文同義詞4-[(5,6,7,8-四氫-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-5,6,7,8-四氫化萘-2-甲酰氨基)苯甲酸;RARΑ激動(dòng)劑(AM580);AM580 AM580;化合物AM580;AM580,RARΑ激動(dòng)劑;AM580,RARALPHA AGONISTS
英文名稱4-[(5,6,7,8-TETRAHYDRO-5,5,8,8-TETRAMETHYL-2-NAPHTHALENYL)CARBOXAMIDO]BENZOIC ACID
英文同義詞AM 580;4-[(5,6,7,8-TETRAHYDRO-5,5,8,8-TETRAMETHYL-2-NAPHTHALENYL)CARBOXAMIDO]BENZOIC ACID;2-Naphthalenecarboxamide,5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-N-3-quinolinyl-;Benzoic acid,4-[[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbonyl]amino]-;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)carbonyl)aminobenz;4-(1,1,4,4-Tetramethyltetralin-6-ylcarbonylamino)benzoic acid;4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydronaphthalene-2-ylcarbonylamino)benzoic acid
CAS號(hào)102121-60-8
分子式C22H25NO3
分子量351.44
EINECS號(hào)
相關(guān)類別信號(hào)轉(zhuǎn)導(dǎo)通路激酶抑制劑;細(xì)胞生物學(xué)試劑;Intracellular receptor
Mol文件102121-60-8.mol
結(jié)構(gòu)式4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 結(jié)構(gòu)式

4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 性質(zhì)

熔點(diǎn)265-267℃
沸點(diǎn)485.24°C (rough estimate)
密度1.154
折射率1.5614 (estimate)
儲(chǔ)存條件-20°C
溶解度溶于DMSO(20mg/ml)或乙醇(10mg/ml)。
形態(tài)白色至類白色固體。
酸度系數(shù)(pKa)4.28±0.10(Predicted)
顏色米白色
穩(wěn)定性可在-20°C下的DMSO中的溶液儲(chǔ)存長(zhǎng)達(dá)3個(gè)月。

4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 用途與合成方法

AM580是視黃酸核受體(RAR)激動(dòng)劑,對(duì)RARα, RARβ和RARγ的Kd值分別為8 nM, 131 nM 和450 nM。

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 Germany3
RTECS號(hào)DH6834890
海關(guān)編碼2924.29.7790

MSDS信息

提供商 語(yǔ)言
英文
更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-104754-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸
AM580
102121-60-85mg600元
2024/11/08HY-104754-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸
AM580
102121-60-810mM * 1mLin DMSO660元

4-[(5,6,7,8-四氫-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 上下游產(chǎn)品信息

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