AGN-195183 (Synonyms: IRX-5183; VTP-195183; NRX-195183)
目录号: PL10805 纯度: ≥99%
CAS No. :367273-07-2
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中文名称
AGN-195183
中文别名
化合物 T14144
英文名称
AGN-195183
英文别名
AGN 195183;AGN-195183;IRX5183;RC87L028HU;NRX195183;4-(4-Chloro-3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)-2,6-difluorobenzoic acid;AGN195183;BDBM50120065;DB05653;Q27288046;4-[(4-Chloro-3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-amino]-2,6-difluoro-benzoic acid;4-[(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-6,7-dihyd;Benzoic acid, 4-[[(4-chloro-5,6,7,8-tetrahydro-3-hydroxy-5,5,8,8-tetraMethyl-2-naphthalenyl)carbonyl]aMino]-2,6-difluoro-;IRX5183 (NRX195183, VTP195183, AGN195183)
Cas No.
367273-07-2
分子式
C22H22ClF2NO4
分子量
437.86
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
AGN-195183 (IRX-5183) 是选择性的 RARα 激动剂,Kd 为 3 nM。AGN-195183 对 RARβ/γ 无活性。
生物活性
AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (K d =3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.
性状
Solid
IC50 & Target[1][2]
IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans)
体外研究(In Vitro)
AGN-195183 (IRX-5183; Compound 4) inhibits the growth of breast cancer cell lines, and is inactive in an in vivo model of topical irritation.AGN-195183 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3. AGN-195183 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. AGN-195183 is currently in Phase I/IIA clinical trials in cancer patients. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.
溶解度数据
In Vitro: DMSO : 11 mg/mL (25.12 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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