ORM-15341 (Synonyms: BAY 1896953; ORM-15341)
目录号: PL04873 纯度: ≥98%
CAS No. :1297537-33-7
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中文名称
ORM-15341
中文别名
ORM-15341
英文名称
ORM-15341
英文别名
ORM-15341;ketodarolutamide;9EPS75QMTL;(S)-5-acetyl-N-(1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-1H-pyrazole-3-carboxamide;GMBPVBVTPBWIKC-NSHDSACASA-N;ZB1629;Q27272459;1H-Pyrazole-3-carboxamide, 5-acetyl-N-((1S)-2-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-1-methylethyl)-;(S)-3-acetyl-N-(1-(3-(3-chloro-4-cyano-phenyl)-1H-pyrazol-1-yl)propan-2-yl)-1H-pyrazole-5-carboxamide
Cas No.
1297537-33-7
分子式
C19H17ClN6O2
分子量
396.83
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ORM-15341是一种有效的雄激素受体(AR)拮抗剂, 作用于AR-HEK293细胞, IC50值为38 nM。
生物活性
ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct. IC50 value: 38 nM Target: androgen receptor in vitro: In competitive AR binding assays, the inhibition constant (Ki) values of ORM-15341 was 8 nM. ORM-15341 functions as a full antagonist for all tested mutant ARs , with IC50 of 25, 51, 700, and 1160 nM for wtAR, AR(F876L), AR(T877A), and AR(W741L).
性状
Solid
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
参考文献
[1]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007.
[2]. Toermaekangas Olli, et al. Preparation of heteroaryl carboxamides as androgen receptor modulators. From PCT Int. Appl. (2012), WO 2012143599 A1 20121026.
溶解度数据
In Vitro: DMSO : 100 mg/mL (252.00 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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