PF-6683324 (Synonyms: Trk-IN-4)
目录号: PL12408 纯度: ≥99%
CAS No. :1799788-94-5
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中文名称
PF-6683324
英文名称
PF-6683324
英文别名
2-(((3S,4R)-3-Fluoro-1-(2-(4-(trifluoromethoxy)phenyl)acetyl)piperidin-4-yl)oxy)-5-(1-methyl-1H-imidazol-4-yl)nicotinamide;BDBM50457842;Chembl4215848;PF-6683324;2-((3R,4S)-3-Fluoro-1-(2-(4-(trifluoromethoxy)phenyl)acetyl)piperidin-4-yloxy)-5-(1-methyl-1H-imidazol-4-yl)nicotinamide;2-[[(3R,4S)-3-Fluoro-1-[[4-(trifluoromethoxy)phenyl]acetyl]piperidin-4-yl]oxy]-5-(1-methyl-1H-imidazol-4-yl)pyridine-3-carboxamide;PF06683324
Cas No.
1799788-94-5
分子式
C24H23F4N5O4
分子量
521.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-6683324 (Trk-IN-4) 是一种有效的 pan-Trk 抑制剂,抑制 TrkA,TrkB 和 TrkC 细胞,IC50 分别为 1.9 nM,2.6 nM 和 1.1 nM。具有抗痛觉过敏作用。
生物活性
PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with IC 50 s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
性状
Solid
IC50 & Target[1][2]
TrkA 1.9 nM (IC50, in cell-based assays) TrkB
体外研究(In Vitro)
PF-6683324 (Trk-IN-4) (Compound 10b) exhibits superb Trk selectivity with >95% inhibition of TrkA and >40% inhibition of only 1 other kinase VEGFR2 (cell-based assay for VEGFR2 IC50>5 μM). 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
参考文献
[1]. Bagal SK, et al. Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain. J Med Chem. 2018 Aug 9;61(15):6779-6800.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (191.77 mM)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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