ERK1/2 inhibitor 1
目录号: PL02032 纯度: ≥99%
CAS No. :2095719-90-5
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中文名称
ERK1/2 inhibitor 1
英文名称
ERK1/2 inhibitor 1
英文别名
ERK1/2 inhibitor 1;(2R)-2-[5-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxo-1H-isoindol-2-yl]-N-[(1S)-2-hydroxy-1-(3-methylphenyl)ethyl]propanamide;(2~{R})-2-[5-[5-chloranyl-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxidanylidene-1~{H}-isoindol-2-yl]-~{N}-[(1~{S})-1-(3-methylphenyl)-2-oxidanyl-ethyl]propanamide;GTPL9973;BDBM50456348;compound 27 [PMID: 29775310];ESN
Cas No.
2095719-90-5
分子式
C29H32ClN5O4
分子量
550.05
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ERK1/2 inhibitor 1 是一种有效的,口服生物可利用的 ERK1/2 抑制剂,在 1 nM 时抑制 ERK1 达60%,抑制 ERK2 的 IC50 为 3.0 nM。
生物活性
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC 50 of 3.0 nM against ERK1 and ERK2, respectively.
性状
Solid
IC50 & Target[1][2]
ERK2 3.0 nM (IC50) ERK1
体外研究(In Vitro)
ERK1/2 inhibitor 1 (Compound 27) shows excellent antiproliferative potency with IC50s of 4.9 and 7.5 nM in A375 and Colo205 cells, respectively. 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]. Heightman TD, et al. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2018 Jun 14;61(11):4978-4992.
溶解度数据
In Vitro: DMSO : 250 mg/mL (454.50 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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