ERK5-IN-2
目录号: PL02923 纯度: ≥98%
CAS No. :1888305-96-1
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中文名称
ERK5-IN-2
英文名称
ERK5-IN-2
英文别名
ERK5-IN-2;4-(2-bromanyl-6-fluoranyl-phenyl)carbonyl-~{N}-pyridin-3-yl-1~{H}-pyrrole-2-carboxamide;4-(2-Bromo-6-fluorobenzoyl)-N-(pyridin-3-yl)-1H-pyrrole-2-carboxamide;9N8
Cas No.
1888305-96-1
分子式
C17H11BrFN3O2
分子量
388.19
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
ERK5-IN-2 是一种具有口服活性,亚微摩尔效力,选择性的 ERK5 抑制剂,对 ERK5 和 ERK5 MEF2D 的 IC50s 分别是 0.82 μM,3 μM。ERK5-IN-2 不与 BRD4 溴结构域相互作用。ERK5-IN-2 抑制肿瘤异种移植生长和 碱性成纤维细胞生长因子 (bFGF) 驱动的基质胶塞血管的生成。
生物活性
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC 50 s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
性状
Solid
IC50 & Target[1][2]
ERK5 0.82 μM (IC50) ERK5 MEF2D 3 μM (IC
体内研究(In Vivo)
ERK5-IN-2 (compound 46) (p.o.; 100?mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin.
ERK5-IN-2 (i.v. or p.o.; 10?mg/kg for 0.083-24?hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2?cell permeability assay in both human and mouse. 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
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543.
溶解度数据
In Vitro: DMSO : 250 mg/mL (644.01 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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