FR 180204
目录号: PL02562 纯度: ≥99%
CAS No. :865362-74-9
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中文名称
FR 180204
中文别名
5-(2-苯基吡唑并[1,5-A]吡啶-3-基)-1H-吡唑并[3,4-C]哒嗪-3-胺;FR 180204 抑制剂;5-(2-苯基吡唑并[1,5-a]吡啶-3-基)-1H-吡唑并[3,4-c]哒嗪-3-胺
英文名称
FR 180204
英文别名
5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine;5-(2-PHENYL-PYRAZOLO[1,5-A]PYRIDIN-3-YL)-1H-PYRAZOLO[3,4-C]PYRIDAZIN-3-YLAMINE;FR 180204 (FR180204);FR180204;FR-180204;FR 180204;ERK inhibitor II;ERK Inhibitor II, FR180204;C18H13N7;5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-2H-pyrazolo[3,4-c]pyridazin-3-amine;5-{2-phenylpyrazolo[1,5-a]pyridin-3-yl}-1H-pyrazolo[3,4-c]pyridazin-3-amine;5-{2-phenylpyrazolo[1,5-a]pyridin-3-yl}-2H-pyrazolo[3,4-c]pyridazin-3-amine;MLS0060102;5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine;5-(2-Phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine
Cas No.
865362-74-9
分子式
C18H13N7
分子量
327.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
FR 180204 是一种 ATP 竞争性的选择性 ERK 抑制剂,对 ERK1 和 ERK2 的 Ki 值分别为 0.31 μM 和 0.14 μM。IC50 值分别为0.51 μM 和0.33 μM。
生物活性
FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC 50 s of 0.51 μM (K i =0.31 μM) and 0.33 μM (K i =0.14 μM), respectively.
性状
Solid
IC50 & Target[1][2]
ERK1 0.31 μM (Ki) ERK2 0.14 μM (Ki)
体外研究(In Vitro)
In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM. FR 180204 inhibits spontaneous mesothelioma cell growth. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss in collagen-induced arthritis mice. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves clinical parameters. 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]. Ohori M, et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63.
[2]. Ohori M, et al. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (152.75 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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