Ravoxertinib (Synonyms: GDC-0994)
目录号: PL04562 纯度: ≥99%
CAS No. :1453848-26-4
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中文名称
Ravoxertinib
中文别名
1-[(1S)-1-(4-氯-3-氟苯基)-2-羟基乙基]-4-[2-[(1-甲基-1H-吡唑-5-基)氨基]-4-嘧啶基]-2(1H)-吡啶酮;GDC-0994 抑制剂;GDC-0994
英文名称
Ravoxertinib
英文别名
GDC-0994;(S)-1-(1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one;GDC0994;Ravoxertinib;R6AXV96CRH;1-[(1~{s})-1-(4-Chloranyl-3-Fluoranyl-Phenyl)-2-Oxidanyl-Ethyl]-4-[2-[(2-Methylpyrazol-3-Yl)amino]pyrimidin-4-Yl]pyridin-2-One;6QB;1-[(1S)-1-(4-CHLORO-3-FLUOROPHENYL)-2-HYDROXYETHYL]-4-{2-[(2-METHYLPYRAZOL-3-YL)AMINO]PYRIMIDIN-4-YL}PYRIDIN-2-ONE;1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-
Cas No.
1453848-26-4
分子式
C21H18ClFN6O2
分子量
440.86
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Ravoxertinib (GDC-0994) 是具有口服活性的 ERK 激酶抑制剂,抑制 ERK1 和 ERK2 的IC50 分别为6.1 nM 和 3.1 nM。
生物活性
Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC 50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
性状
Solid
IC50 & Target[1][2]
ERK1 6.1 nM (IC50) ERK2 3.1 nM (IC50
体外研究(In Vitro)
Ravoxertinib (GDC-0994) also inhibits p90RSK with an IC50 of 12 nM.
Ravoxertinib (GDC-0994) is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively.
Ravoxertinib (GDC0994; 50 nM, 0.5 μM, and 5 μM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib (GDC-0994) is sufficient to achieve the desired target coverage for at least 8 h. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. 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
ClinicalTrial
参考文献
[1]. Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developme
[2]. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.
溶解度数据
In Vitro: DMSO : ≥ 35 mg/mL (79.39 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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