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Ravoxertinib

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Chemical Structure| 1453848-26-4 同义名 : GDC-0994;RG-7842
CAS号 : 1453848-26-4
货号 : A170354
分子式 : C21H18ClFN6O2
纯度 : 99%+
分子量 : 440.858
MDL号 : MFCD28143918
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(79.39 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • ERK2

    ERK2, IC50:0.3 nM

  • ERK1

    ERK1, IC50:1.1 nM
描述 ERK1/2 (extracellular-signal-regulated kinases) is only known substrates of the MEK1/2 as well as the essential node in RAS/RAF/MEK/ERK signaling cascade, which can be activated by catalyzing the phosphorylation on T202/Y204 through MEK1/2. GDC-0994 is a selective inhibitor of ERK1/2 with IC50 value of 6.1nM and 3.1nM (measured by enzyme potency), respectively. Cellular study showed that GDC-0994 could inhibit ERK dependent p-RSK with IC50 value of 12nM in PMA-stimulated HepG2 cells[1]. Distinguished with the other published ERK inhibitors, GDC-0994 did not change the level of p-ERK, suggesting the alternative mechanisms of action with respect to feedback signaling of it[2]. The inhibition of p-RSK in these tumors correlating with potency in vitro and in vivo may be the pharmacodynamics biomarker. Oral administration with GDC-0994 once daily for 21 days caused significant tumor growth inhibition by 49%, 57% and 80% at dose of 30, 60 and 100mg/kg in nude mice bearing HCT116 xenograft tumors[1].
作用机制 Not found
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.34mL

2.27mL

1.13mL

22.68mL

4.54mL

2.27mL
参考文献

[1]Blake JF, Burkard M, 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 Development. J Med Chem. 2016 Jun 23;59(12):5650-60.