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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-ERK-Ravoxertinib
Ravoxertinib

Chemical Structure : Ravoxertinib

CAS No.: 1453848-26-4

Ravoxertinib (GDC-0994, GDC0994)

货号: PC-22330Not For Human Use, Lab Use Only.

Ravoxertinib (GDC-0994) is potent, selective and orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

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10 mg ¥1980 In stock
25 mg ¥3280 In stock
50 mg ¥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ravoxertinib (GDC-0994) is potent, selective and orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
Ravoxertinib (GDC-0994) displays at least 50-fold selectivity against the Invitrogen Selectscreen panel containing 279 kinases.
Ravoxertinib (GDC-0994) potently inhibits ERK dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with IC50 of 12 nM.
Ravoxertinib (GDC-0994) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006).
Ravoxertinib (GDC-0994) (15, 30, or 100 mg/kg, PO, QD) inhibits tumor growth in the HCT116 mouse xenograft model.

物理化学性质&存储条件

分子量 440.86
分子式 C21H18ClFN6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

参考文献

1. Blake JF, et al. J Med Chem. 2016 Jun 23;59(12):5650-60.

2. Varga A, Soria JC, et al. Clin Cancer Res. 2020 Mar 15;26(6):1229-1236.

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