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GDC-0994 98%

GDC-0994

源葉(MedMol)
S80364
1453848-26-4
C21H18ClFN6O2
440.858
品牌 貨號 產品規格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數量
源葉(MedMol) S80364-5mg 98% ￥420.00元 4 - - -
源葉(MedMol) S80364-10mg 98% ￥630.00元 預計交期：2-3天 - - -
源葉(MedMol) S80364-25mg 98% ￥1260.00元 1 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively
產品描述： Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively
靶點： ERK1:6.1 nM (IC50);ERK2:3.1 nM (IC50);p-RSK:12 nM (IC50);ERK
體外研究：
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)
體內研究：
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
參考文獻：
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 Developmement. J Med Chem. 2016 Jun 23;59(12):5650 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. 3. MICHAEL LAI. Opportunity for Pharmaceutical Intervention in Lung Cancer: Selective Inhibition of JAK1/2 to Eliminate EMT-Derived Mesenchymal Cells.
溶解性： soluble  in  DMSO
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 2.268 ml 11.342 ml 22.683 ml
5 mM 0.454 ml 2.268 ml 4.537 ml
10 mM 0.227 ml 1.134 ml 2.268 ml
50 mM 0.045 ml 0.227 ml 0.454 ml
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參考文獻

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摩爾濃度計算器

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