Ravoxertinib (GDC-0994)

製品コードS7554 バッチS755409

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H18ClFN6O2
分子量 439.85 CAS No. 1453848-26-4
Solubility (25°C)* 体外 DMSO 88 mg/mL (200.06 mM)
Ethanol 88 mg/mL (200.06 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
in vitro

GDC-0994 potently inhibits phospho-p90RSK in tumor cells. [1]
in vivo

GDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. [1]

In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 A375 cells
濃度 0.1 µM
反応時間
実験の流れ

Cells were treated with indicted concentrations of the drug.
動物実験 動物モデル Mice
投薬量 40 µg
投与方法 p.o.

カスタマーフィードバック

Data from [Data independently produced by , , Blood, 2018, 131(18):2047-2059]

Data from [Data independently produced by , , Biochim Biophys Acta, 2015, 1852(12):2671-7]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2017, 486(4):1062-1068]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

DUSP22 Ameliorates Endothelial-to-Mesenchymal Transition in HUVECs through Smad2/3 and MAPK Signaling Pathways [ Cardiovasc Ther, 2024, 2024:5583961] PubMed: 38495810
Transcriptional and chromatin profiling of human blood innate lymphoid cell subsets sheds light on HIV-1 pathogenesis [ EMBO J, 2023, e114153.] PubMed: 37382276
Tetrandrine synergizes with MAPK inhibitors in treating KRAS-mutant pancreatic ductal adenocarcinoma via collaboratively modulating the TRAIL-death receptor axis [ Pharmacol Res, 2023, 197:106955] PubMed: 37820855
High-Throughput Functional Evaluation of MAP2K1 Variants in Cancer [ Mol Cancer Ther, 2023, 22(2):227-239] PubMed: 36442478
ERK1/2-Dependent Phosphorylation of GABAB1(S867/T872), Controlled by CaMKIIβ, Is Required for GABAB Receptor Degradation under Physiological and Pathological Conditions [ Int J Mol Sci, 2023, 24(17)13436] PubMed: 37686242
ERK1/2-Dependent Phosphorylation of GABAB1-S867/T872), Controlled by CaMKIIβ, Is Required for GABAB Receptor Degradation under Physiological and Pathological Conditions [ Int J Mol Sci, 2023, 24(17)13436] PubMed: 37686242
Urinary Eubacterium sp. CAG:581 Promotes Non-Muscle Invasive Bladder Cancer (NMIBC) Development through the ECM1/MMP9 Pathway [ Cancers (Basel), 2023, 15(3)809] PubMed: 36765767
Urinary Eubacterium sp. CAG:581 Promotes Non-Muscle Invasive Bladder Cancer (NMIBC) Development through the ECM1/MMP9 Pathway [ Cancers (Basel), 2023, 15(3)809] PubMed: 36765767
A Chemical Proteomics Approach to Discover Regulators of Innate Immune Signaling [ Viruses, 2023, 15(5)1112] PubMed: 37243198
Synergism of Carbamoylated Erythropoietin and Insulin-like Growth Factor-1 in Immediate Early Gene Expression [ Life (Basel), 2023, 13(9)1826] PubMed: 37763230

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。