Ravoxertinib (GDC-0994)

製品コードS7554 バッチS755410

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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	Ravoxertinib (GDC-0994) potently inhibits phospho-p90RSK in tumor cells. ^[1]
in vivo	Ravoxertinib (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, and it inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, subsequently preventing ERK-dependent tumor cell proliferation and survival. ^[1,2]

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 Ravoxertinib (GDC-0994).
動物実験	動物モデル	Mice
	投薬量	40 µg
	投与方法	p.o.

参考

http://www.abstractsonline.com/Plan/ViewAbstract.aspx?mID=3404&sKey=1eb84585-6831-405d-88b2-cef74aaf004e&cKey=22cc177f-4718-4f12-bdf6-a275db718f29&mKey=6ffe1446-a164-476a-92e7-c26446874d93
https://pubmed.ncbi.nlm.nih.gov/27227380/
https://pubmed.ncbi.nlm.nih.gov/35764642/

https://pubmed.ncbi.nlm.nih.gov/36073544/

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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：

Transcriptional repressor Capicua is a gatekeeper of cell-intrinsic interferon responses [ Cell Host Microbe, 2025, 33(4):512-528.e7]	PubMed: 40132591
Combined MEK and PARP inhibition enhances radiation response in rectal cancer [ Cell Rep Med, 2025, 6(8):102284]	PubMed: 40782795
Reciprocal regulation of MMP-28 and EGFR is required for sustaining proliferative signaling in PDAC [ J Exp Clin Cancer Res, 2025, 44(1):68]	PubMed: 39994761
CD22 modulation alleviates amyloid β-induced neuroinflammation [ J Neuroinflammation, 2025, 22(1):32]	PubMed: 39910617
Identification of chemical inhibitors targeting long noncoding RNA through gene signature-based high throughput screening [ Int J Biol Macromol, 2025, 292:139119]	PubMed: 39722392
Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936]	PubMed: 38588697
Targeting ERK-MYD88 interaction leads to ERK dysregulation and immunogenic cancer cell death [ Nat Commun, 2024, 15(1):7037]	PubMed: 39147750
Myeloid cells coordinately induce glioma cell-intrinsic and cell-extrinsic pathways for chemoresistance via GP130 signaling [ Cell Rep Med, 2024, S2666-3791(24)00372-0]	PubMed: 39053460
Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2 [ Elife, 2024, 12RP91507]	PubMed: 38537148
The ERK inhibitor GDC-0994 selectively inhibits growth of BRAF mutant cancer cells [ Transl Oncol, 2024, 45:101991]	PubMed: 38728872

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。