Dabrafenib

製品コードS2807 バッチS280711

印刷

化学情報

Chemical Structure Synonyms GSK2118436, GSK2118436A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H20F3N5O2S2
分子量 519.56 CAS No. 1195765-45-7
Solubility (25°C)* 体外 DMSO 100 mg/mL (192.47 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 ダブラフェニブ (Dabrafenib (GSK2118436、GSK2118436A)) は変異型 BRAFV600E 特異的阻害剤 (無細胞アッセイで IC50 = 0.7 nM) であり、B-Raf(wt), c-Raf(wt) に対する効力は変異型に比べそれぞれ 7/9 倍低くなっています。
in vitro

Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-RafV600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-RafV600E. [1]
in vivo

Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. [1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 A375PF11 cells
濃度 > 10 uM
反応時間 24 h
実験の流れ

Cells were treated with different concentrations of drug for 24 h.
動物実験 動物モデル Male C57Bl/6J mice
投薬量 3 mg/kg
投与方法 Osmotic pumps

カスタマーフィードバック

Data from [Data independently produced by J Clin Invest, 2014, 124(11), 5074-84]

Data from [Data independently produced by J Clin Invest, 2014, 24(3), 1406-17]

Data from [Cell Death Dis, 2014, 5, e1278]

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：

MET receptor serves as a promising target in melanoma brain metastases [ Acta Neuropathol, 2024, 147(1):44] PubMed: 38386085
Dual targeting of MAPK and PI3K pathways unlocks redifferentiation of Braf-mutated thyroid cancer organoids [ Oncogene, 2024, 43(3):155-170] PubMed: 37985676
Antagonism of regulatory ISGs enhances the anti-melanoma efficacy of STING agonists [ Front Immunol, 2024, 15:1334769] PubMed: 38312842
H3K4me3 remodeling induced acquired resistance through O-GlcNAc transferase [ Drug Resist Updat, 2023, 71:100993] PubMed: 37639774
A reversible SRC-relayed COX2 inflammatory program drives resistance to BRAF and EGFR inhibition in BRAFV600E colorectal tumors [ Nat Cancer, 2023, 4(2):240-256] PubMed: 36759733
Interleukin 17 signaling supports clinical benefit of dual CTLA-4 and PD-1 checkpoint inhibition in melanoma [ Nat Cancer, 2023, 4(9):1292-1308] PubMed: 37525015
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, 4(10):101200] PubMed: 37734378
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, S2666-3791(23)00367-1] PubMed: 37734378
MiR126-targeted-nanoparticles combined with PI3K/AKT inhibitor as a new strategy to overcome melanoma resistance [ Mol Ther, 2023, 10.1016/j.ymthe.2023.11.021] PubMed: 37990493
An in vivo avian model of human melanoma to perform rapid and robust preclinical studies [ EMBO Mol Med, 2023, 15(3):e16629] PubMed: 36692026

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。