PLX7904

製品コードS7964 バッチS796401

印刷

化学情報

Chemical Structure Synonyms PB04 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H22F2N6O3S
分子量 512.53 CAS No. 1393465-84-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (195.11 mM)
Water Insoluble
Ethanol 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 PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.
in vitro PLX7940 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Consistent with ERK1/2 re-activation driving the re-acquisition of malignant properties, PLX7904 promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS mediated vemurafenib-resistant cells. PLX7904 is also evaluated in the human SCC cell line A431 and the human breast adenocarcinoma cell line SKBR3 as these cells achieve MAPK pathway activation by upstream signals feeding into RAS (through overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), respectively)[1][2].
in vivo PLX7904 inhibits the COLO205 xenograft growth in eight mice per group[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 WM793, WM115, WM9, WM278, WM1346, WM1366, WM1361A, Sbcl2, 1205Lu, A375, SK-MEL 24, SKMEL-2, and SK-MEL 207 cells
濃度 0, 0.5, 1, 5 μM
反応時間 24 h
実験の流れ

Cells are treated with PB04(PLX7904) at different concentrations (0, 0.05, 0.1, 1, 5 μM) for 24 h. Cells are lysed and analyzed by Western blotting with phospho-MEK1/2, total MEK1/2, phospho-ERK1/2 and total ERK1/2 antibodies.

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：

Oncogenic BRAF induces whole-genome doubling through suppression of cytokinesis [ Nat Commun, 2022, 13(1):4109] PubMed: 35840569
Increased IRF9-STAT2 signaling leads to adaptive resistance toward targeted therapy in melanoma by restraining GSDME-dependent pyroptosis [ J Invest Dermatol, 2022, S0022-202X(22)00096-3] PubMed: 35148998
A Cell-Based MAPK Reporter Assay Reveals Synergistic MAPK Pathway Activity Suppression by MAPK Inhibitor Combination in BRAF-driven Pediatric Low-Grade Glioma Cells [ Mol Cancer Ther, 2020, 25;molcanther.1021.2019] PubMed: 32451331
Analyses of the oncogenic BRAFD594G variant reveal a kinase-independent function of BRAF in activating MAPK signaling. [ J Biol Chem, 2020, 295(8):2407-2420] PubMed: 31929109
Distinct Binding Preferences between Ras and Raf Family Members and the Impact on Oncogenic Ras Signaling. [ Mol Cell, 2019, 76(6):872-884] PubMed: 31606273
Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers [ Cell Rep, 2019, 29(1):118-134] PubMed: 31577942
Identification and characterization of a BRAF fusion oncoprotein with retained autoinhibitory domains. [ Oncogene, 2019, 10.1038/s41388-019-1021-] PubMed: 31558800
Identifying the ErbB/MAPK Signaling Cascade as a Therapeutic Target in Canine Bladder Cancer [ Mol Pharmacol, 2019, 96(1):36-46] PubMed: 31048548
Biochemical Characterization of Full-Length Oncogenic BRAFV600E together with Molecular Dynamics Simulations Provide Insight into the Activation and Inhibition Mechanisms of RAF Kinases. [ Chembiochem, 2019, 10.1002/cbic.201900266] PubMed: 31152574
SOX2‐mediated upregulation of CD24 promotes adaptive resistance toward targeted therapy in melanoma [Hüser L Int J Cancer, 2018, 143(12):3131-3142] PubMed: 29905375

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。