受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
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. |
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]. |
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. |
|
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。