化合物PLX7904 T6949

Product Introduction
Bioactivity


英文名: PLX7904

描述: PLX7904 (PB04) 是一种有效且选择性的悖论破坏剂 RAF 抑制剂，可抑制突变 BRAF 黑色素瘤细胞中 ERK1/2 的激活。在表达突变体 RAS 的细胞中，对 BRAFV600E 的IC50值约为 5 nM。

细胞实验: 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. (Only for Reference)

体外活性: 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].

体内活性: PLX7904在每组八只小鼠中抑制了COLO205异种移植瘤的生长[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 100 mg/mL (195.11 mM)


关键字: Inhibitor | inhibit | PB-04 | Raf kinases | PLX-7904 | PB 04 | Raf | PLX7904 | PLX 7904

相关产品: AD80 | GSK1904529A | Regorafenib | Pelitinib | Sorafenib tosylate | TAK-580 | Pepinh-TRIF TFA | Exarafenib | K-Ras-IN-1 | Kobe2602

相关库: Anti-Prostate Cancer Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Colorectal Cancer Compound Library | Highly Selective Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library

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