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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
PLX4032; RG7204; RO5185426
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
918504-65-1
- 规格:
10 mM * 1 mL/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥567.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥321.0 |
| 规格: | 10 mg | 产品价格: | ¥515.0 |
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Vemurafenib
CAS No. : 918504-65-1
MCE 国际站:Vemurafenib
产品活性:Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的,有效的 B-RAF 选择性抑制剂,能够抑制 RAFV600E 和 c-RAF-1 的活性,IC50 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。
研究领域:MAPK/ERK Pathway | Autophagy
In Vitro: Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.
In Vivo: Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts.
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文献和实验Marker Utility for Combination Therapy
Melanoma is a heterogeneous disease for which monotherapies are likely to fail in the majority of patients due to genomic variations between individuals. Novel treatments, such as vemurafenib and ipilimumab, offer clinical promise
对 1.8 万种基因的 6.5 万种 sg RNA。用这么多的 sgRNA,张锋在肿瘤细胞和多能干细胞中筛选到了影响细胞活性的基因。最最引人注目的是他在黑色素瘤中筛选到了几种全新的 vemurafenib 耐药基因。 等等,这个全新是如何解释?全新就是以前没发现的,而以前是怎么筛的呢?当然是 shRNA 啊。张锋通过对比发现,在同样的细胞株中,用 shRNA 根本无法筛选到这几种“新的”耐药基因! 而这就是 Cas9 的价值!相比于 RNAi,Cas9 可以做到对细胞
肿瘤细胞系而建立的小鼠肿瘤移植模型成为肿瘤研究中常用的小鼠模型,这类移植模型可快速测试潜在肿瘤及转移相关基因,并成为临床前的药物试验主要工具。例如,通过异种移植研究有助于揭示结肠癌(CRC)对药物(如 Vemurafenib) 在小鼠体内的耐受机制,从而实现在临床试验中对 CRC 病人启动了同时针对突变 BRAF(如 V600E)和 EGFR 的靶向联合疗法,表明这类异种移植模型在建立新的联合治疗策略方面的实际意义。异种移植研究也有助于发现特定基因表达特征,研究其介导的器官特异性定位转移的特点
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