| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S81102-5mg |
99.0% | ￥255.00 | 7 | - | - | - |
|
S81102-10mg |
99.0% | ￥425.00 | 6 | - | - | - |
|
S81102-25mg |
99.0% | ￥680.00 | 8 | - | - | - |
|
S81102-50mg |
99.0% | ￥935.00 | 8 | - | - | - |
|
S81102-100mg |
99.0% | ￥1700.00 | 6 | - | - | - |
|
S81102-200mg |
99.0% | ￥2975.00 | 5 | - | - | - |
|
S81102-500mg |
99.0% | ￥4930.00 | 5 | - | - | - |
|
PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
| 产品描述： | PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | B-RafV600E:13 nM (IC50);B-Raf:160 nM (IC50);BRK:130 nM (IC50);FRK:1300 nM (IC50);Csk:1500 nM (IC50);Src:1700 nM (IC50);FAK:1700 nM (IC50);FGFR:1900 nM (IC50);KDR:2300 nM (IC50);HGK:2800 nM (IC50);CSF1R:3300 nM (IC50);Aurora A:3400 nM (IC50);Raf | ||||||||||||||||||||
| 体内研究： | Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-RafV600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-RafV600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation. PLX-4720 treatment at 30 mg/kg/day significant inhibits the tumor growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases | ||||||||||||||||||||
| 参考文献： | 1. Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046. 2. Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71(7), 2750-2760. 3. Nucera C, et al. B-Raf(V600E) and thrombospondin-1 promote thyroid cancer progression. Proc Natl Acad Sci U S A, 2010, 107(23), 10649-10654. 4. Rizzolio S, et al. Neuropilin-1 upregulation elicits adaptive resistance to oncogene-targeted therapies. J Clin Invest. 2018 Aug 31;128(9):3976-3990. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京