产品说明书
Sorafenib Tosylate
 |
同义名 : | Bay 43-9006 Tosylate;Sorafenib (tosylate);BAY 54-9085;BAY 43-9006 mono-p-tosylate |
| CAS号 : | 475207-59-1 | |
| 货号 : | A117299 | |
| 分子式 : | C28H24ClF3N4O6S | |
| 纯度 : | 98% | |
| 分子量 : | 637.027 | |
| MDL号 : | MFCD08235032 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 30 mg/mL(47.09 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 45 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. Sorafenib Tosylate, the tosylate form of Sorafenib, is a multitargeted inhibitor with IC50 values of 6nM, 22nM and 38nM for Raf-1, wt-BRAF and BRAF-V599E mutant, respectively, as well as less potent to mVEGFR2, mVEGFR3, mPDGFRβ, FLT3, c-Kit, VEGFR2 and FGFR1 with IC50 values of 15nM, 20nM, 57nM, 58nM, 68nM, 90nM and 580nM (measured by kinase assays), respectively. Sorafenib inhibited activation of the RAF/MEK/ERK pathway at concentration below 15μM, performing by suppressing p-Erk, in most of cell lines tested (like MDA-MB-231. Mia PaCa 2, HCT 116 and HT-29) independent of which mutation caused aberrant activation of the RAS/RAF pathway. Sorafenib targeted receptor tyrosine kinases and inhibited autophosphorylation of VEGFR-2 and PDGFR-β induced by VEGF165 (30ng/ml) in HUVECs/ NIH 3T3 cells and PDGF BB (10ng/ml) in HAoSMCs, respectively. Oral treatment with Sorafenib, at dose of 7.5-60mg/kg daily for 9 days, illustrated a spectrum of antitumor efficacy in a representative panel of tumor xenograft models in a dose-dependent manner, including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460 and A549. Sorafenib showed significant tumor angiogenesis activity, performing as daily oral administration of 30 or 60 mg/kg Sorafenib produced 50-80% inhibition of microvessel area and microvessel density compared with vehicle group in HT-29 tumors[1]. | ||
| 作用机制 | Sorafenib is a multitargeted ATP-competitive inhibitor.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| CAKI-1 | Growth Inhibition Assay | 48 h | GI50=3.2 μM | 22560627 | |
| EKVX | Growth Inhibition Assay | 48 h | GI50=2.5 μM | 22560627 | |
| HT-29 | Growth Inhibition Assay | 48 h | GI50=2.5 μM | 22560627 | |
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00126503 | Chromophobe Renal Cell Carcino... 展开 >>ma Clear Cell Renal Cell Carcinoma Papillary Renal Cell Carcinoma Recurrent Renal Cell Carcinoma Sarcomatoid Renal Cell Carcinoma Stage IV Renal Cell Cancer 收起 << | Phase 1 Phase 2 | Completed | - | United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Dana-Farber Harvard Cancer Center Boston, Massachusetts, United States, 02115 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Pennsylvania University of Pennsylvania/Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 收起 << |
| NCT00126503 | - | Completed | - | - | |
| NCT03606590 | Hepatocellular Carcinoma | Phase 2 | Recruiting | December 2020 | Spain ... 展开 >> Vall d'Hebron Institute of Oncology (VHIO) Recruiting Barcelona, Spain Contact: Teresa Macarulla, Dr. +34-932748855 tmacarulla@vhio.net Contact: Raquel García Pelaez +34-934893000 rgarcia@vhio.net Principal Investigator: Teresa Macarulla Mercade, Dr. HM Hospitales - Centro Integral Oncológico Clara Campal Recruiting Madrid, Spain, 28050 Contact: Antonio Cubillo, Dr. acubillo@hmhospitales.com Principal Investigator: acubillo@hmhospitales.com acubillo@hmhospitales.com, Dr. 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.57mL 0.31mL 0.16mL |
7.85mL 1.57mL 0.78mL |
15.70mL 3.14mL 1.57mL |
| 参考文献 |
|---|