产品说明书
Regorafenib
 |
同义名 : | 瑞格非尼 ;BAY 73-4506;Fluoro-Sorafenib;Regorafenib. trade name: Stivarga. |
| CAS号 : | 755037-03-7 | |
| 货号 : | A177150 | |
| 分子式 : | C21H15ClF4N4O3 | |
| 纯度 : | 98% | |
| 分子量 : | 482.82 | |
| MDL号 : | MFCD16038047 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(248.54 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KIT and RET, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| DLD1 | 1-20 μM | Growth Inhibition Assay | 48 h | inhibits cell growth in a dose-dependent manner | 25071018 |
| DLD1 | 1-10 μM | Apoptosis Assay | 48 h | induces cell death in a dose-dependent manner | 25071018 |
| DLD1 | 40 μM | Function Assay | 24 h | induces PUMA protein and cell apoptosis | 24763611 |
| 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 |
| NCT02288078 | Rectal Cancer | Phase 2 | Unknown | September 2016 | Japan ... 展开 >> Saiseikai Fukuoka General Hospital Recruiting Fukuoka, Japan, 810-0001 Contact: Yasunori Emi, MD, PhD +81-92-771-8151 emi-y@saiseikai-hp.chuo.fukuoka.jp 收起 << |
| NCT03347292 | Carcinoma, Hepatocellular | Phase 1 | Recruiting | February 17, 2021 | United States, California ... 展开 >> USC Norris Hospital and Clinics Recruiting Los Angeles, California, United States, 90033 United States, Florida H. Lee Moffitt Cancer Center & Research Institute Recruiting Tampa, Florida, United States, 33612 United States, New York Mount Sinai Medical Center Recruiting New York, New York, United States, 10029 United States, Washington Seattle Cancer Care Alliance Recruiting Seattle, Washington, United States, 98109-1023 Germany Universitätsklinikum Köln Not yet recruiting Köln, Nordrhein-Westfalen, Germany, 50937 Universitätsmedizin der Johannes Gutenberg Universität Mainz Not yet recruiting Mainz, Rheinland-Pfalz, Germany, 55131 收起 << |
| NCT01187615 | Small Cell Lung Carcinoma | Phase 1 | Terminated | - | United States, Connecticut ... 展开 >> New Haven, Connecticut, United States, 06519 United States, Nevada Las Vegas, Nevada, United States, 89135-3011 United States, New York New York, New York, United States, 10065 United States, North Carolina Chapel Hill, North Carolina, United States, 27599 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.07mL 0.41mL 0.21mL |
10.36mL 2.07mL 1.04mL |
20.71mL 4.14mL 2.07mL |
