| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R408239-1ml |
1ml |
现货  |
|
| 英文别名 | Fluoro-Sorafenib, Resihance, Stivarga | 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Regorafenib (BAY 73-4506) |
| 生化机理 | 瑞戈非尼（BAY 73-4506，Fluoro-Sorafenib，Resihance，Stivarga）是一种针对（xa0VEGFR1）的多靶点抑制剂、\xa0VEGFR2，\xa0VEGFR3，\xa0PDGFRβ，\xa0Kit（c-Kit），\xa0RET（c-RET）\xa0and\xa0Raf-1/xa0with\xa0IC50\xa0 of 13 nM/4.2 nM/46 nM、22 nM、7 nM、1.5 nM 和 2.5 nM。Regorafenib induces\xa0autophagy. |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 神经生长因子受体 Trk-A |
| 产品介绍 |
Regorafenib (BAY 73-4506)是多靶点抑制剂，对VEGFR1，VEGFR2，VEGFR3，PDGFRβ，Kit，RET和Raf-1的IC50分别为13 nM，4.2 nM，46 nM Information Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respec 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 KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-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. In vivo Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung. cell lines： Concentrations：5 nM-10 μM Incubation Time：96 hours Powder Purity:≥97% |
| ALogP | 4.2 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F |
| PubChem CID | 11167602 |
| 分子量 | 482.82 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 49 mg/mL (196.51 mM); Ethanol: 11 mg/mL (44.11 mM); Water: Insoluble; |
|---|---|
| 熔点 | 208 °C |
| 象形图 | GHS08, GHS09, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H302: 吞食有害 H400: 对水生生物有剧毒 H410: 对水生生物有剧毒并具有长期持续影响 H372: 通过长时间或反复暴露对器官造成损害 H360: 可能损害生育力或未出生的孩子 H362: 可能对母乳喂养的孩子造成伤害 |
| 预防措施声明 |
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P330: 漱口 P263: 避免在怀孕期间/哺乳期间接触。 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。 |
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