| 产品描述: | Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively |
| 靶点: |
VEGFR1:13 nM (IC50);VEGFR2:4.2 nM (IC50);VEGFR3:46 nM (IC50);PDGFRβ:22 nM (IC50);Braf:28 nM (IC50);BRafV600E:19 nM (IC50);Raf-1:2.5 nM (IC50);Raf;VEGFR;c-RET;PDGFR;Autophagy |
| 体内研究: |
Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached |
| 参考文献: |
1. Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255. 2. Heng DY, et al. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol, 2010, 2(1), 39-49. 3. Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
RT |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.926 ml |
9.629 ml |
19.258 ml |
| 5 mM |
0.385 ml |
1.926 ml |
3.852 ml |
| 10 mM |
0.193 ml |
0.963 ml |
1.926 ml |
| 50 mM |
0.039 ml |
0.193 ml |
0.385 ml |
|
| 注意: |
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