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Sorafenib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sorafenib图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议
500mg电议

产品介绍
Sorafenib (Bay 43-9006) 是一种有效的口服活性 Raf 抑制剂,对 Raf-1 和 B-Raf 的 IC50 分别为 6 nM 和 20 nM。 Sorafenib 是一种多激酶抑制剂,对 VEGFR2、VEGFR3、PDGFRβ、FLT3 和 c-Kit 的 IC50 分别为 90 nM、15 nM、20 nM、57 nM 和 58 nM。索拉非尼诱导自噬和细胞凋亡。索拉非尼具有抗肿瘤活性。索拉非尼是一种铁死亡激活剂。

Cell lines

PLC/PRF/5 and HepG2 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

IC50: 6.3 μM for PLC/PRF/5 cells 4.5 μM for HepG2 cells 72 hours

Applications

The effect of sorafenib on cell proliferation was measured by CellTiter-Glo assay. Sorafenib inhibited cell proliferation dose-dependently with an IC50 of 6.3 μmol/L in PLC/PRF/5 and 4.5 μmol/L in HepG2 cells.

Animal models

Female CB17 SCID mice injected with PLC/PRF/5 cells

Dosage form

Oral administration; 10, 30, and 100 mg/kg body weight; once daily for 16 or 21 days

Applications

Sorafenib tosylate produced dose-dependent growth inhibition of s.c. implanted PLC/PRF/5 tumor xenografts in SCID mice. Dose levels of 10 and 30 mg/kg produced significant and dose-dependent TGIs of 49% and 78%, respectively. Sorafenib tosylate produced durable partial tumor regressions in 50% of the mice at the 100 mg/kg dose level.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Sorafenib is an oral multikinase inhibitor with activity against Raf kinase and several receptor tyrosine kinases, including vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), FLT3, Ret, and c-Kit. sorafenib, inhibits tumor growth and disrupts tumor microvasculature through antiproliferative, antiangiogenic, and/or proapoptotic effects. sorafenib blocks Raf kinase signaling, inhibits tumor cell proliferation, and induces apoptosisin vitro. In addition, sorafenib exhibits robust antitumor efficacy.

References

1. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. L Liu, Y Cao, C Chen, X Zhang, A McNabola, D Wilkie Cancer research, 2006

2. Phase II study of sorafenib in patients with advanced hepatocellular carcinoma. GK Abou-Alfa, L Schwartz, S Ricci. Journal of clinical Oncology. 2006