產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 20mg 50mg 200mg
CAS	475207-59-1
別名
化學(xué)名	4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide;4-methylbenzenesulfonic acid
分子式	C21H16ClF3N4O3.C7H8O3S
分子量	637.03
溶解度	≥ 31.85mg/mL in DMSO, ≥ 4.15 mg/mL in EtOH with ultrasonic
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Sorafenib tosylate, also named nexavar, is a small-molecule anticancer compound [1]. It is also a novel oral Raf kinase and a vascular endothelial growth factor receptor (VEGFR) inhibitor. It inhibits tumor cell proliferation and tumor angiogenesis [2]. To HepG2 cells (1× 106), the IC50 of sorafenib tosylate is 2.09μg/ml [3].

Raf is a mitogen-stimulated protein kinase that functions as a component of the signaling cascade that leads to the stimulation of mitogen-activated protein kinase [4].

Vascular endothelial growth factor (VEGF) is a highly specific mitogen for vascular endothelial cells [5].

Treatment with nexavar potently inhibited the cell proliferation of MV4-11 cells (FLT3-ITD) in a dose-dependent manner with an IC50 of 0.88 nM. In MV4-11 cells, sorafenib tosylate of a concentration of 100 nM induced 43.6±5.2% of the cells to undergo apoptosis whereas in EOL-1 cells a concentration as low as 10 nM induced 89.29±1.8% of the cells to be apoptotic [6].

Nude rats at the age of 6 weeks injected with 105 MDA-MB-231 cells were involved. After monotherapy with sorafenib tosylate a significant reduction of the osteolytic lesion volume was observed on days 45 and 55 and of the soft tissue component volume on day 55 in comparison to untreated animals (p < 0.05). Compared to controls, treatment with sorafenib tosylate made bone metastases show significantly decreased values of Amplitude A and kep from day 35 to 55 (Amplitude A: p<0.01; kep p<0.01 on days 35 and 55; p<0.05 on day 45) [7].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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