產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 100mg 500mg 1g 2g
CAS	341031-54-7
別名	SU 11248,SU11248,SU-11248,Sunitinib
化學(xué)名	N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide;(2S)-2-hydroxybutanedioic acid
分子式	C22H27FN4O2.C4H6O5
分子量	532.56
溶解度	≥ 26.65mg/mL in DMSO, ≥ 4.6 mg/mL in H2O with ultrasonic
儲(chǔ)存條件	Store at 4°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：

Sunitinib malate, also called sunitinib, is a novel, oral, multi-targeted , small molecule oxindole tyrosine kinase inhibitor which inhibits multiple receptor tyrosine kinases including platelet-derived growth factor receptor ( and (, vascular endothelial growth factor receptor 1, 2 and 3, c-KIT, FLT3 kinase, colony-stimulating factor 1 receptor and RET kinase [2][3] [4]. The IC50 of sunitinib is approximately 10-20 ng/ml to NB cell lines, which is within the clinically relevant human trough serum concentration (50-100 ng/ml) [1].

Receptor tyrosine kinases activated a number of different intracellular signaling pathways [5].

In neuroblastoma (NB) cell lines, SKN-BE (2), NUB-7, SH-SY5Y and LAN-5, sunitinib significantly inhibited cell proliferation after a treatment for 48 hours, in a concentration-dependent manner [1].

Treatment with 20, 30 or 40 mg/kg of sunitinib made NOD/SCID mice inoculated with xenograft tumor cells show significant reduction (P <0.05) in primary tumor growth (%T/C: 49% for SK-N-BE (2) and 55% for NB12 tumor, T/C: average treated tumor mass/average control tumor mass). Treatment with different doses of sunitinib (20, 30 or 40 mg/kg) for 14 days resulted in a dramatic decrease in the numbers and size of metastatic sites and a significant difference in liver weight in mice injected intravaneously with 106 SK-N-BE(2) cells for 7 days compared with the control group [1].

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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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