Cell lines

Human 786-O and RCC4 cells, murine Renca 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

10 μM, 24 hours

Applications

Sunitinib induced RCC tumor cell apoptosis in all three tumor cell lines. It also inhibited cell proliferation in a dose-dependent manner. For concentrations at which sunitinib caused effective tumor cell death; there were corresponding increases in cleaved PARP. Sunitinib treatment (24 h) of 786-O, RCC4 and Renca tumor cells reduced expression of several key anti-apoptotic and pro-proliferation genes, including Cyclin E, Cyclin D1 and Survivin.

Animal models

Female BALB/c mice injected with Renca cells

Dosage form

Oral administration, 40, 20, 10 mg/kg body weight, daily

Applications

Sunitinib induced tumor cell apoptosis in vivo as early as 1 day post treatment, which occurred in the presence of apparently intact tumor vessels. There appeared to be more apoptosis in the tumor on days 3 and 11 post treatment, with greater disruption of the tumor vasculature. Sunitinib treatment reduced Stat3 activity and induced tumor cell death as early as one day post treatment.

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.

Sunitinib is an oral, multi-targeted and small-molecule inhibitor of receptor tyrosine kinase (RTK) [1].

Sunitinib is a RTK inhibitor against vascular endothelial growth factor receptors (VEGFR1-3), platelet-derived growth factor receptors (PDGFRα and PDGFRβ ), stem cell factor receptor (c-kit), glial cell-line derived neurotrophic factor receptor(RET). Sunitinib has been reported to inhibit the growth in five NPC cell lines (HK1, CNE-2, HON E-1, CNE-1 and C666-1) with the IC50 values of 2.06 ± 0.29μM, 3.45 ± 0.11μM, 4.07 ± 1.07μM, 2.60 ± 0.38 and 7.57 ± 1.74μM, respectively. Apart from these, Sunitinib has been observed to induce apoptosis in NPC cells as well as induce cell cycle arrest at the G0 /G1 phase in HONE-1 and CNE-2 cells. In vivo, Sunitinib treatment could induce a significant reduction in MVD in CNE2 NPC xenograft [1].

References:
[1]Hui EP1, Lui VW, Wong CS, Ma BB, Lau CP, Cheung CS, Ho K, Cheng SH, Ng MH, Chan AT. Preclinical evaluation of sunitinib as single agent or in combination with chemotherapy in nasopharyngeal carcinoma. Invest New Drugs. 2011 Dec;29(6):1123-31.