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Sunitinib

Catalog No.GC17651

RTK inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

Sunitinib Chemical Structure

Cas No.: 557795-19-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$40.00
In stock
100mg
$36.00
In stock
500mg
$71.00
In stock
1g
$113.00
In stock
2g
$155.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment: [1]

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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C 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 experiment: [1]

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.

References:

[1] Xin H, Zhang C, Herrmann A, et al. Sunitinib inhibition of Stat3 induces renal cell carcinoma tumor cell apoptosis and reduces immunosuppressive cells. Cancer research, 2009, 69(6): 2506-2513.

Background

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.

Chemical Properties

Cas No. 557795-19-4 SDF
Chemical Name N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
Canonical SMILES CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C
Formula C22H27FN4O2 M.Wt 398.47
Solubility ≥ 19.9mg/mL in DMSO with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.5096 mL 12.548 mL 25.096 mL
5 mM 0.5019 mL 2.5096 mL 5.0192 mL
10 mM 0.251 mL 1.2548 mL 2.5096 mL
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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