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Sunitinib

Catalog No. T0374L   CAS 557795-19-4
Synonyms: SU 11248

Sunitinib (SU 11248), a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.

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Sunitinib Chemical Structure
Sunitinib, CAS 557795-19-4
Pack Size Availability Price/USD Quantity
100 mg In stock $ 53.00
200 mg In stock $ 81.00
500 mg In stock $ 96.00
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Purity: 99.67%
Purity: 98.62%
Purity: 98.38%
Purity: 98.22%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sunitinib (SU 11248), a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
Targets&IC50 PDGFRβ:2 nM, VEGFR2:80 nM
Kinase Assay Biochemical Tyrosine Kinase Assays: IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST.The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
Cell Research Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3. (Only for Reference)
Synonyms SU 11248
Molecular Weight 398.47
Formula C22H27FN4O2
CAS No. 557795-19-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (62.74 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Sun L, et al. J Med Chem, 2003, 46(7), 1116-1119. 2. Mendel DB, et al. Clin Cancer Res, 2003, 9(1), 327-337. 3. O'Farrell AM, et al. Blood, 2003, 101(9), 3597-3605. 4. Abrams TJ, et al. Mol Cancer Ther, 2003, 2(10), 1011-1021. 5. Yee KW, et al. Blood, 2004, 104(13), 4202-4209.

TargetMolCitations

1. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22. 2. Oeller M, Jaksch-Bogensperger H, Templin M, et al.Transcription Factors STAT3 and MYC Are Key Players of Human Platelet Lysate-Induced Cell Proliferation.International Journal of Molecular Sciences.2022, 23(24): 15782. 3. Xue K H, Jiang Y F, Bai J Y, et al.Melatonin suppresses Akt/mTOR/S6K activity, induces cell apoptosis, and synergistically inhibits cell growth with sunitinib in renal carcinoma cells via reversing Warburg effect.Redox Report.2023, 28(1): 2251234. 4. Liu T, Yue X, Chen X, et al.Nilotinib in combination with sunitinib renders MCL-1 for degradation and activates autophagy that overcomes sunitinib resistance in renal cell carcinoma.Cellular Oncology.2024: 1-18.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Cuproptosis Compound Library Endoplasmic Reticulum Stress Compound Library Orally Active Compound Library Apoptosis Compound Library Cell Cycle Compound Library

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Keywords

Sunitinib 557795-19-4 Angiogenesis Apoptosis Autophagy Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors FLT Mitophagy VEGFR IRE1 PDGFR c-Kit Inositol requiring enzyme 1 Platelet-derived growth factor receptor Vascular endothelial growth factor receptor inhibit Inhibitor SU11248 SU-11248 SU 11248 Mitochondrial Autophagy inhibitor

 

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