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Sunitinib Malate

Cat. No. M1826

Sunitinib Malate Structure

Synonym: SU-11248, Sutent

Size Price Availability Quantity
100mg USD 65 In stock
200mg USD 95 In stock
500mg USD 140 In stock
1g USD 200 In stock
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Quality Control
Biological Activity

Sunitinib is a multitargeted tyrosine kinase inhibitor of VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. It also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. The recommended dose of sunitinib is 50mg per day for 4 weeks followed by 2 weeks off-treatment (Schedule 4/2). Sunitinib demonstrated superior efficacy to interferon-α for the first-line treatment of mRCC. Sunitinib doubled progression-free survival compared with interferon-α; furthermore, median OS with sunitinib was greater than 2 years. Sunitinib has a distinct and predictable profile of adverse events, most of which are manageable with standard medical interventions. Evaluating the ability of Sunitinib (Sutent) to inhibit ligand-dependent receptor phosphorylation in cells, the effect of Sunitinib (Sutent) on ligand-dependent proliferation of cells was examined.

Protocol
Cell Experiment
Cell lines MV411 cells (FLT3-ITD) and OC1-AML5 cell lines
Preparation method Cell lines were starved overnight in medium containing 0.1% FBS prior to addition of SU11248 and FL (50 ng/mL; FLT3-WT cells only). Proliferation was measured after 48 hours of culture using the Alamar Blue assay (Alamar Biosciences, Sacramento, CA) in triplicate for each condition, as described by the manufacturer. Trypan blue cell viability assays were performed in parallel and yielded similar results.
Concentrations 0~10 μM
Incubation time 48 h
Animal Experiment
Animal models MV4;11 or RS4;11 cells
Formulation citrate-buffered solution (pH 3.5)
Dosages 40, 20, 5 and 1 mg/kg/d
Administration orally (PO)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 532.56
Formula C22H27FN4O2.C4H6O5
CAS Number 341031-54-7
Purity >99%
Solubility DMSO 15 mg/mL
Storage at -20°C
References

Dynamic changes of live/apoptotic circulating tumour cells as predictive marker of response to Sunitinib in metastatic renal cancer.
Rossi et al. Br J Cancer. 2012 Sep 6. PMID: 22955853.

Polymorphisms in Endothelial Nitric Oxide Synthase (eNOS) and Vascular Endothelial Growth Factor (VEGF) Predict Sunitinib-Induced Hypertension.
Eechoute et al. Clin Pharmacol Ther. 2012 Sep 5. PMID: 22948895.

Sunitinib treatment does not improve blood supply but induces hypoxia in human melanoma xenografts.
Gaustad et al. BMC Cancer. 2012 Sep 4;12(1):388. PMID: 22947392.

SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo.
O'Farrell AM, et al. Blood. 2003 May 1;101(9):3597-605. PMID: 12531805.

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Keywords: Sunitinib Malate, SU-11248, Sutent supplier, VEGFR/PDGFR, inhibitors

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