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.
|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.|
|Incubation time||48 h|
|Animal models||MV4;11 or RS4;11 cells|
|Formulation||citrate-buffered solution (pH 3.5)|
|Dosages||40, 20, 5 and 1 mg/kg/d|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 15 mg/mL|
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.
|Related VEGFR/PDGFR Products|
Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous KIT mutation, D816V in KIT Exon 17 (IC50 = 0.5 nM).
|Nintedanib Ethanesulfonate Salt
BIBF 1120 esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
|Pazopanib HCl (GW786034 )
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
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