Sunitinib Inhibitor CAS No. 557795-19-4

Cat. No.	Name	Size	Price
KI0234	Sunitinib	50 mg	$235.2
	Sunitinib	100 mg	$352
	Sunitinib	500 mg	$432

Chemical Characteristic

Product Name	Sunitinib
Synonyms	Sutent, SU-11248
CAS No.	557795-19-4
Molecular Weight	398.474
Formula	C₂₂H₂₇FN₄O₂
Chemical Name	N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
Smiles	[nH]1c(c(c(c1/C=C/1\C(=O)Nc2c1cc(cc2)F)C)C(=O)NCCN(CC)CC)C
Chemical Structure
Documents	HPLC MS COA

Biological activities

Sunitinib is a multitargeted kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR) -1, 2 and 3, platelet-derived growth factor receptors (PDGFR)-α and β, Flt3 (Fms-like tyrosyl kinase-3), Ret, and Kit. ^[1] Sunitinib inhibits VEGFR2 and PDGFRβ with IC50 of 80 and 2 nM, respectively. ^[2] SU11248 exhibits competitive inhibition against Flk-1 and PDGFRβ with K_{i values of 9 and 8 nM, respectively.^[3] Sunitinib inhibits PDGFR, VEGFR, and FLT3 with IC50 of 5??0 nM. Treatment of the KIT-expressing SCLC-derived NCI-H526 cell line in vitro with sunitinib results in dose-dependent inhibition of stem cell factor-stimulated KIT phosphotyrosine levels and proliferation. ^[4] Sunitinib inhibits FLT3-WT(wild type) phosphorylation in a dose-dependent manner with an IC50 of approximately 250 nM. SU11248 inhibits FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM. Sunitinib dramatically inhibits cellular proliferation of the FLT3-ITD cell line MV4;11 in a dose-dependent manner with an IC50 of 1 to 10 nM. ^[5] Sunitinib inhibits 5637 and TCC-SUP cells with an IC50 of 5.3 µg/mL(9.9 µM) and 4 µg/mL(7.5 µM), respectively.^[1] Sunitinib inhibits endothelial cell proliferation and motility at the same concentrations by suppressing VEGFR-2 signaling. ^[6] Sunitinib-treated tumors displays significantly reduced ki-67 expression compared with control untreated tumors. ^[1] Treatment of NCI-H526 tumors with SU11248 alone results in a NCI-H526 SCLC tumor growth delay. ^[4] SU11248 (20 mg/kg/d) dramatically regresses FLT3-ITD tumors in the subcutaneous tumor xenograft model and prolongs survival in the bone marrow engraftment model. With 5, 10, and 20 mg/kg/d of orally administered SU11248, the mean survival time is significantly prolonged to 46, 56, and at least 83 days, respectively. ^[5] Sunitinib inhibits the growth of clear cell renal cell carcinoma (ccRCC) xenograft tumors and decreases tumor microvessel density as soon as 12 hours after treatment. ^[6] SU11248 selectively inhibits Flk-1/KDR (VEGF receptor 2) and PDGF receptor β phosphorylation (in a time- and dose-dependent manner) when plasma concentrations of inhibitor reached or exceeded 50??00 ng/mL.^[7]}

Protocols

Sunitinib malate is dissolved in distilled water . ^[1]

References

[1] Sonpavde G, et al. Sunitinib malate is active against human urothelial carcinoma and enhances the activity of cisplatin in a preclinical model. Urol Oncol. 2009, 27(4): 391-399. [2] Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003, 46(7): 1116-1119. [3] Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003, 9(1): 327-337. [4] Abrams TJ, et al. SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003, 2(5): 471-478. [5] O'Farrell AM, et al. Blood. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. 2003, 101(9): 3597-3605. [6] Huang D, et al. Sunitinib acts primarily on tumor endothelium rather than tumor cells to inhibit the growth of renal cell carcinoma. Cancer Res. 2010, 70(3): 1053-1062. [7] Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003, 9(1): 327-337.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services