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Toceranib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Toceranib图片
CAS NO:356068-94-5
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 396.47
Formula C22H25FN4O2
CAS No.356068-94-5 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1mg/mL
Ethanol: <1mg/mL
Chemical Name (Z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-N-(2-(pyrrolidin-1-yl)ethyl)-1H-pyrrole-3-carboxamide
SynonymsSU-11654; PHA291639; SU 11654; PHA 291639; SU11654; PHA-291639; Toceranib; Trade name: Palladia.
实验参考方法
In Vitro

In vitro activity: Toceranib, also known as PHA-291639 and SU 11654, is an inhibitor of receptor tyrosine kinase (RTK) with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. It is used in the treatment of canine mast cell tumor (also called mastocytoma). Toceranib is an veterinary drug that was approved for use in dog. Toceranib is likely to act mostly through inhibition of the kit tyrosine kinase, though it may also have an anti-angiogenic effect.


Kinase Assay: Toceranib (SU11654) is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including PDGFR and Flk-1/KDR, with Kis of 5 and 6 nM, respectively.


Cell Assay: he BR, C2, and P815 cells were counted and resuspended in 24-well plates at a concentration of 0.5 × 106 cells/well (BR and C2) or 0.25 × 106 cells/well (P815) in complete medium. Cells were left untreated, or SU11652, SU11654, or SU11655 was added to a final concentration of 0.01 to 1 μM. Cells were collected after 24, 48, and 72 hours of culture and were counted to determine the number of cells surviving.

In VivoIn mouse xenograft models, oral administration of SU11654 and related compounds affects the growth of multiple tumor cell lines originating from a variety of tissues, leading to either tumor regression or tumor growth inhibition
Animal model Mouse xenograft models
Formulation & Dosage Oral
References J Vet Intern Med. 2012 Mar-Apr;26(2):355-62; BMC Vet Res. 2014 May 6;10:105.