Toceranib phosphate (formerly known as PHA291639; SU11654), phosphate salt of Toceranib, is a novel and potent receptor tyrosine kinase (RTK) inhibitor with antineoplastic/anticancer activities. It inhibits Flk-1/KDR and PDGFRβ with Kis of 6 nM and 5 nM, respectively. It is used in the treatment of canine mast cell tumor in dogs as an approved veterinary drug. Toceranib is likely to act mostly through inhibition of the kit tyrosine kinase, though it may also have an anti-angiogenic effect.
理化性质和储存条件
| Molecular Weight (MW) | 494.46 |
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| Formula | C22H28FN4O6P |
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| CAS No. | 874819-74-6 (phosphate); |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 2 mg/mL (4.0 mM) |
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| Water: 2 mg/mL (4.0 mM) |
| 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 phosphate |
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| Synonyms | SU-11654 phosphate; PHA291639 phosphate; SU 11654; PHA-291639 phosphate; SU11654; PHA 291639; Toceranib phosphate; Trade name: Palladia. |
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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. |
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| In Vivo | In 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 |
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| Animal model | Mouse xenograft models |
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| Formulation & Dosage | Oral |
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| References | J Vet Intern Med. 2012 Mar-Apr;26(2):355-62; BMC Vet Res. 2014 May 6;10:105. |
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