| Identification | Back Directory | [Name]
Toceranib Phosphate | [CAS]
874819-74-6 | [Synonyms]
PHA 291639E
SU11654 phosphate
PHA 291639 phosphate
Toceranib (phosphate)
Toceranib phosphate(SU 11654)
Toceranib (PHA 291639) phosphate
(Z)-5-((5-Fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-n-(2-(pyrrolidin-1-yl)ethyl)-1h-pyrrole-3-carboxamide phosphate
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-(2-pyrrolidin-1-ylethyl)-1H-pyrrole-3-carboxamide,phosphoric acid
5-[(Z)-(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(1-pyrrolidinyl)ethyl]-1H-pyrrole-3-carboxamide phosphate
1H-Pyrrole-3-carboxaMide, 5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)Methyl]-2,4-diMethyl-N-[2-(1-pyrrolidinyl)ethyl]-, phosphate (1:1) | [EINECS(EC#)]
639-691-4 | [Molecular Formula]
C22H28FN4O6P | [MDL Number]
MFCD25372034 | [MOL File]
874819-74-6.mol | [Molecular Weight]
494.453 |
| Chemical Properties | Back Directory | [Melting point ]
>270°C (dec.) | [storage temp. ]
-20°C Freezer | [solubility ]
DMSO (Slightly, Heated) | [form ]
Solid | [color ]
Yellow to Dark Orange | [InChIKey]
AOORBROPMMRREB-HBPAQXCTSA-N | [SMILES]
P(O)(O)(O)=O.C(/C1NC(C)=C(C(=O)NCCN2CCCC2)C=1C)=C1/C(NC2=CC=C(F)C=C/12)=O |
| Hazard Information | Back Directory | [Description]
Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. It is a receptor tyrosine kinase inhibitor and is used in the treatment of canine mast cell tumor also called mastocytoma. It may also have an anti-angiogenic effect. | [Uses]
Toceranib Phosphate is a useful compound in the treatment of chemotherapy-induced diarrhea. | [Side effects]
Common side effects of Toceranib Phosphate may include diarrhoea, decreased or lack of appetite, claudication or weight loss. Less common side effects include muscle pain, low white blood cell count, low blood protein levels, blood clots (which may appear as swelling in the legs or difficulty breathing), pancreatitis, loss of nose colour, changes in skin hair, nosebleeds, seizures, high blood pressure and itching. Serious side effects include prolonged loss of appetite, severe diarrhoea or bloody stools, bruising or bleeding. In cats, gastrointestinal effects, low blood counts, liver and kidney problems, and hair loss have been reported. | [in vivo]
Administration of Toceranib phosphate (PHA 291639 phosphate) significantly decreases the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving Toceranib phosphate (PHA 291639 phosphate) and cyclophosphamide (CYC) demonstrate a significant increase in serum concentrations of IFN-γ, which is inversely correlated with Treg numbers after 6 weeks of combination treatment[3]. | [target]
KIT | [IC 50]
PDGFRβ: 5 nM (Ki); Flk-1: 6 nM (Ki) |
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