|Company Name:||J & K SCIENTIFIC LTD. |
|Product Name:||Sunitinib Malate|
|Synonyms:||SUNITINIB MALATE;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 (2S)-hydroxybutanedioate;N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide(2S)-2-hydroxybutanedioatesalt;Sunitinib Malate(Sutent);Butanedioic acid, 2-hydroxy-, (2S)-, coMpd. with 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 (1:1);N-(2-(DiethylaMino)ethyl)-5-((Z)-(5-fluoro-1,2-dih;Butanedioic acid, 2-hydroxy-, (2S)-, coMpd. with 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;(Z)-N-(2-(diethylaMino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)Methyl)-2,4-diMethyl-1H-pyrrole-3-carboxaMide (S)-2-hydroxysuccinate|
|Product Categories:||APIs;Heterocycles;Intermediates & Fine Chemicals;Pfizer compounds;Pharmaceuticals;Tyrosine Kinase Inhibitors;SU-11248;Inhibitors;Oxetanes|
|Sunitinib Malate Chemical Properties|
|Sunitinib Malate Usage And Synthesis|
|Anticancer drug||Sunitinib malate is a kind of novel oral multi-targeted anticancer drugs and belongs to multi-targeted tyrosine kinase inhibitor with its trade name being “suntent”. It was successfully developed by Pfizer Company and has dual anti-tumor effect. Moreover, it is the only therapeutic drug which can go beyond the 2-year survival period of advanced kidney cancer and plays a central role in the field of carcinoma and gastrointestinal stromal tumor therapeutic areas. It entered into market in February 2006 in the United States. This drug was the first anti-cancer drug which was approved by the US FDA and can simultaneously treat two diseases. |
Sunitinib exerts its therapeutic role through preventing the tumor cells from getting the blood and nutrients needed for growth. Clinical trials have showed that the drug can delay the growth rate of gastrointestinal stromal tumors, and can shrink the size of renal cell tumors. Sunitinib malate is the first novel targeted drug being capable of selectively targets drugs for a variety of new tyrosine kinase receptors. It combine two kinds of anti-tumor mechanisms including both stopping the formation of anti-angiogenic which is responsible for supplying blood to tumor and direct attack of tumor cells. It represents the advent of a new round of targeted therapies, being able to attack the tumor directly without the toxicity of the conventional chemotherapy.
The indications of Sunitinib malate are as follows:
1, Patients who failed in the treatment with matinib mesylate or of intolerant gastrointestinal stromal tumors (GIST).
2, inoperable advanced renal cell carcinoma (RCC).
3, advanced pancreatic endocrine tumors.
The above information is edited by the Chemicalbook of Dai Xiongfeng.
|Chemical Properties||Yellow Solid|
|Usage||Sunitinib Malate (Sutent, SU11248) 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.|
|Usage||Sunitinib Malate 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|
|Usage||A multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). Antineoplastic.|
|Biological Activity||Potent, ATP-competitive VEGFR, PDGFR β and KIT inhibitor (K i values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFR β and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.|
|Sunitinib Malate Preparation Products And Raw materials|