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Sunitinib

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Sunitinib Basic information

Product Name:
Sunitinib
Synonyms:
  • Sunitinib--- free base
  • Sunitinib,Sutent
  • 5-(5-Fluoro-2-oxo-1,2-dihydroindol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid N-(2-diethylaminoethyl)amide
  • Suniti
  • N-[2-(diethylaMino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]Methyl}-2,4-diMethyl-1H-pyrrole-3-carboxaMide
  • SUTENT SUNITINIB
  • N-(2-diethylaminoethyl)-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)meth yl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
  • Sunitinib malate(TINIBS)
CAS:
557795-19-4
MF:
C22H27FN4O2
MW:
398.47
Product Categories:
  • SU-11248
  • Inhibitors
  • anti-neoplastic
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Active Pharmaceutical Ingredients
  • Sunitinib
  • Molecular Targeted Antineoplastic
  • Heterocyclic Compounds
  • Tyrosine Kinase Inhibitors
  • Pharmaceutical intermediate
  • API
  • Isotope Labelled Compounds
Mol File:
557795-19-4.mol
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Sunitinib Chemical Properties

Melting point:
189-191°C
Boiling point:
572.1±50.0 °C(Predicted)
Density 
1.2
Flash point:
299.8℃
storage temp. 
2-8°C
solubility 
Chloroform (Slightly), Methanol (Slightly)
pka
8.5(at 25℃)
form 
Solid
color 
Yellow to Dark Orange
CAS DataBase Reference
557795-19-4(CAS DataBase Reference)
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Safety Information

Safety Statements 
24/25
HS Code 
29337900
Hazardous Substances Data
557795-19-4(Hazardous Substances Data)
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Sunitinib Usage And Synthesis

Description

Sunitinib is an inhibitor of multiple receptor tyrosine kinases (RTKs) involved in tumor proliferation and angiogenesis, including platelet-derived growth factor receptors (PDGFR), vascular endothelial growth factor receptors (VEGFR), and stem cell factor receptor (KIT). It was launched as an oral treatment for gastrointestinal stromal tumors (GIST) and advanced renal-cell carcinoma (RCC). In vitro, sunitib inhibits VEGFR2, PDGFRα, PDGFRβ, KIT, and FLT3 receptors with IC50 values in the 4–14nM range, and the ligand-dependent autophosphorylation of VEGFR2 and PDGFRb with IC50s of approximately 10 nM. In addition, it inhibits the growth of tumor cells expressing dysregulated target RTKs in vitro and inhibits PDGFRb- and VEGFR2-dependent tumor angiogenesis in vivo. Sunitinib exhibits broad and potent antitumor activity, causing regression in murine models of human epidermal (A431), colon (Colo205 and HT-29), lung (NCI-H226 and H460), breast (MDA-MB-435), prostate (PC3-3M-luc), and renal (786-O) cancers, and suppressing or delaying the growth of many others, including the C6 rat and SF763 T human glioma xenografts and B16 melanoma lung cancer.

Chemical Properties

Yellow Solid

Originator

Sugen (US)

Uses

A multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). Antineoplastic

Uses

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.

Uses

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.

Uses

Labelled Sunitinib (S820000), a multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK).

Uses

Labelled Sunitinib, a multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK).

brand name

(Pfizer).

Clinical Use

Tyrosine kinase inhibitor:
Treatment of metastatic renal cell carcinoma (MRCC), gastrointestinal stromal tumours (GIST) and pancreatic neuroendocrine tumours (pNET)

Drug interactions

Potentially hazardous interactions with other drugs
Antipsychotics: avoid with clozapine (increased risk of agranulocytosis).
Antivirals: avoid concomitant use with boceprevir.
Avoid concomitant use with other inhibitors or inducers of CYP3A4. Dose alterations may be required.

Metabolism

Metabolised mainly via the cytochrome P450 isoenzyme CYP3A4 to its primary active metabolite, which itself is then further metabolised via CYP3A4.
Elimination is primarily via faeces. In a human mass balance study of [14C]sunitinib, 61% of the dose was eliminated in faeces and 16% by the renal route.

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