Sunitinib

Bezeichnung:Sunitinib

CAS-Nr557795-19-4

Englisch Name:Sunitinib

CBNumberCB9728174

SummenformelC22H27FN4O2

Molgewicht398.47

MOL-Datei557795-19-4.mol

Sunitinib physikalisch-chemischer Eigenschaften

Schmelzpunkt	189-191°C
Siedepunkt	572.1±50.0 °C(Predicted)
Dichte	1.2
Flammpunkt	299.8℃
storage temp.	2-8°C
Löslichkeit	Chloroform (Slightly), Methanol (Slightly)
pka	8.5(at 25℃)
Aggregatzustand	Solid
Farbe	Yellow to Dark Orange
CAS Datenbank	557795-19-4(CAS DataBase Reference)

Sicherheit

S-Sätze:	24/25
HS Code	29337900
Giftige Stoffe Daten	557795-19-4(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Sunitinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Yellow Solid
Originator
Sugen (US)
Verwenden
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.
Verwenden
Labelled Sunitinib (S820000), a multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK).
Definition
ChEBI: Sunitinib is a member of pyrroles and a monocarboxylic acid amide. It has a role as an angiogenesis inhibitor, an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, a vascular endothelial growth factor receptor antagonist, an immunomodulator and a neuroprotective agent. It is functionally related to a 3-methyleneoxindole.
Trademarks
(Pfizer).
Charakteristisch
Class: receptor tyrosine kinase
Treatment: RCC, GIST
Elimination half-life = 70 h
Protein binding = 95%
Clinical Use
Tyrosine kinase inhibitor:
Treatment of metastatic renal cell carcinoma (MRCC), gastrointestinal stromal tumours (GIST) and pancreatic neuroendocrine tumours (pNET)
target
VEGFR-1
Arzneimittelwechselwirkung
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.
Stoffwechsel
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.
Einzelnachweise
[1]hui ep1, lui vw, wong cs, ma bb, lau cp, cheung cs, ho k, cheng sh, ng mh, chan at. preclinical evaluation of sunitinib as single agent or in combination with chemotherapy in nasopharyngeal carcinoma. invest new drugs. 2011 dec;29(6):1123-31.

Sunitinib Upstream-Materialien And Downstream Produkte

Sunitinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

557795-19-4, Sunitinib Verwandte Suche:

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