Pazopanib

Bezeichnung:Pazopanib

CAS-Nr444731-52-6

Englisch Name:Pazopanib

CBNumberCB91562449

SummenformelC21H23N7O2S

Molgewicht437.52

MOL-Datei444731-52-6.mol

Pazopanib physikalisch-chemischer Eigenschaften

Schmelzpunkt	285-289°C (dec.)
Siedepunkt	728.8±70.0 °C(Predicted)
Dichte	1.40
Flammpunkt	359℃
storage temp.	Refrigerator
Löslichkeit	Aqueous Acid (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Heated)
pka	10.19±0.60(Predicted)
Aggregatzustand	Yellow powder.
Farbe	White to Beige

Sicherheit

R-Sätze:	43-62/63
S-Sätze:	36/37/39-28B
HS Code	29350090
Giftige Stoffe Daten	444731-52-6(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Pazopanib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Pazopanib is a multi-kinase inhibitor that inhibits the VEGF receptors VEGFR1, VEGFR2, and VEGFR3 (IC₅₀s = 10, 30, and 47 nM, respectively, in a cell-free enzyme assay). It also inhibits PDGFRα, PDGFRβ, and c-Kit (IC₅₀s = 71, 84, and 74 nM, respectively, in a cell-free enzyme assay) as well as additional receptor tyrosine kinases. Pazopanib inhibits upregulation of the surface adhesion proteins ICAM-1 and VCAM-1 induced by VEGF in multiple myeloma cells cocultured with human umbilical vein endothelial cells (HUVECs) and decreases multiple myeloma cell adhesion to HUVECs. It also inhibits proliferation of multiple myeloma cells cocultured with HUVECs. Pazopanib (30 and 100 mg/kg) reduces tumor growth, induces apoptosis, decreases angiogenesis, and increases survival in a multiple myeloma mouse xenograft model. Formulations containing pazopanib have been used in the treatment of cancer.
Chemische Eigenschaften
Off-White Solid
Charakteristisch
Class: receptor tyrosine kinase
Treatment: RCC, STS
Oral bioavailability = 14–39%
Elimination half-life = 31 h
Protein binding > 99.9%
Verwenden
Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Verwenden
An oral angiogenesis inhibitor targeting VEGFR and PDGFR.
Verwenden
Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Verwenden
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-α/β, and c-Kit.
Definition
ChEBI: A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.
Clinical Use
Tyrosine kinase inhibitor:
Treatment of metastatic renal cell carcinoma and soft tissue sarcoma
target
VEGFR1
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antibacterials: avoid with clarithromycin, rifampicin and telithromycin.
Antifungals: avoid with itraconazole, ketoconazole and voriconazole.
Antipsychotics: avoid with clozapine (increased risk of agranulocytosis).
Antivirals: avoid with atazanavir, boceprevir, indinavir, ritonavir and saquinavir.
Grapefruit juice: avoid concomitant administration.
Avoid concomitant use with other inhibitors or inducers of CYP3A4. Dose alterations may be required.
Stoffwechsel
Metabolism primarily by CYP3A4, with minor contributions from CYP1A2 and CYP2C8. The four principle pazopanib metabolites account for only 6% of the exposure in plasma. One of these metabolites inhibits the proliferation of VEGF-stimulated human umbilical vein endothelial cells with a similar potency to that of pazopanib, the others are 10- to 20-fold less active.
Therefore, activity of pazopanib is mainly dependent on parent pazopanib exposure.
Elimination is mostly via the faeces.

Pazopanib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

444731-52-6, Pazopanib Verwandte Suche:

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