Cediranib (maleate)

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 100mg
ArtNr HY-13049-100mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
AZD-2171 maleate
CAS No.
857036-77-2
Purity
>98%
MW
5665775
Formula
C29H31FN4O7
Solubility
DMSO: >= 45 mg/mL
Biological Description
Cediranib (AZD2171) maleate is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/<=3 nM, similar activity against c-Kit and PDGFRbeta, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-alpha, CSF-1R and Flt3.
IC50 value: 0.5 nM (VEGFR2); 5 nM/<=3 nM(Flt1/4) [1]
Target: VEGFR2; Flt1/4
in vitro: Cediranib maleate inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 uM in MG63 cell lines. Cediranib has been shown to block Flt1-associated kinase with IC50 of 5 nM and VEGF-C and VEGF-D receptor Flt-4 with IC50 less than 3 nM. In addition, the IC50 values for inhibition of c-Kit and PDGFRbeta tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 uM Cediranib is assayed with 100 uM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro [1].
in vivo: Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated [1]. Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts [2].
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Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 100mg
Lieferbar: In stock
Listenpreis: 588,93 €
Rabatt: -10,0%
Preis: 530,04 €
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