Cediranib (AZD217) (Synonyms: AZD 2171, ZD 2171) |
رقم الكتالوجGC16421 |
Cediranib (AZD217) (AZD2171) هو مثبط VEGFR tyrosine kinase قوي للغاية ومتوفر عن طريق الفم مع IC50s من <1 ، <3 ، 5 ، 5 ، 36 ، 2 نانومتر لـ Flt1 ، KDR ، Flt4 ، PDGFRα ؛ ، PDGFR7777 ؛ 77#945 كيت ، على التوالي.
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Cas No.: 288383-20-0
Sample solution is provided at 25 µL, 10mM.
Cediranib (also known as AZD2171) is a highly potent KDR tyrosine kinase inhibitor that ATP-competitively inhibits recombinant KDR tyrosine kinase as well as other members of vascular endothelial growth factor receptor (VEGFR) family, including Flt-1 (VEGFR-1) and Flt-4 (VEGFR-3) with the half maximal inhibition concentration IC50 values of <0.001 μmol/L, 0.005 μmol/L and <0.003 μmol/L respectively [1].
Cediranib also potently inhibits a few members of platelet-derived growth factor receptor (PDGFR) family, including c-Kit, PDGFR-β, PDGFR-α, CSF-1R and Flt-3, with IC50 values of 0.002 μmol/L, 0.005 μmol/L, 0.036 μmol/L, 0.11 μmol/L anf > 1 μmol/L respectively due to their similar structure to VEGFR family members [1].
References:
[1] Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO, Chester R, Jackson JA, Boffey SJ, Kilburn LL, Barnett S, Richmond GH, Wadsworth PF, Walker M, Bigley AL, Taylor ST, Cooper L, Beck S, Jürgensmeier JM, Ogilvie DJ. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res. 2005 May 15;65(10):4389-400.
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