Model NO.: CAS: 443913-73-3 Molecular Formula: C22h24brfn4o2 Storage: Store at -20°c Trademark: gongchuang Origin: Hubei CAS: 443913-73-3 Molecular Weight: 475.35 Targets: Vegfr-1/2/3 Pdgfrβ Ret Specification: GMP, ISO HS Code: 3001200010
|Molecular Formula ||C22H24BrFN4O2 |
|Molecular Weight ||475.35 |
|Storage ||Store at -20°C |
|Targets ||VEGFR-1/2/3 PDGFRβ RET |
|IC50 ||22/4/5.2nM 39nM 35nM |
Vandetanib (INN, trade name Caprelsa) is an anti-cancer drug that is used for the treatment of certain tumours of the thyroid gland.It acts as a kinase inhibitor of a number of cell receptors, mainly the vascular endothelial growth factor receptor (VEGFR), the epidermal growth factor receptor(EGFR), and the RET-tyrosine kinase.The drug was developed by AstraZene
Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay.
Vandetanib also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC50 of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC50 of 2.7 μM (A549) to 13.5 μM (Calu-6). Vandetanib displays an inhibitory effect on the basal ABCG2-ATPase. Parental and ABCG2-expressing A431 cells showed similar sensitivities toward Vandetanib. Exposure to EGFR inhibitors decreases pEGFR levels in A431 cells, with Vandetanib displaying only a moderate effect. Vandetanib displays a slight but measurable effect, whereas gefitinib, pelitinib and neratinib completely inhibit ABCG2-mediated efflux of mitoxantrone from A431/ABCG2 cells, similarly to the specific ABCG2 inhibitor Ko143.Vandetanib inhibits both PC3wt and PC3R cell lines with similar IC50 of 13.3 μM and 11.5 μM, respectively. Vandetanib suppresses phosphorylation of VEGFR2 in HUVEC and EGFR in hepatoma cells and inhibits cell proliferation. Vandetanib causes an accumulation of cells in the G0-G1 phases in GEO and OVCAR-3 cells and increases apoptosis in OVCAR-3, ZR-75-1, MCF-10A ras, and GEO cells. Vandetanib causes a dose-dependent inhibition of EGFR phosphorylation in mouse NIH-EGFR fibroblasts and human MCF-10A ras breast cancer cells, two cell lines that overexpress the human EGFR. Vandetanib treatment results in a dose-dependent inhibition of soft agar growth in seven human cell lines (breast, colon, gastric, and ovarian) with functional EGFR but lacking VEGFR2.
ZD6474 is a dual inhibitor of VEGFR-2 and EGFR with IC50 values of 40 nM and 500 nM, respectively.
ZD6474 showed potent inhibition activities against recombinant VEGFR-2 and EGFR in the in vitro assays. The inhibition of VEGFR-2 was 2.7-fold more potent than that of VEGFR-3 (Flt-4) kinase and 40-fold more potent than that of VEGFR-1. In human umbilical vein endothelial cells, treatment of ZD6474 resulted in significant inhibition of cell proliferation stimulated by VEGF and EGF with IC50 values of 60 and 170 nM, respectively. Through inhibiting the kinase activity of EGFR, ZD6474 can inhibit cell growth of various cancer cell lines, including lung, ovarian, breast and colon cancers. Besides that, ZD6474 administration inhibited tumor growth in a dose-dependent manner in many tumor xenograft models
Other Small molecular API
|E7080 ||417716-92-8 |
|Afatinib diMaleate ||439081-18-2 |
|XL184 S-MALATE ||1140909-48-3 |
|Crizotinib ||877399-52-5 |
|Axitinib ||319460-85-0 |
|WZ4002 ||1213269-23-8 |
|Vandetanib ||443913-73-3 |
|Sunitinib ||557795-19-4 |
|Regorafenib ||755037-03-7 |
|Imatinib ||152459-95-5 |
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