All AbMole products are for research use only, cannot be used for human consumption.
Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase (IC50=40 nM). Vandetanib also inhibited VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM). Vandetanib had little effect on PDGFRβ, FLT-1, TIE-2 and FGFR1. IC50 was 1.1-3.6 μM, and had little effect on MEK, CDK2, C-kit, erbB2, FAK, PDK1, Akt and IGF-1R, with IC50 > 10 μM. Vandetanib inhibited the proliferation of HUVEC stimulated by VEGF-, EGF- and BFGF-with IC50 of 60 nM, 170 nM and 800 nM, respectively, but had little effect on the growth of basal endothelial cells. Vandetanib inhibits VEGFR-dependent tumor angiogenesis and EGFR - and RET - dependent tumor cell proliferation and survival to act on key signaling pathways in cancer. In transplanted tumor mice, Vandetanib inhibited the phosphorylation of VEGFR-2 and EGFR in tumor tissue, significantly reduced tumor vascular density, enhanced tumor cell apoptosis, inhibited tumor growth, improved survival rate, reduced the number of intrahepatic metastases, and upregulated VEGF, TGF-α, and EGF in tumor tissue. Vandetanib is currently being studied in phase III in patients with unresectable locally advanced or metastatic inherited or dispersed MTC.
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Vandetanib purchased from AbMole
| Molecular Weight | 475.35 |
| Formula | C22H24BrFN4O2 |
| CAS Number | 443913-73-3 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
|---|
| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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Products are for research use only. Not for human use. We do not sell to patients.
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