Vandetanib (443913-73-3) is a potent and selective inhibitor of VEGFR2 (KDR IC50 = 40 nM). Also inhibits fms-like tyrosine kinase 4 (VEGFR3, IC50 = 110 nM) and epidermal growth factor receptor (EGFR/HER1, IC50 = 500 nM) but shows selectivity against a panel of other tyrosine and serine-threonine kinases. Inhibits colony formation in seven cancer cell lines.2 Displays anti-angiogenesis activity.3 Vandetanib(443913-73-3)是VEGFR2的一种有效的选择性抑制剂(KDR IC50 = 40 nM)。 也可抑制fms样酪氨酸激酶4 (VEGFR3, IC50 = 110 nM)和表皮生长因子受体(EGFR/HER1, IC50 = 500 nM),但对其他酪氨酸和丝氨酸-苏氨酸激酶显示选择性。 抑制7种癌细胞的集落形成 显示抗血管生成activity.3
References/Citations:
Wedge et al. (2002), ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis and tumor growth following oral administration; Cancer Res., 62 4645
Ciardiello et al. (2003), Antitumor effects of ZD6474, a small molecule vascular endothelial growth factor receptor tyrosine kinase inhibitor, with additional activity against epidermal growth factor receptor tyrosine kinase; Clin. Cancer Res., 9 1546
Herbst et al. (2007), Vandetanib (ZD6474): an orally available receptor tyrosine kinase inhibitor that selectively targets pathways critical for tumor growth and angiogenesis; Expert Opin. Investig. Drugs, 16 239
CAS:
443913-73-3
Catalog Number:
10-2185
Activity:
VEGFR2 inhibitor
Chemical Names:
4-(4-Bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-yl)methoxy]quinazoline
Alternate Name:
ZD6474
Molecular Weight:
475.35
Molecular Formula:
C22H24BrFN4O2 Solubility:
Soluble in DMSO (30 mg/ml); Ethanol (10 mg/ml with warming)
Physical Properties:
White to off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
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