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My CartCAS：443913-73-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 443913-73-3 |
| Name | Vandetanib |
| Molecular Formula | C22H24BrFN4O2 |
| Molecular Weight | 475.35 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 669-841-4 |
| MDL | MFCD07772346 |
| SMILES | FC1=CC(Br)=CC=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C23)OC |
| Target Point | VEGFR |
| Passage | Angiogenesis;Protein Tyrosine Kinase/RTK |
| Background | Vandetanib is a potent VEGFR2 inhibitor. |
| Biological Activity | Vandetanib是有效的 VEGFR2 抑制剂，IC50 为40 nM。Vandetanib抑制VEGFR3和EGFR，IC50分别为110 nM和500 nM。[1-4] |
| In Vitro | Vandetanib抑制VEGF，EGF和bFGF刺激的HUVEC增殖，IC50为60 nM，170 nM和800 nM，对基底内皮细胞生长无影响。Vandetanib对PDGFRβ，Flt1，Tie-2和FGFR1不敏感，IC50为1.1-3.6μM，而对ICK，CDK2，c-Kit，erbB2，FAK，PDK1，Akt和IGF-1R几乎没有活性，IC50高于10μM。 Vandetanib抑制肿瘤细胞生长，IC50为2.7μM(A549)至13.5μM(Calu-6)[1]。与同一试验中的Cat S抑制剂LHVS(IC50 =0.001μM)相比，Odanacatib是抗原呈递的弱抑制剂，在小鼠B细胞系中测量(IC50 = 1.5±0.4μM)。与LHVS相比，Odanacatib还显示对小鼠脾细胞中MHC II恒定链蛋白Iip10的加工的抑制作用较弱(最小抑制浓度分别为1-10μM和0.01μM)[2]。 Vandetanib抑制HUVEC中VEGFR-2的磷酸化和肝癌细胞中EGFR的磷酸化并抑制细胞增殖[4]。 |
| In Vivo | 在H1650异种移植模型中，Vandetanib(15 mg/kg，po)具有优于吉非替尼的抗肿瘤效果，并抑制肿瘤生长，IC50为3.5±1.2μM[3]。在荷瘤小鼠中，Vandetanib(50或75 mg/kg)抑制肿瘤组织中VEGFR-2和EGFR的磷酸化，显著降低肿瘤血管密度，增强肿瘤细胞凋亡，抑制肿瘤生长，提高存活率，减少肝内转移的数量，并在肿瘤组织中上调VEGF，TGF-α和EGF [4]。 |
| Cell Experiment | 通过改良的MTT测定法测量生长抑制。简而言之，将细胞以每孔2000个细胞的密度接种在96孔板上，并暴露于每个吉非替尼或Vandetanib72小时。 |
| Animal Experiment | 将100万个H1650细胞或H1650/PTEN细胞(具有转染的PTEN基因的H1650细胞)皮下注射到每只小鼠的背部。在注射后第10天，将小鼠随机分配至三组，其接受载体，Vandetanib(15mg/kg /天)或吉非替尼(15mg/kg /天)。Vandetanib和吉非替尼每天口服一次，每周五次。定期测定肿瘤体积和体重。 |
| Data Literature Source | [1]. Wedge SR，et al. ZD6474 inhibits vascular endothelial growth factor signaling，angiogenesis，and tumor growth following oral administration. Cancer Res. 2002 Aug 15;62(16):4645-55. [2]. Hegedus C，et al. Interaction of the EGFR inhibitors gefitinib，vandetanib，pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance. Biochem Pharmacol. 2012 Aug 1;84(3):260-7. [3]. Takeda H，et al. Vandetanib is effective in EGFR-mutant lung cancer cells with PTEN deficiency. Exp Cell Res. 2013 Feb 15;319(4):417-23. [4]. Inoue K，et al. Vandetanib，an inhibitor of VEGF receptor-2 and EGF receptor，suppresses tumor development and improves prognosis of liver cancer in mice. Clin Cancer Res. 2012 Jul 15;18(14):3924-33. Vandetanib物理化学性质 |
| Unit | Piece |
| Specification | 10mg 50mg 100mg |
Vandetanib是有效的 VEGFR2 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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