Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vandetanib hydrochloride (D6474 hydrochloride) 是一种有效的,口服的VEGFR2/KDR 酪氨酸激酶抑制剂 (IC50=40 nM)。Vandetanib hydrochloride 对于VEGFR3/FLT4(IC50=110 nM) 和EGFR/HER1(IC50=500 nM)也有抑制作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
Vandetanib hydrochloride 的其他形式现货产品:
产品描述 | Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity with IC 50 of 40 nM. Vandetanib hydrochloride also has some additional activity versus the tyrosine kinase activity of VEGFR3/FLT4 ( IC 50 =110 nM) and EGFR/HER1 ( IC 50 =500 nM) [1]. |
体外活性 | Vandetanib inhibits VEGFR3 and EGFR with IC 50 of 110 nM and 500 nM, respectively. However, Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC 50 of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC 50 above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC 50 of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC 50 of 2.7 μM (A549) to 13.5 μM (Calu-6) [1]. Odanacatib is a weak inhibitor of antigen presentation, measured in a mouse B cell line (IC 50 =1.5±0.4 μM), compared to the Cat S inhibitor LHVS (IC 50 =0.001 μM) in the same assay. Odanacatib also shows weak inhibition of the processing of the MHC II invariant chain protein Iip10 in mouse splenocytes compared to LHVS (minimum inhibitory concentration 1-10 μM versus 0.01 μM, respectively) [2]. Vandetanib suppresses phosphorylation of VEGFR-2 in HUVECs and EGFR in hepatoma cells and inhibits cell proliferation [4]. |
体内活性 | Vandetanib (15 mg/kg, p.o.) shows a superior anti-tumor effect than gefitinib in the H1650 xenograft model, and with IC 50 of 3.5±1.2 μM for inhibiting tumor growth [3]. In tumor-bearing mice, vandetanib (50 or 75 mg/kg) suppresses phosphorylation of VEGFR-2 and EGFR in tumor tissues, significantly reduces tumor vessel density, enhances tumor cell apoptosis, suppresses tumor growth, improves survival, reduces number of intrahepatic metastases, and upregulates VEGF, TGF-α, and EGF in tumor tissues [4]. |
分子量 | 511.81 |
分子式 | C22H25BrClFN4O2 |
CAS No. | 524722-52-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Vandetanib hydrochloride 524722-52-9 Vandetanib Hydrochloride Inhibitor inhibitor inhibit