首页工具

购物车

Vandetanib

产品编号 T1656 CAS 443913-73-3

别名: ZD6474, 凡德他尼

Vandetanib (ZD6474) 是一种具有口服活性的VEGFR2/KDR 酪氨酸激酶抑制剂，IC50值为40 nM。它也抑制VEGFR3/FLT4和EGFR/HER1，IC50值分别为110和500 nM。

TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

Vandetanib, CAS 443913-73-3

规格	价格/CNY	货期
5 mg	￥ 229	现货
10 mg	￥ 372	现货
25 mg	￥ 494	现货
50 mg	￥ 891	现货
100 mg	￥ 1,643	现货
500 mg	￥ 3,671	现货
1 mL * 10 mM (in DMSO)	￥ 413	现货

大包装超大折扣，点击咨询

其他形式的 Vandetanib:

选择批次

纯度: 100%

纯度: 99.7%

纯度: 98.83%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR.
靶点活性	EGFR:500 nM (cell free), VEGFR3:110 nM (cell free), VEGFR2:40 nM (cell free)
体外活性	Vandetanib (ZD6474) 是一种强效的KDR/VEGFR2酪氨酸激酶活性抑制剂（IC50：40 nM），对VEGFR3（IC50：110 nM）和EGFR/HER1酪氨酸激酶活性（IC50：500 nM）也有一定抑制作用。ZD6474对KDR酪氨酸激酶的抑制作用能强效抑制VEGF激活的内皮细胞（人脐静脉内皮细胞）增殖（IC50：60 nM）[1]。ZD6474能剂量依赖性抑制小鼠NIH-EGFR成纤维细胞和人MCF-10A ras乳腺癌细胞中EGFR的磷酸化，并在具有功能性EGFR但缺乏VEGFR-2的七种人类细胞系中，剂量依赖性抑制软琼脂生长。ZD6474与紫杉醇或多西他赛联合治疗在体外观察到增长抑制和凋亡的剂量依赖性超加性效应[2]。Vandetanib和neratinib对基础ABCG2-ATP酶活性表现出抑制效果，在相对高浓度（10-20 mM）时，vandetanib能抑制激活的ABCG2-ATP酶活性[3]。
体内活性	给予ZD6474 (2.5 mg/kg, 静脉注射) 能够逆转由VEGF引起的低血压变化(63%)，但对由基础成纤维细胞生长因子引起的变化无显著影响。每日一次口服50 mg/kg ZD6474给缺乏胸腺的小鼠（这些小鼠体内已经皮下植入了A549肿瘤细胞）同样显著抑制了由肿瘤引起的新血管生成（5天后抑制率达63%）。对于用50 mg/kg/day ZD6474处理24天的Calu-6肿瘤进行组织学分析显示，非坏死区域内CD31（内皮细胞）染色显著减少（>70%）[1]。ZD6474对携带可触知GEO结肠癌异种移植瘤的裸鼠治疗显示出剂量依赖性的肿瘤生长抑制作用。ZD6474在GEO肿瘤异种移植瘤模型中的抗肿瘤活性，在与紫杉醇联合应用时得到增强。所有使用ZD6474加紫杉醇治疗的小鼠观察到肿瘤退缩，并且伴随着显著增强的抗血管生成抑制作用[2]。Vandetanib (15 mg/kg) 对H1650/PTEN和H1650亲本异种移植瘤的生长具有相似的效果[4]。
激酶实验	The ability of ZD6474 to inhibit the kinase activity associated with the VEGFRs KDR, Flt-1, and Flt-4 was determined using a previously described ELISA. Briefly, ZD6474 was incubated with enzyme, 10 mm MnCl2, and 2 μm ATP in 96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate. Phosphorylated tyrosine was then detected by sequential incubation with a mouse IgG anti-phosphotyrosine 4G10 antibody, a horseradish peroxidase-linked sheep anti-mouse immunoglobulin antibody, and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid). Microcal Origin software was used to interpolate IC50 values by nonlinear regression. This methodology was adapted to examine selectivity versus tyrosine kinases associated with EGFR, PDGFRβ, Tie-2, FGFR1, c-kit, erbB2, IGF-IR, and FAK. All enzyme assays (tyrosine or serine-threonine) used appropriate ATP concentrations at or just below the respective Km (0.2–14 μm). Selectivity versus serine-threonine kinases (CDK2, AKT, and PDK1) was examined using a relevant scintillation proximity assay (SPA) in 96-well plates. CDK2 assays contained 10 mm MnCl2, 4.5 μm ATP, 0.15 μCi of [γ-33P]ATP/reaction, 50 mm HEPES (pH 7.5), 1 mm DTT, 0.1 mm sodium orthovanadate, 0.1 mm sodium fluoride, 10 mm sodium glycerophosphate, 1 mg/ml BSA fraction V, and a retinoblastoma substrate (part of the retinoblastoma gene, 792–928, expressed in a glutathione S-transferase expression system; 0.22 μm final concentration). Reactions were allowed to proceed at room temperature for 60 min before quenching for 2 h with 150 μl of a solution containing EDTA (62 mm final concentration), 3 μg of a rabbit immunoglobulin anti-glutathione S-transferase antibody and protein A SPA-polyvinyltoluene beads (0.8 mg/reaction). Plates were then sealed, centrifuged (1200 × g for 5 min), and counted on a Topcount NXT Microplate scintillation counter for 30 s [1].
细胞实验	HUVEC proliferation in the presence and absence of growth factors was evaluated using [3H]thymidine incorporation. Briefly, HUVECs isolated from umbilical cords were plated (at passage 2–8) in 96-well plates (1000 cells/well) and dosed with ZD6474 ± VEGF or EGF (3 ng/ml) or bFGF (0.3 ng/ml). The cultures were incubated for 4 days (37°C; 7.5% CO2) and then pulsed with 1 μCi/well [3H]thymidine and reincubated for 4 h. Cells were harvested and assayed for the incorporation of tritium using a beta counter. IC50 data were interpolated as described above [1].
动物实验	Methodology to enable blood pressure measurement in anesthetized rats was as described previously. Briefly, anesthesia was induced in male Alderley Park rats using α-chloralose by the i.v. route and then maintained with thiopentone via the i.p. route. Once surgical anesthesia was established, the carotid artery was cannulated to enable blood pressure recording using a pressure transducer and a Lectromed MT8P amplifier. The jugular vein was cannulated to allow growth factor administration. Body temperature was maintained with a thermostatically controlled heated blanket coupled to a rectal thermometer. Human VEGF165 (32 μg/kg) or bFGF (40 μg/kg) was administered as a bolus injection [0.1 ml/250 g body weight in 0.85% (w/v) sodium chloride], and a maximal blood pressure drop was recorded within 2 min (typically 26–30 mm Hg). These changes were sustainable for more than 20 min in control experiments. ZD6474 (2.5 mg/kg) or vehicle alone [25% (w/v) hydroxypropyl-β-cyclodextrin in Sorensons phosphate buffer (pH 5.5)] was administered i.v., and blood pressure was recorded 5 min later to determine the effect on growth factor-induced hypotension [1].

别名	ZD6474, 凡德他尼
分子量	475.35
分子式	C22H24BrFN4O2
CAS No.	443913-73-3

存储

|Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 27.5 mg/mL (57.85 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1037 mL	10.5186 mL	21.0371 mL	52.5928 mL
	5 mM	0.4207 mL	2.1037 mL	4.2074 mL	10.5186 mL
	10 mM	0.2104 mL	1.0519 mL	2.1037 mL	5.2593 mL
	20 mM	0.1052 mL	0.5259 mL	1.0519 mL	2.6296 mL
	50 mM	0.0421 mL	0.2104 mL	0.4207 mL	1.0519 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

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. Ciardiello F, et al. 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. 2003 Apr;9(4):1546-56. 3. 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. 4. 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. 5. Chang Z, Zhang Y, Liu J, et al. Snail promotes the generation of vascular endothelium by breast cancer cells[J]. Cell Death & Disease. 2020, 11(6): 1-17.

文献引用

1. Jin Y, Chen X, Gao Z, et al. Bisdemethoxycurcumin alleviates vandetanib-induced cutaneous toxicity in vivo and in vitro through autophagy activation. Biomedicine & Pharmacotherapy. 2021, 144: 112297. 2. Chang Z, Zhang Y, Liu J, et al. Snail promotes the generation of vascular endothelium by breast cancer cells. Cell Death & Disease. 2020, 11(6): 1-17

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +