计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。
概述
Vandetanib is an antagonist of VEGFR (Flk and Flk) and EGFR families. Specifically inhibits kinase activity of Flk-1. Vandetanib is an inhibitor of Flt-4.An antagonist of VEGFR (Flk and Flk) and EGFR families.
Information
Vandetanib (ZD6474) is a potent inhibitor ofVEGFR2with IC50 of 40 nM in a cell-free assay. It also inhibitsVEGFR3andEGFRwith IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity again
In vitro
Vandetanib also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC50 of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC50 of 2.7 μM (A549) to 13.5 μM (Calu-6). Vandetanib displays an inhibitory effect on the basal ABCG2-ATPase. Parental and ABCG2-expressing A431 cells showed similar sensitivities toward Vandetanib. Exposure to EGFR inhibitors decreases pEGFR levels in A431 cells, with Vandetanib displaying only a moderate effect. Vandetanib displays a slight but measurable effect, whereas gefitinib, pelitinib and neratinib completely inhibit ABCG2-mediated efflux of mitoxantrone from A431/ABCG2 cells, similarly to the specific ABCG2 inhibitor Ko143. Vandetanib inhibits both PC3wt and PC3R cell lines with similar IC50 of 13.3 μM and 11.5 μM, respectively. Vandetanib suppresses phosphorylation of VEGFR2 in HUVEC and EGFR in hepatoma cells and inhibits cell proliferation. Vandetanib causes an accumulation of cells in the G0-G1 phases in GEO and OVCAR-3 cells and increases apoptosis in OVCAR-3, ZR-75-1, MCF-10A ras, and GEO cells. Vandetanib causes a dose-dependent inhibition of EGFR phosphorylation in mouse NIH-EGFR fibroblasts and human MCF-10A ras breast cancer cells, two cell lines that overexpress the human EGFR. Vandetanib treatment results in a dose-dependent inhibition of soft agar growth in seven human cell lines (breast, colon, gastric, and ovarian) with functional EGFR but lacking VEGFR2.
In vivo
Vandetanib (2.5 mg/kg, i.v.), reverses a VEGF-induced hypotension by 63% but does not significantly affect a bFGF-induced hypotension. Vandetanib (100 mg/kg) inhibits the tumor-induced blood vessel formation by 79%. Vandetanib (12.5-100 mg/kg, orally) shows great tumor growth inhibition in human tumor xenografts including Calu-6, PC-3, MDA-MA-231, SKOV-3, SW620, A549, A431, B16-F10(AP3) and Lewis Lung, with little effects on body weight. In PC3wt xenografts, administration of Vandetanib alone exerts paradoxical tumor growth stimulating effects. In PC3R xenografts, the low dose of Vandetanib (25 mg/kg) has no significant effect relative to control, whereas the high dose (50 mg/kg) significantly inhibits tumor growth compared with control. In contrast, the high-dose combination reveals a significant negative interaction between Vandetanib 50 mg/kg and docetaxel 30 mg/kg in PC3R cells. In tumor-bearing mice, Vandetanib suppresses phosphorylation of VEGFR2 and EGFR in tumor tissues, significantly decreases tumor vessel density, enhances tumor cell apoptosis, suppresses tumor growth, improves survival, reduces number of intrahepatic metastases, and up-regulates VEGF, TGF-alpha and EGF in tumor tissues. Treatment with Vandetanib is not associated with serious adverse events, including ALT abnormality, bone marrow suppression or body weight loss. Vandetanib treatment of nude mice bearing palpable GEO colon cancer xenografts (which are sensitive to inhibition of EGFR signaling) induces dose-dependent tumor growth inhibition.
Cell Data
cell lines：HT-29, HCT-15, HCT116, COLO205, LS-174T, SW480, SW620, T84, LoVo and COLO320
Concentrations：0.1–100 μM
Incubation Time：72 hours
Powder Purity:≥99%
规格
别名
凡德他尼 (ZD6474)
英文别名
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
规格或纯度
Moligand™, 2mM in DMSO
英文名称
Vandetanib (ZD6474)
生化机理
凡德他尼（ZD6474）是 VEGFR2 的强效抑制剂，在无细胞试验中的 IC50 为 40 nM。它还能抑制 VEGFR3 和表皮生长因子受体，IC50 分别为 110 nM 和 500 nM。对 PDGFRβ、Flt1、Tie-2 和 FGFR1 不敏感，IC50 为 1.1-3.6 μM。对 MEK、CDK2、c-Kit、erbB2、FAK、PDK1、Akt 和 IGF-1R 没有活性，IC50 超过 10 μM。凡德他尼（ZD6474）通过增加活性氧（ROS）水平来增加细胞凋亡和诱导自噬。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
表皮生长因子受体抑制剂
名称和识别符
EC号
669-841-4
分子类型
小分子
Isomeric SMILES
CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=C(C=C4)Br)F)OC
PubChem CID
分子量
475.36
技术文档
高级数据
关联靶点（人）
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(26 活性数据)
DDR1
Tchem
上皮盘状结构域受体 1(Epithelial discoidin domain-containing receptor 1)
(2 活性数据)
RET
Tclin
原癌基因酪氨酸蛋白激酶受体 Ret(Proto-oncogene tyrosine-protein kinase receptor Ret)
(7 活性数据)
RIPK2
Tchem
受体相互作用丝氨酸/苏氨酸蛋白激酶 2(Receptor-interacting serine/threonine-protein kinase 2)
(2 活性数据)
LCK
Tclin
酪氨酸蛋白激酶Lck(Tyrosine-protein kinase Lck)
(2 活性数据)
BCR
Tclin
断点簇区域蛋白质(Breakpoint cluster region protein)
(1 活性数据)
FLT1
Tclin
血管内皮生长因子受体 1(Vascular endothelial growth factor receptor 1)
(1 活性数据)
KDR
Tclin
血管内皮生长因子受体 2(Vascular endothelial growth factor receptor 2)
(10 活性数据)
ABL1
Tclin
酪氨酸蛋白激酶ABL1(Tyrosine-protein kinase ABL1)
(9 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 25 mg/mL (97.13 mM); Ethanol: 23 mg/mL (89.36 mM); Water: Insoluble;
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H302: 吞食有害
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P301+P312: 如误吞咽：如感觉不适，呼叫急救中心/医生。
P302+P352: 如皮肤沾染：用水充分清洗。
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）