若您需要咨询产品或有任何技术问题,请通过官方电话 400 885 9050 或邮箱 info.cn@stemcell.com 与我们联系

Vandetanib

酪氨酸激酶抑制剂;抑制VEGFR1、KDR、FLT-4、EGFR、FGFR、ABL、RET和SRC

产品号 #(选择产品)

产品号 #73532_C

酪氨酸激酶抑制剂;抑制VEGFR1、KDR、FLT-4、EGFR、FGFR、ABL、RET和SRC

总览

Vandetanib(凡德他尼)是一种多激酶抑制剂,主要靶向受体酪氨酸激酶,例如血管内皮生长因子受体(VEGFR1、KDR和FLT4)、表皮生长因子受体(EGFR)和成纤维细胞生长因子受体(FGFR;Morabito 等人)。它最强效抑制KDR,IC₅₀值为40 nM。它还能抑制非受体酪氨酸激酶,例如RET、ABL和SRC,以及多种丝氨酸/苏氨酸激酶(Carlomagno et al.; Hennequin et al.; Kiselyov et al.; Levinson & Boxer)。

癌症研究
·抑制小鼠异种移植模型中的肿瘤生长,包括RET/PTC乳头状甲状腺癌和肺癌(Hennequin et al.; Carlomagno et al.)。
·抑制多种癌细胞系中的血管生成、细胞生长和转移(Morabito et al.; Wedge et al.)。

细胞类型
癌细胞及细胞系
 
种属
人,小鼠,非人灵长类,其它细胞系,大鼠
 
研究领域
癌症
 
CAS 编号
443913-73-3
 
化学式
C₂₂H₂₄BrFN₄O₂
 
纯度
≥98%
 
通路
酪氨酸激酶
 
靶点
ABL,EGFR,FGFR,FLT4,KDR,RET,SRC,VEGFR1
 

产品说明书及文档

请在《产品说明书》中查找相关支持信息和使用说明,或浏览下方更多实验方案。

Document Type
Product Name
Catalog #
Lot #
Language
Product Name
Vandetanib
Catalog #
73532
Lot #
All
Language
English
Document Type
Safety Data Sheet
Product Name
Vandetanib
Catalog #
73532
Lot #
All
Language
English

相关材料与文献

技术资料 (2)

文献 (6)

Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain. Levinson NM and Boxer SG PloS one 2012

Abstract

Chronic myeloid leukemia (CML) is caused by the kinase activity of the BCR-Abl fusion protein. The Abl inhibitors imatinib, nilotinib and dasatinib are currently used to treat CML, but resistance to these inhibitors is a significant clinical problem. The kinase inhibitor bosutinib has shown efficacy in clinical trials for imatinib-resistant CML, but its binding mode is unknown. We present the 2.4 Å structure of bosutinib bound to the kinase domain of Abl, which explains the inhibitor's activity against several imatinib-resistant mutants, and reveals that similar inhibitors that lack a nitrile moiety could be effective against the common T315I mutant. We also report that two distinct chemical compounds are currently being sold under the name bosutinib"�
Vandetanib (ZD6474), a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) tyrosine kinases: current status and future directions. Morabito A et al. The oncologist 2009

Abstract

Vandetanib is a novel, orally available inhibitor of different intracellular signaling pathways involved in tumor growth, progression, and angiogenesis: vascular endothelial growth factor receptor-2, epidermal growth factor receptor, and REarranged during Transfection tyrosine kinase activity. Phase I clinical trials have shown that vandetanib is well tolerated as a single agent at daily doses textless or =300 mg. In the phase II setting, negative results were observed with vandetanib in small cell lung cancer, metastatic breast cancer, and multiple myeloma. In contrast, three randomized phase II studies showed that vandetanib prolonged the progression-free survival (PFS) time of patients with non-small cell lung cancer (NSCLC) as a single agent when compared with gefitinib or when added to chemotherapy. Rash, diarrhea, hypertension, fatigue, and asymptomatic QTc prolongation were the most common adverse events. Antitumor activity was also observed in medullary thyroid cancer. Four randomized phase III clinical trials in NSCLC are exploring the efficacy of vandetanib in combination with docetaxel, the Zactima in cOmbination with Docetaxel In non-small cell lung Cancer (ZODIAC) trial, or with pemetrexed, the Zactima Efficacy with Alimta in Lung cancer (ZEAL) trial, or as a single agent, the Zactima Efficacy when Studied versus Tarceva (ZEST) and the Zactima Efficacy trial for NSCLC Patients with History of EGFR-TKI chemo-Resistance (ZEPHYR) trials. Based on a press release by the sponsor of these trials, the PFS time was longer with vandetanib in the ZODIAC and ZEAL trials; the ZEST trial was negative for its primary superiority analysis, but was successful according to a preplanned noninferiority analysis of PFS. Ongoing phase II and III clinical trials will better define the appropriate schedule, the optimal setting of evaluation, and the safety of long-term use of vandetanib.
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2. Kiselyov AS et al. Chemical biology & drug design 2007

Abstract

Novel derivatives of 1,2,4-triazoles are described as potent ATP-competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR-1/2). A number of compounds display VEGFR-2 inhibitory activity comparable to that of Vatalanib and Vandetanib in both homogenous time-resolved fluorescence enzymatic and cellular assays. Several active molecules feature high intrinsic permeability (textgreater30 x 10(-5) cm/min) across Caco-2 cell monolayer.

更多信息

更多信息
种属 Human, Mouse, Non-Human Primate, Other, Rat
Cas Number 443913-73-3
Chemical Formula C₂₂H₂₄BrFN₄O₂
纯度 ≥ 98%
Target ABL, EGFR, FGFR, FLT4, KDR, RET, SRC, VEGFR1
Pathway Tyrosine Kinase
质量保证:

产品仅供研究使用,不用于针对人或动物的诊断或治疗。 欲获悉更多关于STEMCELL的质控信息,请访问 STEMCELL.CN/COMPLIANCE.
Copyright © 2025 by STEMCELL Technologies. All rights reserved.