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位置:首页 > 品牌 > Sigma-Aldrich > VEGFR Tyrosine Kinase Inhibitor VI, AAL-993-CAS 269390-77-4-Calbiochem

VEGFR Tyrosine Kinase Inhibitor VI, AAL-993-CAS 269390-77-4-Calbiochem

品牌
Sigma-Aldrich
CAS
269390-77-4
货号
676504
规格纯度
The VEGFR Tyrosine Kinse Inhibitor VI, ALL-993, also referenced under CAS 269390-77-4, controls the biological activity of VEGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Cancer applications.
参考价格
2566.78 *本价格含增值税费
促销
服务
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数量
-+
产品名称:
269390-77-4
VEGFR Tyrosine Kinase Inhibitor VI, AAL-993-CAS 269390-77-4-Calbiochem
2-((4-Pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide, ZK260253, PDGFR Tyrosine Kinase Inhibitor XXIII, VEGFR2 Kinase Inhibitor XXXIII, VEGFR1 Kinase Inhibitor VIII, VEGFR3 Kinase Inhibitor VII, AAL993
PDGFR Tyrosine Kinase Inhibitor XXIII, 2-((4-Pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide, ZK260253, VEGFR2 Kinase Inhibitor XXXIII, VEGFR1 Kinase Inhibitor VIII, VEGFR3 Kinase Inhibitor VII, AAL993
产品介绍:

产品说明

一般描述

A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC50 = 1.24 nM against VEGF-induced human VEGFR-2 phosphorylation in CHO cells) by targeting the ATP-binding site of VEGFR in its inactive "DFG-out" conformation and effectively suppresses tumor growths (50 to 100 mg/kg; p.o.) via its anti-angiogenesis activity in mice and rats in vivo, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-β, and c-Abl only at higher concentrations (IC50 = 236, 380, 640, and 2820 nM, respectively). AAL933 and two other VEGFR inhibitors, KRN633 and SU5416, are also shown to inhibit hypoxia-induced HIF-1α expression (by <90% at 30 M) and transcription activation. Unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells.
A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC50 = 1.24 nM against VEGF-induced human VEGFR-2 phosphorylation in CHO cells) by targeting the ATP-binding site of VEGFR in its inactive "DFG-out" conformation, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-β, and c-Abl only at higher concentrations (IC50 = 236, 380, 640, and 2820 nM, respectively) and displaying little or no activity against EGFR/HER-1/ErbB (IC50 = 10.4 M) and six other kinases (IC50 ≥10 M). Reported to be orally available in mice (Conc. in plasma = 9.5, 4.7, 1.5, and 1.1 M, respectively, 0.5 h, 1 h, 1.5 h, and 2 h after p.o. dosage of 50 mg/kg), rats, and dogs, and effectively suppress tumor growths (50 to 100 mg/kg; p.o.) via its anti-angiogenesis activity in various cancer models in vivo, including murine melanoma B16-BL6, rat mammary adenocarcinoma BN472, as well as human prostate cancer DU145-grafted mice in vivo. AAL933 and two other VEGFR inhibitors, KRN633 and SU5416, are also shown to inhibit hypoxia- (1% O2) induced HIF-1α expression (by <90% at 30 M) and transcription activation (IC50 = 6.53, 3.79, and 8.24 M, respectively, by AAL933, KRN633, and SU5416 in HeLa-HRE-Luc reporter assays). However, unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells.

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Ban, H.S., et al. 2010. Cancer Lett.296, 17; Manley, P.W., et al. 2004. Biochim. Biophys. Acta1697, 17; Manley, P.W., et al. 2002. J. Med. Chem.45, 5687.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C20H16F3N3O
分子量371.36

产品性质

质量水平100
测定≥97% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 off-white
溶解性DMSO: 100 mg/mL
运输ambient
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 2
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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