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CAS No.: 761437-28-9

NVP-TAE 226 Catalog No. CSN13117

Synonyms: TAE226

NVP-TAE 226 is a potent FAK inhibitor with IC50 of 5.5 nM, modestly potent to Pyk2 (IC50=3.5 nM) and 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Pyk2

IC50:3.5nM FAK

IC50:5.5nM
描述Both abnormal activity of FAK (focal adhesion kinase) and IGF-IR (Insulin-like growth factor-I receptor) contribute to highly infiltrative and rapid growth characteristics in tumors, as FAK can regulate tumor migration, while the expression of IGF-IR correlate with tumor grade and involved in proliferation and survival. NVP-TAE 226 is multiple-target tyrosine kinase inhibitor with IC50 of 5.5nM and 120-160nM for FAK and IGF-IR (measured by in vitro kinase assays), respectively. Treatment with NVP-TAE 226 at concentration of 0.25-1μM could dose-dependently inhibit extracellular matrix (ECM)–induced activation of FAK on its Tyr397 phosphorylation site, as well as IGF-1-induced activation of IGF-1/AKT signaling, shown as decreased p-IGF1R, p-AKT and p-ERK, in U87 cells. Also NVP-TAE 226 significant inhibited glioma cell growth and disrupted cell cycle distribution with a marked decline in cyclin B1 and p-cdc2 protein expression at concentration of 10μM, as well as induces apoptosis in glioma cells containing mut-p53 at concentration of 1μM, including U251, LN18 and LN229 cell lines. As prediction, inhibition of FAK by 1μM NVP-TAE 226 significantly decreased the invasive propensity of glioma cells U87, U87/EGFRvIII, U251, and LN18. Oral administration of NVP-TAE 226 at dose of 50mg/kg and 75mg/kg prolonged the survial of prolongs the survival of glioma cell LN229 xenograft animals^[1].
作用机制NVP-TAE 226 is a potent ATP-competitive inhibitor of several tyrosine protein kinases.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
BT474 cells	1 μM	Function assay	24 h	Induction of apoptosis in human BT474 cells assessed as cleavage of 89 kDa PARP at 1 uM after 24 hrs by Western blotting	18989950
HCT116 cells	-	Proliferation assay	48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay, IC50=0.4 μM	25180654
HUVEC	-	Function assay	72 h	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay, IC50=1 μM	23845217

更多
动物研究
剂量
Mice: 50 mg/kg, 75 mg/kg^[1] (p.o.), 12.5 mg/kg - 100 mg/kg^[2] (gavage)

给药途径
p.o.

动物研究
剂量	Mice: 50 mg/kg, 75 mg/kg^[1] (p.o.), 12.5 mg/kg - 100 mg/kg^[2] (gavage)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1325 mL
- 10.6624 mL
- 21.3249 mL
- 5 mM
- 0.4265 mL
- 2.1325 mL
- 4.2650 mL
- 10 mM
- 0.2132 mL
- 1.0662 mL
- 2.1325 mL

技术信息

CAS号

761437-28-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H25ClN6O3

运输

蓝冰

分子量

468.94

别名

TAE226

溶解度

DMSO	94.0 mg/mL (200.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

0.5% methylcellulose+water

30 mg/mL

suspension

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NVP-TAE 226 Catalog No. CSN13117

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