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TAE226 (NVP-TAE226)

现货
Catalog No.
A8557
强效的ATP竞争性FAK抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
5mg
¥ 1,190.00
现货
10mg
¥ 1,890.00
现货
100mg
¥ 11,800.00
现货

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Background

TAE226 (NVP-TAE226) is a selective inhibitor of FAK with IC50 value of 5.5 nM [1].

Focal Adhesion Kinase (FAK) also known as PTK2 protein tyrosine kinase 2 (PTK2) is a focal adhesion-associated protein kinase and plays an important role in cellular adhesion and spreading processes [1].

TAE226 (NVP-TAE226) is a potent FAK inhibitor and has a different selectivity with the reported FAK inhibitor PF-562271. When tested with glioma cell lines U87, U87/EGFR, U87/EGFRvIII and U251 that expressed different level of FAK, TAE226 (NVP-TAE226) showed effective inhibition on the growth of the 4 cell lines in a dose dependent manner (1 and 10 μmol/L) and U87/EGFR, as well as U87/EGFRvIII, which had higher p-FAK expression than U87 were more sensitive to TAE226 (NVP-TAE226). Then, it was shown that TAE226 (NVP-TAE226) treatment inhibited Glioma cell invasion and induced apoptosis when tested with U251 and LN18 cell lines [1]. In the medullary thyroid tumor cell line MZ-CRC-1, TAE226 (NVP-TAE226) (100 nM and 1000 nM) treatment for 72 h inhibited cell proliferation, prolonged cellular processes and decreased cell invasion ability [2].

In male nude mice model with U87 subcutaneous xenograft, administration of TAE226 (NVP-TAE226) (50 or 75 mg/kg) prolonged the median survival of animals by 7 days with significant difference compared with control group (29 days) [1].

It is also reported that TAE226 (NVP-TAE226) is a potent inhibitor for Pyk2 with IC50 value of 3.5 nM [1].

References:
[1].  Liu, T.J., et al., Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther, 2007. 6(4): p. 1357-67.
[2].   Plaza-Menacho, I., et al., Focal adhesion kinase (FAK) binds RET kinase via its FERM domain, priming a direct and reciprocal RET-FAK transactivation mechanism. J Biol Chem, 2011. 286(19): p. 17292-302.

文献引用

1.Menanteau-Ledouble S, Lawrence ML, et al. "Invasion and replication of Yersinia ruckeri in fish cell cultures." BMC Vet Res. 2018 Mar 9;14(1):81. PMID:29523132

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt468.94
Cas No.761437-28-9
FormulaC23H25ClN6O3
SynonymsTAE 226;TAE-226
Solubility≥23.45mg/mL in DMSO
Chemical Name2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide
SDFDownload SDF
Canonical SMILESCNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人神经胶质瘤细胞系U87、U87/EGFR、U87/vIII和U251

制备方法

在DMSO中的溶解度大于23.5mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

1和10 μM

实验结果

在所有测试的人神经胶质瘤细胞系中,TAE226呈浓度依赖性地显著抑制肿瘤生长。与U87细胞相比,具有更高p-FAK (Tyr397)水平的U87/EGFR和U87/vIII细胞对TAE226更敏感。

动物实验 [1]:

动物模型

携带颅内胶质瘤异种移植物小鼠

给药剂量

50和75 mg/kg;口服给药;每日1次,持续5日,停药2日再给药,持续4周

实验结果

在U87细胞异种移植小鼠中,50或75 mg/kg TAE226将存活期中值分别延长6天和7天。 在LN229细胞异种移植小鼠中,TAE226显著延长19天的存活期中值。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Liu, T.J., et al., Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther, 2007. 6(4): p. 1357-67.

生物活性

描述 TAE226(NVP-TAE226)是一种有效的FAK抑制剂,其IC50值为5.5 nM。
靶点 PYK2 FAK Insulin Receptor IGF-1R c-Met  
IC50 3.5 nM 5.5 nM 43.5 nM 140 nM 160 nM  

质量控制

化学结构

TAE226 (NVP-TAE226)

相关生物数据

TAE226 (NVP-TAE226)