TAE226(NVP-TAE226)是一种强效的ATP竞争性抑制剂，能抑制多种酪氨酸蛋白激酶，尤其是FAK和IGF-IR激酶，其IC50值分别为5.5nM和140nM。
Cas No.:761437-28-9
Sample solution is provided at 25 µL, 10mM.
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TAE226(NVP-TAE226) is a potent ATP-competitive inhibitor that inhibits a variety of tyrosine protein kinases, especially FAK and IGF-IR kinases, with IC50 values of 5.5nM and 140nM, respectively. TAE226 antagonizes both FAK and IGF-IR signaling pathways, resulting in growth inhibition, cell cycle arrest, attenuation of tumor invasion, and induction of apoptosis. TAE226 also effectively inhibits Pyk2 and the insulin receptor (InsR), with IC50 values of 3.5nM and 44nM, respectively[1][2].
In vitro, treatment with 1 and 10μM TAE226 for 1–5 days inhibited the growth of U87, U87/EGFR, and U87/EGFRvIII cell lines in a dose-dependent manner, with U87/EGFR and U87/EGFRvIII cells showing greater sensitivity to TAE226[1].
In vivo, oral administration of TAE226 (50 or 75mg/kg) once daily for 5 days followed by 2 days off for 4 weeks extended the median survival of U87 xenograft animals by 6 and 7 days, respectively[1]. Oral administration of TAE226 (50 or 75mg/kg) once daily for 5 days followed by 2 days off for 4 weeks extended the median survival of LN229 xenograft animals by 19 and 25 days[1].
References:
[1] Liu TJ, LaFortune T, Honda T, 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):1357-1367.
[2] Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9(6):e99083.
TAE226(NVP-TAE226)是一种强效的ATP竞争性抑制剂，能抑制多种酪氨酸蛋白激酶，尤其是FAK和IGF-IR激酶，其IC50值分别为5.5nM和140nM。TAE226能够阻断FAK和IGF-IR信号通路，从而实现生长抑制、细胞周期停滞、肿瘤侵袭减弱以及细胞凋亡诱导的效果。TAE226还能够有效抑制Pyk2和胰岛素受体（InsR），其IC50值分别为3.5nM和44nM[1][2]。
体外实验中，用1和10μM的TAE226处理1–5天，可剂量依赖性地抑制U87、U87/EGFR和U87/EGFRvIII细胞系的生长，其中U87/EGFR和U87/EGFRvIII细胞对TAE226更为敏感[1]。
体内实验中，口服给予TAE226（50或75mg/kg），每日一次，连续给药5天后停药2天，按此周期持续4周，可使U87移植瘤动物的中位生存期分别延长6天和7天[1]。同样的给药方案下，口服给予TAE226（50或75mg/kg），每日一次，连续给药5天后停药2天，持续4周，可使LN229移植瘤动物的中位生存期分别延长19天和25天[1]。
| Cell experiment [1]: | |
Cell lines | U87, U87/EGFR, and U87/EGFRvIII cell lines |
Preparation Method | Cell lines were treated with different concentrations of TAE226 (1 and 10μM), and viable cells were counted at days 1, 3, and 5 after treatment using a trypan blue exclusion method. |
Reaction Conditions | 1 and 10μM; 1-5d |
Applications | TAE226 treatment significantly retarded the growth of all cell lines tested in a concentration-dependent manner, albeit having no direct correlation between FAK and IGF-IR expression and sensitivity to TAE226 treatment. U87/EGFR and U87/EGFRvIII cells were more sensitive to TAE226. Day 5 after TAE226 treatment, there were 22%, 14%, and 17% of viable U87, U87/EGFR and U87/EGFRvIII cells over their untreated control, respectively. |
| Animal experiment [1]: | |
Animal models | Male nude mice implanted with U87 cells and LN229 cells, respectively |
Preparation Method | Four days after injection of the tumor cells, mice were randomized into three groups for each cell line. Mice in group 1 were treated with 50mg/kg TAE226 in 200μL of 0.5% methylcellulose, via an oral gavage. The mice in group 2 received 75mg/kg TAE226 in 200μL of 0.5% methylcellulose. The mice in group 3 the same vehicle used for administration of TAE226 (control). Treatment frequency was once a day for 5 days and off for 2 days, for a duration of 4 weeks. Detecting animal survival rate. |
Dosage form | 50, 75mg/kg/d; p.o.; 5 days a week for 4 weeks |
Applications | Treatment with TAE226 at 50 or 75mg/kg extended the median survival of U87 xenograft animals by 6 and 7 days, respectively. TAE226 treatment of LN229-engrafted animals significantly prolonged their median survival by 19 and 25 days |
References: | |
| Cas No. | 761437-28-9 | SDF | |
| 别名 | TAE 226;TAE-226 | ||
| 化学名 | 2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide | ||
| Canonical SMILES | CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC | ||
| 分子式 | C23H25ClN6O3 | 分子量 | 468.94 |
| 溶解度 | ≥ 23.45mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1325 mL | 10.6623 mL | 21.3247 mL |
| 5 mM | 426.5 μL | 2.1325 mL | 4.2649 mL |
| 10 mM | 213.2 μL | 1.0662 mL | 2.1325 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet