TAE226 (NVP-TAE226)|761437-28-9|(TAE226)-陌孚医药/Medlife

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TAE226 (NVP-TAE226) (Synonyms: TAE226)

目录号: PC16081 纯度: ≥98%

CAS No. :761437-28-9

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PC16081-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1656.00	请登录

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中文名称

TAE226 (NVP-TAE226)

中文别名

2-[[5-氯-2-[[2-甲氧基-4-(4-吗啉)苯基]氨基]-4-嘧啶]氨基]-N-甲基苯甲酰胺;2-[[5-氯-2-[[2-甲氧基-4-(4-吗啉基)苯基]氨基]-4-嘧啶基]氨基]-N-甲基苯甲酰胺;TAE226 NVP-TAE226 抑制剂

英文名称

TAE226 (NVP-TAE226)

英文别名

2-((5-Chloro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide;TAE226 (NVP-TAE226);2-((5-Chloro-2-((2-methoxy-4-morpholinophenyl)-amino)pyrimidin-4-yl)amino)-N-methylbenzamide;2-[[5-Chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methylbenzamide;2-[5-chloro-2-[2-methoxy-4-(4-morpholinyl)phenylamino]pyrimidin-4-ylamino]-N-methylbenzamide;NVP-TAE 226;NVPTAE226;TAE226;TAE-226;2-({5-Chloro-2-[(2-Methoxy-4-Morpholin-4-Ylphenyl)amino]pyrimidin-4-Yl}amino)-N-Methylbenzamide;2-[5-chloro-2-(2-methoxy-4-morpholin-4-yl-phenylamino)-pyrimidin-4-ylamino]-N-methyl-benzamide;2jkk;CHEMBL458997;Kinome_1212;SureCN375524;C23H25ClN6O3;UYJNQQDJUOUFQJ-UHF

Cas No.

761437-28-9

分子式

C₂₃N₆O₃ClH₂₅

分子量

468.94

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC₅₀s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC₅₀s of 3.5 nM and 44 nM, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 5.5 nM (FAK), 3.5 nM (Pyk2), 140 nM (IGF-IR), 40 nM (InsR), 0.16 μM (c-Met), 0.36 μM (KDR), 0.48 μM (Flt3)

体外研究(In Vitro)

NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC₅₀ range of 100 to 300 nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G₂-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr) protein expression. NVP-TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an 体外研究 Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G₂-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Treatment with NVP-TAE 226 (TAE226) at 50 or 75 mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042, respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages, compared with vehicle-treated animals).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Liu TJ, et al. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation 体外研究 and in vivo. Mol Cancer Ther, 2007, 6(4), 1357-1367. [Information]

[2]. Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9(6):e99083. [Information]

[3]. Lietha D, et al. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One. 2008;3(11):e3800. [Information]

溶解度数据

体外研究:

DMSO : 11.11 mg/mL (23.69 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1325 mL	10.6623 mL	21.3247 mL
5 mM	0.4265 mL	2.1325 mL	4.2649 mL
10 mM	0.2132 mL	1.0662 mL	2.1325 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 1.11 mg/mL (2.37 mM); Suspended solution; Need ultrasonic

此方案可获得 1.11 mg/mL (2.37 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: 1.11 mg/mL (2.37 mM); Clear solution; Need ultrasonic

此方案可获得 1.11 mg/mL (2.37 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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