化合物 NVP-TAE 226|T1918|TargetMol

NVP-TAE 226
761437-28-9

￥443 1mg 起订

￥987 5mg 起订

￥1630 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 NVP-TAE 226

英文名称：: NVP-TAE 226

CAS号：: 761437-28-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.17%

产品类别：: 抑制剂

货号：: T1918

Product Introduction

Bioactivity

Name	NVP-TAE 226
Description	NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.
Cell Research	Cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2 × 104 in 24-well culture plates for 24 h before drug treatment. Culture medium is used for mock treatment. Cells are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyze(Only for Reference)
Kinase Assay	Kinase assay: Kinase activities are assayed in Buffer A or C at 30°C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated during a 10 min incubation. Controls are performed with appropriate dilutions of dimethylsulfoxide. In a few cases phosphorylation of the substrate is assessed by autoradiography after SDS-PAGE. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/ml 10 mM DTT, with 5 μl 40 μM GS-1 peptide, a specific GSK-3 substrate, (YRRAAVPPSPSLSRHSSPHQSpEDEEE), in buffer A, in the presence of 15 μM [γ-32P] ATP (3,000 Ci/mmol; 1 mCi/ml) in a final volume of 30 μl. After 30 min incubation at 30°C, 25 μl aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and 20 seconds later, the filters are washed five times (for at least 5 min each time) in a solution of 10 ml phosphoric acid/liter of water. The wet filters are counted in the presence of 1 ml ACS scintillation fluid.
In vitro	在体内模型中,NVP-TAE226（100 mg/kg,p.o.）对MIA PaCa-2人胰腺肿瘤生长具有显著抑制效果,但不影响体重.在体内模型中,NVP-TAE226剂量依赖性地抑制4T1小鼠乳腺瘤生长和肺转移,这与Y397上FAK的自磷酸化和丝氨酸473上Akt磷酸化的抑制相关.NVP-TAE226（75 mg/kg）使负荷颅内胶质瘤异种移植小鼠的存活率显著增加.在人结肠癌SCID小鼠模型中,NVP-TAE226（100 mg/kg,p.o.）使微血管密度显著降低.
In vivo	NVP-TAE226（0.1-10 μM）对HMEC1细胞的微管形成具有抑制作用。在血清饥饿的U87细胞中,NVP-TAE226（<1 μM）抑制细胞外基质诱导的FAK(Tyr397)自身磷酸化。在U87和U251细胞中,NVP-TAE226（<1 μM）也会抑制IGF-I-诱导的IGF-1R磷酸化及其下游靶点基因活性（如MAPK 和Akt）。在体外胶质瘤细胞系人工基底膜侵袭实验中,与对照组相比, NVP-TAE226（1 μM）对肿瘤细胞侵袭具有抑制效果（>50%）。在caspase-3/7活化和poly(ADP-ribose)聚合酶裂解以及膜联蛋白V凋亡试验中,NVP-TAE226（1 μM）对胶质瘤细胞系,包括野生型p53,仅表现出G(2)-M期阻滞,但负荷突变体p53的胶质瘤细胞则会出现细胞凋亡。在人成神经细胞瘤细胞系SK-N-AS中, NVP-TAE226（5 μM）抑制FAK磷酸化。在人成神经细胞瘤细胞系SK-N-AS中,NVP-TAE226（<10 μM）的治疗会使细胞活性降低,细胞周期阻滞,以及细胞凋亡增加。在U87和U251细胞中,NVP-TAE226（<10 μM）阻碍肿瘤细胞生长,并减弱G(2)-M细胞周期进程,这与细胞周期素B1和磷酸化cdc2(Tyr15)蛋白质表达的减少相关。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 87 mg/mL (185.5 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
Keywords	inhibit \| TAE 226 \| TAE-226 \| IGF-1R \| Focal adhesion kinase \| Insulin Receptor \| NVP-TAE-226 \| Inhibitor \| Apoptosis \| NVP-TAE226 \| PTK2 protein tyrosine kinase 2 \| Pyk2 \| NVP-TAE 226 \| NVPTAE 226 \| Proline-rich tyrosine kinase 2 \| NVP TAE 226 \| PTK2 \| FAK
Inhibitors Related	Lidocaine hydrochloride \| Metronidazole \| Apocynin \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate \| Kaempferol
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Metabolism Compound Library \| Kinase Inhibitor Library \| Apoptosis Compound Library \| Anti-Aging Compound Library \| Membrane Protein-targeted Compound Library \| Tyrosine Kinase Inhibitor Library

TAE226|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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