NVP-TAE 226
作者：齐岳
发布时间：2023-08-24
09:17:21
点击数：
产品名称：NVP-TAE 226
产品描述：
| 产品描述 | NVP-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. |
| 靶点活性 | FAK:5.5 nM, PYK2:3.5 nM |
| 体外活性 | 在体内模型中,NVP-TAE226（100 mg/kg,p.o.）对MIA PaCa-2人胰腺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*SCID小鼠模型中,NVP-TAE226（100 mg/kg,p.o.）使微血管密度显著降低. |
| 体内活性 | 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**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。 |
| 激酶实验 | 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. |
| 细胞实验 | 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) |
| 别名 | TAE226 |
| 分子量 | 468.94 |
| 分子式 | C23H25ClN6O3 |
| CAS No. | 761437-28-9 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 87 mg/mL (185.5 mM)
Ethanol: <1 mg/mL
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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