TAE-226CAS号: 761437-28-9分子式: C23H25ClN6O3分子量: 468.94描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
TAE226, TAE-226,TAE 226,NVPTAE226
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外观 |
Powder
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可溶性/溶解性 |
DMSO 94 mg/mL (200.45 mM)
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生物活性 | |
靶点 |
PYK2 ,FAK ,Insulin Receptor ,IGF-1R ,c-Met
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In vitro(体外研究) |
NVP-TAE226 ( NVP-TAE226 (5 μM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. NVP-TAE226 ( NVP-TAE226 (0.1 μM-10 μM) inhibits tube formation of HMEC1 cells.
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In vivo(体内研究) |
NVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. NVP-TAE226 inhibits 4T1 murine breast tumor growth and metastasis to the lung in a dose-dependent manner in vivo model, associated with inhibition of FAK autophosphorylation at Y397 and Akt phosphorylation at Serine473.
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分子结构图