WAY-600,1062159-35-6

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YZ剂描述：

产品名称：WAY-600

产品别名：4-[6-(1H-indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine

英文别名：WAY-600

靶点：mTOR

CAS：1062159-35-6

纯度：0.9934

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：WAY-600 is a potent, ATP-competitive and selective inhibitor of <b>mTOR</b> with <b>IC50</b> of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

溶解性：体外:
DMSO 22mg/mL(44.48mM)
Ethanol 2mg/mL(4.04mM)
Water <1mg/mL

体外研究：

免疫复合物激酶试验表明mTORC2-特异性底物His6-AKT或mTORC1底物His6-S6K被WAY-600剂量依赖性YZ。在细胞模型中，WAY-600剂量依赖性完全YZmTOR信号和AKT功能。在MDA361，人乳腺癌细胞中，WAY-600显著YZcap-依赖性和总体蛋白质合成。WAY-600在各种癌细胞系中表现出抗增殖活性，包括G1细胞周期阻滞和选择性细胞凋亡。在U87MG，MDA361 和LNCap 细胞中，WAY-600下调血管生成因子，VEGF和HIF-1α。

体内研究：

Administration of WAY-600 (10 mg/kg, daily) inhibits HepG2 tumor growth in nude mice. Daily HepG2 tumor growth of WAY-600-administrated mice is significantly lower than that of vehicle control mice. Importantly, the in vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5 mg/kg, p.o. daily).

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