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产品介绍
产品介绍
产品信息
抗原名称
mTOR；mTORC1；mTORC2；PI3Kα；PI3Kγ；PI3Kδ
商品描述
INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.
分子量
309.33
纯度
>98%
可溶性
DMSO : 58 mg/mL (187.5 mM)
Ethanol : 2 mg/mL (6.46 mM)
Ethanol : 2 mg/mL (6.46 mM)
外观
白色至类白色固体
In vitro(体外研究)
INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors.
In vivo(体内研究)
In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models.
背景
别名
沙帕色替；INK 128; INK128;Sapanisertib; MLN0128
分子式
C15H15N7O
CAS号
1224844-38-5
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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