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GNE-477

CAS No. : 1032754-81-6

MCE 国际站：GNE-477

产品活性：GNE-477 是一种高效的双重 PI3K (IC₅₀=4 nM)/mTOR (K_i=21 nM) 抑制剂。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K  |  mTOR

In Vitro: GNE-477 (Compound 8) has improved potency in the MCF7.1 cell proliferation assay with an EC₅₀ of 143 nM.

In Vivo: GNE-477 also exhibits stasis in a PC3 tumor growth inhibition study. In an experiment evaluating the tumor growth inhibition of a PC3 tumor xenograft over 14 days, stasis is achieved at a 20 mg/kg QD dose and significant inhibition is observed with doses as low as 1 mg/kg QD. GNE-477 is generally well tolerated during this study as demonstrated by acceptable levels of weight loss comparable to that observed with the animals in the vehicle cohort.

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