GNE-477

Research use only, not for human use.

A potent, dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Ki of 21 nM for mTOR.

A potent, dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Ki of 21 nM for mTOR; inhibits MCF7.1 cell proliferation with EC50 of 143 nM; displays desirable pharmacokinetic properties, exhibits stasis in a PC3 tumor growth inhibition study.

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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.

GNE477 | GNE 477

PI3K/Akt/mTOR signaling

PI3K

mTOR|PI3Kα

Cancer

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1032754-81-6

504.6288

C21H28N8O3S2

>98% (HPLC)

DMSO: < 9.2 mg/mL

NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(CN5CCN(S(=O)(C)=O)CC5)S4)=N2)C=N1

2-Pyrimidinamine, 5-[7-methyl-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-

(-20℃)

With Ice Pack

≥ 2 years