GNE-477( GNE477 | GNE 477 )

Catalog No. M10157 CAS No. 1032754-81-6

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-477
Note

Research use only, not for human use.
Brief Description

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

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.
In Vitro

——
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.
Synonyms

GNE477 | GNE 477
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

mTOR|PI3Kα
Research Area

Cancer
Indication

——

CAS Number

1032754-81-6
Formula Weight

504.6288
Molecular Formula

C21H28N8O3S2
Purity

>98% (HPLC)
Solubility

DMSO: < 9.2 mg/mL
SMILES

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

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

1. Heffron TP, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11.

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