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GNE 477

  Cat. No.:  DC8257   Featured
Chemical Structure
1032754-81-6
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More than 5000 active chemicals with high quality for research!
Field of application
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1032754-81-6
Chemical Name: 5-[7-Methyl-4-(Morpholin-4-yl)-6-[(4-Methylsulfonylpiperazin-1-yl)Methyl]thieno[3,2-d]pyriMidin-2-yl]pyriMidin-2-aMine
Synonyms: GNE-477,GNE477
SMILES: NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(CN5CCN(S(=O)(C)=O)CC5)S4)=N2)C=N1
Formula: C21H28N8O3S2
M.Wt: 504.63
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
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[1].
In Vitro: GNE-477 (Compound 8) has improved potency in the MCF7.1 cell proliferation assay with an EC50 of 143 nM[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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