GNE 477


CAS No. : 1032754-81-6

GNE 477,1032754-81-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000194
Synonyms:5-(7-methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine
Molecular Formula:C₂₁H₂₈N₈O₃S₂
Molecular Weight:504.63
Target:mTOR
IC50:4 nM(PI3Kα); 21 nM(mTOR, Kiapp)
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Cat No:I000194
Cas No:1032754-81-6
Product-Name:GNE 477
MDL No:MFCD20527726
InChI:InChI=1S/C21H28N8O3S2/c1-14-16(13-27-3-5-29(6-4-27)34(2,30)31)33-18-17(14)25-19(15-11-23-21(22)24-12-15)26-20(18)28-7-9-32-10-8-28/h11-12H,3-10,13H2,1-2H3,(H2,22,23,24)
InChIKey:AKKCGLXULFRAET-UHFFFAOYSA-N
SMILES:CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)S(=O)(=O)C

GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
IC50 value: 4 nM(PI3Kα); 21 nM(mTOR, Kiapp)
Target: PI3K/mTOR inhibitor
GNE-477 is a potent dual PI3K/mTOR inhibitor that displays desirable pharmacokinetic properties in each of three species studied. GNE-477 also exhibited stasis in a PC3 tumor growth inhibition study.


[1]. Heffron TP, et al. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11.

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