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GNE-477 CAS: 1032754-81-6

Category: Inhibitors
Product Name: GNE-477
Cat No: I000194
CAS No: 1032754-81-6
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
SMILES: O=S(N1CCN(CC2=C(C)C3=NC(C4=CN=C(N)N=C4)=NC(N5CCOCC5)=C3S2)CC1)(C)=O
Solubility: DMSO: < 9.2 mg/mL
Target: mTOR
IC50: 4 nM(PI3Kα); 21 nM(mTOR, Kiapp)
Storage: Desiccate at -20°C
CAS 1032754-81-6,GNE-477
  • Description

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.

  • References


[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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