GNE-477 - CAS 1032754-81-6
Catalog number:
1032754-81-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H28N8O3S2
Molecular Weight:
504.63
COA:
Inquire
Targets:
mTOR
Description:
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.
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Purity:
>98%
MSDS:
Inquire
1.Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP1, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046. Epub 2010 Mar 12.
Efforts to identify potent small molecule inhibitors of PI3 kinase and mTOR led to the discovery of the exceptionally potent 6-aryl morpholino thienopyrimidine 6. In an effort to reduce the melting point in analogs of 6, the thienopyrimidine was modified by the addition of a methyl group to disrupt planarity. This modification resulted in a general improvement in in vivo clearance. This discovery led to the identification of GNE-477 (8), a potent and efficacious dual PI3K/mTOR inhibitor.
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CAS 1032754-81-6 GNE-477

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