Description
OSI-027 can inhibit mTORC1, mTORC2 and mTOR with IC50 of 22 nM, 65 nM and 4 nM.
Storage
2 years at -20centigrade Powder
Targets
mTORC1, mTORC2, mTOR
Molecular Formula
C21H22N6O3
Chemical Name
(1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[1,5-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid
Solubility
DMSO 18 mg/mL, Water
In vitro
OSI-027 is a potent, selective small molecule inhibitor of the catalytic site of mTOR, targeting both mTORC1 and mTORC2. OSI-027 can inhibit mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM. OSI-027 can inhibit phosphorylation of AKT at S473 and T308 in a concentration-dependent manner in BT-474 and IGR-OV1 cells under normal culture conditions and in MDA-MB-231 cells upon insulin stimulation..OSI-027 potently inhibits proliferation and induces apoptosis in cells expressing the T315I-BCR-ABL mutation. OSI-027 can dose-dependently attenuate Akt phosphorylation at the mTORC2-specific Ser473 site and the downstream substrate of Akt, PRAS40.
In vivo
Treated with OSI-027 in GEO colorectal xenograft model, OSI-027 (65 mg/kg) inhibited both mTORC1 and mTORC2 effectors. After 2 hours, decreased 4E-BP1, Akt, and S6 phosphorylation was observed and inhibition of S6 andAkt was sustained for 24 hours.
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