OSI-027 --- mTOR Inhibitor [936890-98-1] [936890-98-1]

Bioss

OSI-027 --- mTOR Inhibitor [936890-98-1] [936890-98-1]

16

936890-98-1

Research Use Only

Unconjugated

98 - 98.0

C21 H22 N6 O3

406.44

OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. It shows more than 100-fold selectivity for mTOR relative to PI3Kalpha, PI3Kbeta, PI3Kgamma, and DNA-PK. It inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo. OSI-027 shows robust antitumor activity in several different human xenograft models representing various histologies. In COLO 205 and GEO colon cancer xenograft models, OSI-027 showed superior efficacy compared with rapamycin. OSI-027 is currently in Phase I clinical trials in patients with advanced solid tumors or lymphoma.

COC1C=CC=C2C=C(NC2=1)C1N=C([C@@H]2CC[C@H](CC2)C(O)=O)N2N=CN=C(N)C2=1

-20°C

12161509