bs-60113C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 406.44

Formula: C21 H22 N6 O3

CAS Number: 936890-98-1

InChi Key: JROFGZPOBKIAEW-HAQNSBGRSA-N

InChi: InChI=1S/C21H22N6O3/c1-30-15-4-2-3-13-9-14(25-16(13)15)17-18-19(22)23-10-24-27(18)20(26-17)11-5-7-12(8-6-11)21(28)29/h2-4,9-12,25H,5-8H2,1H3,(H,28,29)(H2,22,23,24)/t11-,12-

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

Purity: 98.0

Solubility: DMSO up to 50 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

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 PI3Kα, PI3Kβ, PI3Kγ, 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.