OSI-027

OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively[1][2].

Product Specifications

CAS Number

[936890-98-1]

Product Name Alternative

ASP7486

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; mTOR

Type

Reference compound

Related Pathways

Autophagy; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/OSI-027.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@H]1CC[C@H](C2=NC(C(N3)=CC4=C3C(OC)=CC=C4)=C5C(N)=NC=NN52)CC1)O

Molecular Formula

C21H22N6O3

Molecular Weight

406.44

Precautions

H302, H315, H319, H335

References & Citations

[1]Falcon BL, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71 (5) :1573-83.|[2]Zhi X, et al. OSI-027 modulates acute graft-versus-host disease after liver transplantation in a rat model. Liver Transpl. 2017 Sep;23 (9) :1186-1198.|[3]Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2 (12) :1944-56.|[4]Mateo J, et al. A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies. Br J Cancer. 2016;114 (8) :889-896.