| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H22N6O3 |
| Molecular Weight | 406.4378 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=CC2=C1NC(=C2)C3=C4N(N=CN=C4N)C(=N3)[C@H]5CC[C@@H](CC5)C(O)=O
InChI
InChIKey=JROFGZPOBKIAEW-HAQNSBGRSA-N
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-
| Molecular Formula | C21H22N6O3 |
| Molecular Weight | 406.4378 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
OSI-027 is an orally bioavailable mammalian inhibitor of mTOR kinase and has antineoplastic activity. OSI-027 binds to and inhibits of the catalytic site of mTOR, which is a central part of two protein complexes, mTORC1 and mTORC2, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. OSI-027 is in phase I clinical trial for the investigation on patients with advanced solid tumors or lymphoma.
Originator
Approval Year
Cmax
AUC
Sourcing
PubMed
Patents
Sample Use Guides
OSI-027 downregulated multidrug resistance (MDR)-1, which has been implicated in chemotherapy resistance in pancreatic ductal adenocarcinoma (PDAC) cells and enhanced apoptosis induced by gemcitabine in the three PDAC cell lines. Human PDAC cell lines (Panc-1, BxPC-3, CFPAC-1) were plated at a density of 3000 cells per well in 96-well plates and the media was removed and replaced by serum free media. 24 hours later the serum free media was replaced by complete media with the addition of OSI-027 at concentration 1.25, 2.5, 5, 10, 20, 40, and 80 μM for at 24, 48, and 72 hours.
