Details
Stereochemistry | ACHIRAL |
Molecular Formula | C28H27N7O |
Molecular Weight | 477.5603 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)CN1C2=C(C=C(NC3=NC=CC=N3)C=C2)C4=C1C5=C(C6=CN(C)N=C6CC5)C7=C4CNC7=O
InChI
InChIKey=AEULIVPVIDOLIN-UHFFFAOYSA-N
InChI=1S/C28H27N7O/c1-15(2)13-35-22-8-5-16(32-28-29-9-4-10-30-28)11-18(22)24-19-12-31-27(36)25(19)23-17(26(24)35)6-7-21-20(23)14-34(3)33-21/h4-5,8-11,14-15H,6-7,12-13H2,1-3H3,(H,31,36)(H,29,30,32)
CEP-11981 is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR) and Tie2 receptor tyrosine kinases with potential antiangiogenic and antineoplastic activities. Preclinical studies have shown that CEP-11981 exhibits promising permeability, metabolic stability, and pharmacokinetic properties across multiple species. Studies of pharmacologic activity across angiogenesis assays, animal tumor models, and human tumor models have shown sustained, dose-related antiangiogenic and antitumor inhibition. In clinical trals CEP-11981 administration leads to disease stabilization in patients with recurrent or refractory solid tumors. Despite acceptable tolerability of CEP-11981 at the MTD, further development by the sponsor has ceased.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25152243
CEP-11981 was tolerated at doses between 3.0 and 97.4 mg/m2.
Route of Administration:
Intravenous
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856691-93-5
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CHEMBL2010872
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J8AY0Z4CBP
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11751922
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DTXSID80234942
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admin on Sat Dec 16 01:57:25 GMT 2023 , Edited by admin on Sat Dec 16 01:57:25 GMT 2023
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C82379
Created by
admin on Sat Dec 16 01:57:25 GMT 2023 , Edited by admin on Sat Dec 16 01:57:25 GMT 2023
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)