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Details

Stereochemistry ACHIRAL
Molecular Formula C28H27N7O
Molecular Weight 477.5613
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CEP-11981

SMILES

CC(C)Cn1c2ccc(cc2c3c4CNC(=O)c4c-5c(CCc6c5cn(C)n6)c31)Nc7ncccn7

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)

HIDE SMILES / InChI

Molecular Formula C28H27N7O
Molecular Weight 477.5613
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

PubMed

PubMed

TitleDatePubMed
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
2012 Jan 26
Patents

Sample Use Guides

CEP-11981 was tolerated at doses between 3.0 and 97.4 mg/m2.
Route of Administration: Intravenous
Substance Class Chemical
Created
by admin
on Sat Jun 26 16:34:22 UTC 2021
Edited
by admin
on Sat Jun 26 16:34:22 UTC 2021
Record UNII
J8AY0Z4CBP
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CEP-11981
Code English
BOL-303213X
Code English
4H-INDAZOLO(5,4-A)PYRROLO(3,4-C)CARBAZOL-4-ONE, 2,5,6,11,12,13-HEXAHYDRO-2-METHYL-11-(2-METHYLPROPYL)-8-(2-PYRIMIDINYLAMINO)-
Systematic Name English
Code System Code Type Description
CAS
856691-93-5
Created by admin on Sat Jun 26 16:34:22 UTC 2021 , Edited by admin on Sat Jun 26 16:34:22 UTC 2021
PRIMARY
ChEMBL
CHEMBL2010872
Created by admin on Sat Jun 26 16:34:22 UTC 2021 , Edited by admin on Sat Jun 26 16:34:22 UTC 2021
PRIMARY
FDA UNII
J8AY0Z4CBP
Created by admin on Sat Jun 26 16:34:22 UTC 2021 , Edited by admin on Sat Jun 26 16:34:22 UTC 2021
PRIMARY
PUBCHEM
11751922
Created by admin on Sat Jun 26 16:34:22 UTC 2021 , Edited by admin on Sat Jun 26 16:34:22 UTC 2021
PRIMARY
EPA CompTox
856691-93-5
Created by admin on Sat Jun 26 16:34:22 UTC 2021 , Edited by admin on Sat Jun 26 16:34:22 UTC 2021
PRIMARY
NCI_THESAURUS
C82379
Created by admin on Sat Jun 26 16:34:22 UTC 2021 , Edited by admin on Sat Jun 26 16:34:22 UTC 2021
PRIMARY
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