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Details

Stereochemistry ABSOLUTE
Molecular Formula C29H22ClN3O2
Molecular Weight 479.957
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CP-609754

SMILES

CN1C=NC=C1[C@@](O)(C2=CC=C(Cl)C=C2)C3=CC4=C(C=C3)N(C)C(=O)C=C4C5=CC=CC(=C5)C#C

InChI

InChIKey=JAHDAIPFBPPQHQ-GDLZYMKVSA-N
InChI=1S/C29H22ClN3O2/c1-4-19-6-5-7-20(14-19)24-16-28(34)33(3)26-13-10-22(15-25(24)26)29(35,27-17-31-18-32(27)2)21-8-11-23(30)12-9-21/h1,5-18,35H,2-3H3/t29-/m1/s1

HIDE SMILES / InChI

Molecular Formula C29H22ClN3O2
Molecular Weight 479.957
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

CP-609754 is a farnesyltransferase inhibitor, originally developed by OSI Pharmaceuticals and Pfizer for the treatment of patients with Ras-positive cancer. CP-609754 demonstrated in vivo antitumor activity against 3T3 H-ras (61L) tumors. The compound was investigated in phase 1 clinical trials in patients with advanced malignant tumors, and dose 640 mg twice per day was established as a recommended for phase 2 clinical trials. The clinical trials, however, were not conducted because of disappointing results of other farnesyl transferase inhibitors, and in 2006 the drug was licensed to Link Medicine for the treatment of neurodegenerative diseases. Under the codename LNK-754, the compound was investigated in mouse models of Parkinson's disease and two models of Alzheimer's disease, where positive results were demonstrated. Two phase 1 clinical trials of LNK-754 in healthy volunteers and patients with mild Alzheimer's disease were conducted in 2009, but no further development of the drug was reported.

Approval Year

Patents

Patents

Substance Class Chemical
Created
by admin
on Sat Dec 16 05:13:11 GMT 2023
Edited
by admin
on Sat Dec 16 05:13:11 GMT 2023
Record UNII
L0S47W9GPY
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CP-609754
Common Name English
2(1H)-QUINOLINONE, 6-((R)-(4-CHLOROPHENYL)HYDROXY(1-METHYL-1H-IMIDAZOL-5-YL)METHYL)-4-(3-ETHYNYLPHENYL)-1-METHYL-
Systematic Name English
CP-609,754
Code English
LNK-754
Code English
OSI-754
Code English
Classification Tree Code System Code
NCI_THESAURUS C2020
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
Code System Code Type Description
PUBCHEM
46208720
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
PRIMARY
CAS
1190094-64-4
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
PRIMARY
FDA UNII
L0S47W9GPY
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
PRIMARY
DRUG BANK
DB12640
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
PRIMARY
EPA CompTox
DTXSID40152294
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
PRIMARY
NCI_THESAURUS
C2551
Created by admin on Sat Dec 16 05:13:11 GMT 2023 , Edited by admin on Sat Dec 16 05:13:11 GMT 2023
PRIMARY