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
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
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 05:13:11 GMT 2023
by
admin
on
Sat Dec 16 05:13:11 GMT 2023
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Record UNII |
L0S47W9GPY
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Record Status |
Validated (UNII)
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Record Version |
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C2020
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1190094-64-4
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L0S47W9GPY
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DB12640
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DTXSID40152294
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C2551
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