1190094-64-4
1190094-64-4 structure
- Name: CP-609754(OSI754)
- Chemical Name: 6-[(R)-(4-chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]-4-(3-ethynylphenyl)-1-methylquinolin-2-one
- CAS Number: 1190094-64-4
- Molecular Formula: C29H22ClN3O2
- Molecular Weight: 479.95700
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Farnesyl Transferase
- Create Date: 2016-03-02 02:49:25
- Modify Date: 2024-01-02 23:10:40
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CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL[1].
| Name | 6-[(R)-(4-chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]-4-(3-ethynylphenyl)-1-methylquinolin-2-one |
|---|---|
| Synonyms |
unii-l0s47w9gpy
CP-609754(OSI754) |
| Description | CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL[1]. |
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| Related Catalog | |
| In Vitro | CP-609754 (CP-609,754) is a reversible inhibitor of farnesyltransferase with a slow on/off rate. CP-609,754 inhibits farnesylation (IC50=1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with SDS-PAGE analysis of [35S]methionine-labeled material[1]. CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. |
| In Vivo | CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo[1]. With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED50 for tumor growth inhibition is 28 mg/kg[1]. With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL[1]. |
| References |
| Density | 1.23±0.1 g/cm3 |
|---|---|
| Boiling Point | 702.4±60.0 °C |
| Molecular Formula | C29H22ClN3O2 |
| Molecular Weight | 479.95700 |
| Exact Mass | 479.14000 |
| PSA | 60.05000 |
| LogP | 4.85790 |