CP-609754(OSI754)|CAS 1190094-64-4|DC Chemicals

Cas No.:	1190094-64-4
Chemical Name:	6-[(R)-(4-chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]-4-(3-ethynylphenyl)-1-methylquinolin-2-one
Synonyms:	CP-609754; CP609754; CP 609754; LNK 754; OSI 754
SMILES:	O=C1C=C(C2C=C(C#C)C=CC=2)C2C=C(C=CC=2N1C)[C@@](C1N(C)C=NC=1)(C1C=CC(Cl)=CC=1)O
Formula:	C₂₉H₂₂ClN₃O₂
M.Wt:	479.96
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	1: Moulder SL, Mahany JJ, Lush R, Rocha-Lima C, Langevin M, Ferrante KJ, Bartkowski LM, Kajiji SM, Noe DA, Paillet S, Sullivan DM. A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors. Clin Cancer Res. 2004 Nov 1;10(21):7127-35. PubMed PMID: 15534083.

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].
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].
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].
References:	[1]. Stacy L Moulder, et al. A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors. Clin Cancer Res. 2004 Nov 1;10(21):7127-35.

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