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CP-609754

Catalog No. T38050 CAS 1190094-64-4

CP-609754 shows selective inhibition of farnesyltransferase.

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CP-609754, CAS 1190094-64-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 84.00
5 mg	In stock	$ 197.00
10 mg	In stock	$ 328.00
25 mg	In stock	$ 558.00
50 mg	In stock	$ 788.00
100 mg	In stock	$ 1,120.00
500 mg	In stock	$ 2,230.00
1 mL * 10 mM (in DMSO)	In stock	$ 226.00

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Purity: 99.04%

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Description	CP-609754 shows selective inhibition of farnesyltransferase.
Targets&IC50	Farnesylation:1.72 ng/mL
In vitro	CP-609754 (CP-609,754) serves as a reversible farnesyltransferase inhibitor, characterized by a slow on/off rate, effectively inhibiting the farnesylation of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with an IC50 of 1.72 ng/mL, as evidenced by SDS-PAGE analysis of [35S]methionine-labeled material[1]. The compound exhibits competitive inhibition toward the prenyl acceptor (H-Ras protein) while being noncompetitive relative to the prenyl donor, farnesyl PPI. It operates by engaging with the farnesyltransferase-farnesyl PPI complex and vying for H-Ras protein binding, demonstrating selective inhibition of both H- and K-Ras proteins' farnesylation in 3T3 transfectants[1].
In vivo	CP-609754 exhibits antitumor activity in vivo against 3T3 H-ras (61L) tumors. Administration of CP-609754 orally twice daily leads to tumor regression at a dose of 100 mg/kg, and the effective dose for inhibiting 50% of tumor growth (ED50) is 28 mg/kg. Continuous intraperitoneal (i.p.) infusion of CP-609754 results in over 50% inhibition of tumor growth and more than 30% reduction in tumor farnesyltransferase activity in mice, provided the plasma concentration of CP-609754 remains above 118 ng/mL[1].

Molecular Weight	479.96
Formula	C29H22ClN3O2
CAS No.	1190094-64-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (208.35 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Clinical Compound Library Metabolism Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

CP-609754 1190094-64-4 Metabolism Transferase Malignant farnesylation Farnesyltransferase Tumor Inhibitor LNK-754 CP 609754 H-Ras Ftase OSI 754 Farnesyl Transferase LNK 754 OSI-754 inhibit OSI754 LNK754 K-Ras Advanced CP609754 inhibitor

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