CP-609754

SKU: orb1303724

Description

CP-609754 is a potent and selective farnesyltransferase inhibitor. It is a valuable research tool for studying Ras protein signaling and has been utilized in both in vitro and in vivo cancer research models to investigate oncogenesis and potential therapeutic strategies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1190094-64-4
• MW: 479.96
• Purity: 99.87% (May vary between batches)
• Formula: C₂₉H₂₂ClN₃O₂
• SMILES: Cn1cncc1[C@@](O)(c1ccc(Cl)cc1)c1ccc2n(C)c(=O)cc(-c3cccc(c3)C#C)c2c1
• Target: Transferase
• Solubility: DMSO:100 mg/mL (208.35 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.33 mM)

Bioactivity

• Target IC50:
  Farnesylation:1.72 ng/mL
• 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.
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Advanced, CP 609754, CP609754, CP-609754, Malignant, H-Ras, Inhibitor, Ftase, Farnesyl Transferase, Farnesyl transferase (FTase), farnesylation, Farnesyltransferase, OSI 754, OSI754, OSI-754, LNK 754, LNK754, LNK-754, K-Ras, inhibit, Tumor

Compound Identifiers

PubChem CID

46208720