Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CP-609754 shows selective inhibition of farnesyltransferase.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (208.35 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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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