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CP-609754
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Catalog No. T38050Cas No. 1190094-64-4
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng/mL) and K-Ras (IC50=46 ng/mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on/off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng/mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg/kg twice daily and an ED50 for tumor growth inhibition at 28 mg/kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng/mL[1].
[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.
CP-609754
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Purity: 99.87%
Catalog No. T38050Cas No. 1190094-64-4
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng/mL) and K-Ras (IC50=46 ng/mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on/off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng/mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg/kg twice daily and an ED50 for tumor growth inhibition at 28 mg/kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng/mL[1].
[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.
[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.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $50 | In Stock | In Stock | |
| 5 mg | $118 | In Stock | In Stock | |
| 10 mg | $197 | In Stock | In Stock | |
| 25 mg | $335 | In Stock | In Stock | |
| 50 mg | $473 | In Stock | In Stock | |
| 100 mg | $672 | In Stock | In Stock | |
| 200 mg | $885 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $136 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.87%
Appearance:Solid
Color:White
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng/mL) and K-Ras (IC50=46 ng/mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on/off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng/mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg/kg twice daily and an ED50 for tumor growth inhibition at 28 mg/kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng/mL[1]. [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. |
| 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 |
| Smiles | Cn1cncc1[C@@](O)(c1ccc(Cl)cc1)c1ccc2n(C)c(=O)cc(-c3cccc(c3)C#C)c2c1 |
| Relative Density. | 1.23 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (208.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.33 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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