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CP-609754
🥰Excellent
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
🥰Excellent
Purity: 99.86%
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $50 | In Stock | |
| 5 mg | $118 | In Stock | |
| 10 mg | $197 | In Stock | |
| 25 mg | $335 | In Stock | |
| 50 mg | $473 | In Stock | |
| 100 mg | $672 | In Stock | |
| 200 mg | $885 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $136 | In Stock |
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Purity:99.86%
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Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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