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Quantity Discount Table - Order More To Get More Price Discount
| Quantity | mg | Unit Price ($/mg or $/Unit) | Final Price |
|---|---|---|---|
| 1 | 5 | $60.35 | Total: $301.75 |
| 1 | 10 | $51.12 | Total: $511.20 |
| 1 | 25 | $43.31 | Total: $1,082.75 |
| 1 | 50 | $36.92 | Total: $1,846.00 |
| 1 | 100 | $31.95 | Total: $3,195.00 |
Overview
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 ngmL) and K-Ras (IC50=46 ngmL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow onoff rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ngmL[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 mgkg twice daily and an ED50 for tumor growth inhibition at 28 mgkg[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 ngmL[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.
Chemical Properties
| Molecular Formula | C29H22ClN3O2 |
| Molecular Weight | 479.96 |
| CAS Numbers | 1190094-64-4 |
| Solubility | DMSO |
| Purity | 98% by HPLC |
| SMILES Code | Cn1cncc1[C@@](O)(c1ccc(Cl)cc1)c1ccc2n(C)c(=O)cc(-c3cccc(c3)C#C)c2c1 |
Storage and Handling
0C Short Term, -20C Long Term
References
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.