| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
OSI754 (also known as CP-609754, CP-609,754, LNK-754) is a novel and potent farnesyltransferase inhibitor (TFI) that has potential anticancer activity. Since farnesyltransferase is known to prevent proper functioning of Ras, a family of proteins often abnormally activated in cancer, FTIs were first developed as potential anticancer agents. A number of FTIs underwent preclinical testing but were found to have major side effects, while others entered clinical development in a variety of cancers, only to be discontinued at phase I due to a lack of efficacy.
| ln Vitro |
Reversible farnesyl growth enzyme kinase with a slow on/off rate is CP-609754 (CP-609,754). The analysis of compounds tagged with [35S]methionine using SDS-PAGE [1] indicates that CP-609754 is competitive for the isoprene receptor (H-Ras protein), but not for the isoprene donor farnesyl PPI. When it comes to binding to Ras protein, CP-609754 reacts to and competes with the farnesyltransferase-farnesylPPI complex. In 3T3 transfectants, CP-609754 specifically prevents the farnesylation of H- and K-Ras proteins [1].
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| ln Vivo |
In vivo activity of CP-609754 (CP-609,754) against 3T3 H-ras (61L) cancers has been reported [1]. Tumor suppression was achieved by continuous intraperitoneal infusion of CP-609754; tumor growth inhibition was >50%, tumor farnesyl transcriptase activity was inhibited >30%, and CP-609754 tumor growth concentration remains above 118 ng/mL. Tumor regression reached a dose of 100 mg/kg when CP-609754 was applied twice a day to the side wall [1].
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| References | |
| Additional Infomation |
LNK 754 has been investigated in Mild Alzheimer's Disease.
CP-609,754 is a quinolinone derivative that inhibits farnesyl protein transferase, an enzyme that mediates the farnesylation of RAS, causing possible inhibition of the RAS pathway. |
| Molecular Formula |
C29H22CLN3O2
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| Molecular Weight |
479.96
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| Exact Mass |
479.14
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| CAS # |
1190094-64-4
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| Related CAS # |
(Rac)-CP-609754;439153-64-7
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| PubChem CID |
46208720
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.23±0.1 g/cm3
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| Boiling Point |
702.4±60.0 °C
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| LogP |
4.857
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
874
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1C=NC=C1[C@@](C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC=CC(=C5)C#C)C)O
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| InChi Key |
JAHDAIPFBPPQHQ-GDLZYMKVSA-N
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| InChi Code |
InChI=1S/C29H22ClN3O2/c1-4-19-6-5-7-20(14-19)24-16-28(34)33(3)26-13-10-22(15-25(24)26)29(35,27-17-31-18-32(27)2)21-8-11-23(30)12-9-21/h1,5-18,35H,2-3H3/t29-/m1/s1
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0835 mL | 10.4175 mL | 20.8351 mL | |
| 5 mM | 0.4167 mL | 2.0835 mL | 4.1670 mL | |
| 10 mM | 0.2084 mL | 1.0418 mL | 2.0835 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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