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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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Elacytarabine (also known as CP 4055; CP-4055), an antineoplastic drug, is a lipid-conjugated (5'-elaidic acid ester) derivative and a prodrug of the nucleoside analog cytarabine (arabinoside; Ara-C). Elacytarabine exhibits antitumor properties. As a prodrug, CP-4055 is intracellularly converted by deoxycytidine kinase into cytarabine triphosphate, which then inhibits DNA synthesis by competing with cytidine for DNA incorporation. When CP-4055 is compared to cytarabine, it exhibits higher absorption and retention in cells, which leads to higher activation of cytarabine triphosphate by deoxycytidine kinase, lower deamination and deactivation by deoxycytidine deaminase, and higher inhibition of DNA synthesis. In addition to inhibiting RNA synthesis, this agent has an effect that cytarabine does not.
Molecular Formula |
C27H45N3O6
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Molecular Weight |
507.6627
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Exact Mass |
507.33
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CAS # |
188181-42-2
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Appearance |
Powder
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SMILES |
CCCCCCCC/C=C/CCCCCCCC(=O)OC[C@@H]1[C@H]([C@@H]([C@@H](O1)N2C=CC(=NC2=O)N)O)O
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InChi Key |
FLFGNMFWNBOBGE-FNNZEKJRSA-N
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InChi Code |
InChI=1S/C27H45N3O6/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-23(31)35-20-21-24(32)25(33)26(36-21)30-19-18-22(28)29-27(30)34/h9-10,18-19,21,24-26,32-33H,2-8,11-17,20H2,1H3,(H2,28,29,34)/b10-9+/t21-,24-,25+,26-/m1/s1
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Chemical Name |
[(2R,3S,4S,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl (E)-octadec-9-enoate
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Synonyms |
Elacytarabine; CP 4055
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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 |
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) |
DMSO: ~125 mg/mL (~246.2 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.10 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 20.8 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: ≥ 2.08 mg/mL (4.10 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 20.8 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 | 1.9698 mL | 9.8491 mL | 19.6982 mL | |
5 mM | 0.3940 mL | 1.9698 mL | 3.9396 mL | |
10 mM | 0.1970 mL | 0.9849 mL | 1.9698 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00405743 | Completed | Drug: CP-4055 | Hematologic Malignancies AML |
Clavis Pharma | May 2006 | Phase 1 Phase 2 |
NCT00498407 | Completed | Drug: CP-4055 | Advanced Colorectal Cancer Colorectal Cancer |
Clavis Pharma | May 2007 | Phase 2 |
NCT00831636 | Completed | Drug: CP-4055 | Ovarian Cancer | Clavis Pharma | April 2008 | Phase 1 Phase 2 |
NCT00498836 | Completed | Drug: CP-4055 Drug: Sorafenib (Nexavar) |
Malignant Melanoma | Clavis Pharma | March 2007 | Phase 2 |
NCT00232726 | Completed | Drug: CP-4055 (ELACYT) |
Malignant Melanoma Neoplasm Metastasis |
Clavis Pharma | September 2005 | Phase 2 |