Antibodies
Cytarabine
- 貨號 Cat. No.
- S1648
- 規格 Size
- 50mg
- 品牌 Brand
- Selleckchem
Description
Cytarabine
Catalog No.S1648
Cytarabine (Cytosine arabinoside, AraC) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Cytarabine (Cytosine arabinoside, AraC) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. | |||||
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| Targets | DNA synthesis | |||||
| IC50 | ||||||
| In vitro | Cytarabine (AraC) is phosphorylated into a triphosphate form (Ara-CTP) involving deoxycytidine kinase (dCK), which competes with dCTP for incorporation into DNA, and then blocks DNA synthesis by inhibiting the function of DNA and RNA polymerases. Cytarabine displays a higher growth inhibitory activity towards wild-type CCRF-CEM cells compared to other acute myelogenous leukemia (AML) cells with IC50 of 16 nM. [1] Increasing concentrations of Cytarabine (IC50 of 0.69 μM) results in decreased metabolic activity of sensitive rat leukemic cell line RO/1, and the cell toxity can be highly enhanced by transfection with human wt dCK (IC50 of 0.037 μM) but not the inactive, alternatively spliced dCK forms. [2] Cytarabine apparently induces apoptosis of rat sympathetic neurons at 10 μM, of which 100 μM shows the highest toxicity and kills over 80% of the neurons by 84 hours, involving the release of mitochondrial cytochrome-c and the activation of caspase-3, and the toxicity can be attenuated by p53 knockdown and delayed by bax deletion. [3] | |||||
| In vivo | Cytarabine is highly effective against acute leukaemias, which causes the characteristic G1/S blockage and synchronization, and increases the survival time for leukaemic Brown Norway rats in a weak dose-related fashion indicating that the use of higher dosages of Cytarabine does not contribute to its antileukaemic effectiveness in man. [4] Cytarabine (250 mg/kg) also causes placental growth retardation and increases placental trophoblastic cells apoptosis in the placental labyrinth zone of the pregnant Slc:Wistar rats, which increases from 3 hour after the treatment and peaks at 6 hour before returning to control levels at 48 hour, with remarkably enhanced p53 protein, p53 trancriptional target genes such as p21, cyclinG1 and fas and caspase-3 activity. [5] | |||||
| Features | The 1st of a series of cancer drugs that alters the sugar component of nucleosides. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| In Vitro Growth Inhibition Assay | Stock solution of Cytarabine is prepared in absolute ethanol, and serial dilutions of Cytarabine are prepared. CCRF-CEM cells are suspended in RPMI medium supplemented with 10% FBS, 0.1% gentamicin, and 1% sodium pyruvate. The cells are suspended in their respective media to give 10 mL volumes of cell suspension at a final density of 3-6 × 104 cells/mL. Appropriate volumes of Cytarabine solution are transferred to the cell suspensions, and incubation is continued for 72 hours. The cells are spun down and resuspended in fresh Cytarabine -free medium, and final cell counts are determined. The data are analyzed by sigmoidal curve fitting of the cell count versus Cytarabine concentration, and the results are expressed as the IC50 (Cytarabine concentration that inhibits cell growth to 50% of the control value). |
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Cell Assay: [2]
| Cell lines | Rat leukemic cell lines RCL/0, RO/1 and K7 and human myelomonocytic leukemic U937 |
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| Concentrations | ~100 μM |
| Incubation Time | 24, 48 and 72 hours |
| Method | Cells are incubated in the presence of different concentrations of Cytarabine at 37 °C for 24, 48, and 72 hours. At the time of 20-, 44-, or 68-hour incubation in the presence of Cytarabine, 10 mL of cell proliferation reagent WST-1 solution is added. After 2- and 4-hour incubation with WST-1, cell metabolic activity is assessed with colorimetric changes quantified by measuring the absorbance in a spectrophotometer at 450 nm. And cell division times are calculated from eosin counting in parallel with viability assay |
Animal Study: [4]
| Animal Models | Brown Norway rat with myelocytic leukaemia |
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| Dosages | 5 - 1000 mg/kg |
| Administration | Injection i.v. |
| Solubility | Saline, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01956812 | Not yet recruiting | Metastatic Pancreatic Cancer|Pancreatic Cancer | Immunomedics, Inc. | 2013-12 | Phase 3 |
| NCT01830322 | Withdrawn | Metastatic Pancreatic Adenocarcinoma | Cornerstone Pharmaceuticals, Inc. | 2014-01 | Phase 2 |
| NCT02016417 | Not yet recruiting | Nasopharyngeal Carcinoma | Cancer Hospital of Guangxi Medical University | 2014-01 | Phase 2 |
| NCT01964430 | Not yet recruiting | Pancreatic Neoplasms|Digestive System Neoplasms|Neoplasms by Site|Neoplasms|Endocrine Gland Neoplasms|Pancreatic Diseases|Digestive System Diseases|Endocrine System Diseases|Gemcitabine|Antimetabolite | Celgene Corporation | 2014-01 | Phase 3 |
| NCT01852890 | Not yet recruiting | Pancreatic Neoplasms | University of Iowa|Joseph J. Cullen | 2014-02 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 243.22 |
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| Formula | C9H13N3O5 |
| CAS No. | 147-94-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 1 mg/mL (4 mM) |
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| Water | 48 mg/mL (197 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 4-amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one |
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