| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 5g |
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Purity: ≥98%
Cytarabine (formerly Ara-C; MK-8242; SCH-900242; SCH900242; MK8242; AC-1075; CHX 3311; Arabitin; Aracytidine), a pyrimidine nucleoside analog approved for cancer treatment, is an antimetabolite anticancer drug used mainly for treating leukemia. In wild-type CCRF-CEM cells, it inhibits DNA synthesis with an IC50 of 16 nM, giving it additional antiviral and immunosuppressive qualities.
| Targets |
Microbial Metabolite; HSV-1
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| ln Vitro |
Cytarabine (AraC) is phosphorylated into a triphosphate form (Ara-CTP) by deoxycytidine kinase (dCK), which inhibits the activity of DNA and RNA polymerases to prevent DNA synthesis by competing with dCTP for incorporation into DNA. With an IC50 of 16 nM, cytarabine exhibits a greater growth inhibitory activity against wild-type CCRF-CEM cells than against other acute myelogenous leukemia (AML) cells.[1] The metabolic activity of the sensitive rat leukemic cell line RO/1 decreases with increasing concentrations of cytarabine (IC50 of 0.69 μM). Transfection with human wt dCK (IC50 of 0.037 μM) can greatly increase the cell toxity, but not the inactive, alternatively spliced dCK forms.[2] Rat sympathetic neurons appear to undergo apoptosis when exposed to cytarabine at concentrations of up to 10 μM. The highest toxicity of cytarabine is at 100 μM, which results in the death of over 80% of the neurons in 84 hours through the activation of caspase-3 and the release of mitochondrial cytochrome-c. The toxicity can be mitigated by p53 knockdown and postponed by bax deletion.[3]
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| Enzyme Assay |
Cytarabine is prepared in absolute ethanol as a stock solution, and Cytarabine is prepared in serial dilutions. The RPMI medium containing 10% FBS, 0.1% gentamicin, and 1% sodium pyruvate is supplemented with CCRF-CEM cells. To achieve a final density of 3-6 × 104 cells/mL, the cells are suspended in their respective media to yield 10 mL volumes of cell suspension. After adding the appropriate amounts of cytarabine solution to the cell suspensions, the incubation process is extended for a full 72 hours. Final cell counts are obtained after the cells are spun down and resuspended in new Cytarabine-free medium. The results are expressed as the IC50, or the concentration of cytarabine that inhibits cell growth to 50% of the control value. The data are analyzed by fitting a sigmoidal curve to the relationship between the cell count and cytarabine concentration.
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| Cell Assay |
Different concentrations of cytarabine are incubated with cells for 24, 48, and 72 hours at 37 °C. 10 milliliters of the cell proliferation reagent WST-1 solution are added after the 20-, 44-, or 68-hour incubation period in the presence of cytarabine. Following a 2- or 4-hour incubation period with WST-1, colorimetric alterations are measured by calculating the absorbance at 450 nm in a spectrophotometer to determine the metabolic activity of the cells. Additionally, cell division times are determined by counting eosin in tandem with a viability test.
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| Animal Protocol |
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| References |
| Molecular Formula |
C9H13N3O5
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| Molecular Weight |
243.22
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| Exact Mass |
243.09
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| Elemental Analysis |
C, 44.45; H, 5.39; N, 17.28; O, 32.89
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| CAS # |
147-94-4
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)O
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| InChi Key |
UHDGCWIWMRVCDJ-CCXZUQQUSA-N
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| InChi Code |
InChI=1S/C9H13N3O5/c10-5-1-2-12(9(16)11-5)8-7(15)6(14)4(3-13)17-8/h1-2,4,6-8,13-15H,3H2,(H2,10,11,16)/t4-,6-,7+,8-/m1/s1
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| Chemical Name |
4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1115 mL | 20.5575 mL | 41.1150 mL | |
| 5 mM | 0.8223 mL | 4.1115 mL | 8.2230 mL | |
| 10 mM | 0.4112 mL | 2.0558 mL | 4.1115 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 |
| NCT01593488 | Active Recruiting |
Drug: liposomal cytarabine | Acute Lymphoblastic Leukemia | National Cancer Institute, Naples | March 2012 | Phase 2 |
| NCT03069352 | Active Recruiting |
Drug: Cytarabine Drug: Placebo |
Acute Myeloid Leukemia (AML) | AbbVie | May 23, 2017 | Phase 3 |
| NCT04330820 | Active Recruiting |
Drug: Venetoclax Oral Tablet | Relapsed Adult AML Refractory AML |
Technische Universität Dresden | April 6, 2020 | Phase 1 Phase 2 |
| NCT03623373 | Active Recruiting |
Drug: Cytarabine Drug: Acalabrutinib |
Mantle Cell Lymphoma | Washington University School of Medicine |
November 29, 2018 | Phase 2 |
| NCT02658487 | Active Recruiting |
Drug: Cytarabine Drug: Vosaroxin |
Acute Myeloid Leukemia Myeloid Sarcoma |
Vanderbilt-Ingram Cancer Center | March 2016 | Phase 2 |
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