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Cytarabine

Catalog No. T1272   CAS 147-94-4
Synonyms: Ara-C, Cytosine Arabinoside, Cytosine β-D-arabinofuranoside, Arabinocytidine

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

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Cytarabine Chemical Structure
Cytarabine, CAS 147-94-4
Pack Size Availability Price/USD Quantity
25 mg In stock $ 30.00
50 mg In stock $ 39.00
100 mg In stock $ 53.00
200 mg In stock $ 67.00
500 mg In stock $ 93.00
1 g In stock $ 110.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 99.93%
Purity: 99.92%
Purity: 99.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.
Targets&IC50 DNA synthesis:16 nM
In vitro METHODS: Primary AML cells were treated with Cytarabine (10-5000 nM) for 24 h. Cell viability was measured using MTT method.
RESULTS: Cytarabine showed a dose-dependent growth inhibitory effect with an IC50 of 1.12 μM. [1]
METHODS: Human histiocytic lymphoma cells U937 were treated with Cytarabine (10-1000 nM) for 72 h, and the cell cycle was detected by Flow Cytometry.
RESULTS: Cytarabine dose-dependently decreased the proportion of cells in G1 phase and increased the proportion of cells in S phase in cells treated with 10 and 100 nM. At the highest dose of 1000 nM, Cytarabine caused a significant increase in the proportion of sub-G1 and G2/M phases. [2]

Translated with DeepL.com (free version)
In vivo METHODS: To study chemotherapy resistance in AML, Cytarabine (10-60 mg/kg) was administered intraperitoneally to NSG mice bearing human AML tumors once daily for five days.
RESULTS: In all mice treated with 60 mg/kg Cytarabine, cytoreduction occurred at 2 weeks post-treatment and relapsed 4-13 weeks post-treatment. There was a dose-response relationship in the model in terms of minimum leukemia burden and time to peripheral blood relapse. [3]
METHODS: To assay antitumor activity in vivo, Cytarabine (6.25 mg/kg once daily) and sorafenib (60 mg/kg twice daily) were administered intraperitoneally to a NOD-SCID-IL2R γnull mouse model harboring the human AML tumor U937 once weekly or for forty-eight days.
RESULTS: Cytarabine in combination with sorafenib produced potent anti-AML activity in vivo. [4]

Translated with DeepL.com (free version)
Kinase Assay 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).
Cell Research 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(Only for Reference)
Synonyms Ara-C, Cytosine Arabinoside, Cytosine β-D-arabinofuranoside, Arabinocytidine
Molecular Weight 243.22
Formula C9H13N3O5
CAS No. 147-94-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (226.13 mM)

H2O: 24.3 mg/mL (100 mM)

TargetMolReferences and Literature

1. Desai UN, et al. Enhancement of the cytotoxic effects of Cytarabine in synergism with Hesperidine and Silibinin in Acute Myeloid Leukemia: An in-vitro approach. J Cancer Res Ther. 2015 Apr-Jun;11(2):352-7. 2. Tomic B, et al. Cytarabine-induced differentiation of AML cells depends on Chk1 activation and shares the mechanism with inhibitors of DHODH and pyrimidine synthesis. Sci Rep. 2022 Jul 5;12(1):11344. 3. Robin L. Perry,et al. Ara-C Treatment of Acute Myeloid Leukemia Does Not Lead to Prolonged Enrichment of Stem Cells or a Cell Cycle Arrest. Blood. 2010; 116(21):2178. 4. Hu S, et al. Activity of the multikinase inhibitor sorafenib in combination with cytarabine in acute myeloid leukemia. J Natl Cancer Inst. 2011 Jun 8;103(11):893-905. 5. Yamauchi H, et al. Biol Reprod, 2004, 70(6), 1762-1767. 6. Shepshelovich D, et al. Pharmacodynamics of cytarabine induced leucopenia: a retrospective cohort study. Br J Clin Pharmacol. 2015 Apr;79(4):685-91. 7. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931

TargetMolCitations

1. He S, Li Y, Shi X, et al.DNA methylation landscape reveals LIN7A as a decitabine-responsive marker in patients with t (8; 21) acute myeloid leukemia.Clinical Epigenetics.2023, 15(1): 1-13. 2. Islam S, Rahaman M H, Yu M, et al.Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition.Cancers.2023, 15(4): 1044. 3. Zhao Y, Zhao N, Cai Y, et al.An algal lectin griffithsin inhibits Hantaan virus infection in vitro and in vivo.Frontiers in Cellular and Infection Microbiology.2022, 12: 1813. 4. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931 5. Wang B, He B S, Ruan X L, et al. An integrated microfluidics platform with high-throughput single-cell cloning array and concentration gradient generator for efficient cancer drug effect screening. Military Medical Research. 2022, 9(1): 1-17. 6. Wang B, Pei J, Zhang H, et al.Dihydropyridine-derived calcium channel blocker as a promising anti-hantavirus entry inhibitor.Interventions for emerging infectious diseases.2023, 16648714. 7. He S, Li Y, Wang L, et al.DNA methylation landscape reveals GNAS as a decitabine-responsive marker in patients with acute myeloid leukemia.Neoplasia.2024, 49: 100965.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Traditional Chinese Medicine Monomer Library Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library Cancer Cell Differentiation Compound Library Human Metabolite Library

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Keywords

Cytarabine 147-94-4 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Microbiology/Virology Endogenous Metabolite DNA/RNA Synthesis Nucleoside Antimetabolite/Analog HSV Herpes simplex virus Orthopoxvirus Cytosine b-D-arabinofuranoside Cytosine beta-D-arabinofuranoside Ara-C Cytosine Arabinoside inhibit Cytosine β-D-arabinofuranoside Inhibitor Arabinocytidine inhibitor

 

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