Cytarabine

Catalog No.S1648 Batch:S164808

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Technical Data

Formula

C9H13N3O5

Molecular Weight 243.22 CAS No. 147-94-4
Solubility (25°C)* In vitro DMSO 49 mg/mL (201.46 mM)
Water 49 mg/mL (201.46 mM)
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Targets
DNA synthesis [1]
(CCRF-CEM cells)
16 nM
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 (from 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).

Cell Assay:

[2]

  • Cell lines

    Rat leukemic cell lines RCL/0, RO/1 and K7 and human myelomonocytic leukemic U937

  • 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

  • Dosages

    5 - 1000 mg/kg

  • Administration

    Injection i.v.

Customer Product Validation

Data from [Data independently produced by , , Leukemia, 2015, 29(8): 1702–1712]

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2017, 36(1):22]

Data from [Data independently produced by , , J Pharmacol Exp Ther, 2014, 350(3): 646-56]

Selleck's Cytarabine has been cited by 94 publications

EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] PubMed: 38155773
ULK2 Is a Key Pro-Autophagy Protein That Contributes to the High Chemoresistance and Disease Relapse in FLT3-Mutated Acute Myeloid Leukemia [ Int J Mol Sci, 2024, 25(1)646] PubMed: 38203816
Mitocurcumin utilizes oxidative stress to upregulate JNK/p38 signaling and overcomes Cytarabine resistance in acute myeloid leukemia [ Cell Signal, 2024, 114:111004] PubMed: 38048856
The ESCRT protein CHMP5 promotes T cell leukemia by controlling BRD4-p300-dependent transcription [ bioRxiv, 2024, 2024.01.29.577409] PubMed: 38352301
iPSC-derived reactive astrocytes from patients with multiple sclerosis protect cocultured neurons in inflammatory conditions [ J Clin Invest, 2023, 133(13)e164637] PubMed: 37219933
Posttranslational splicing modifications as a key mechanism in cytarabine resistance in acute myeloid leukemia [ Leukemia, 2023, 37(8):1649-1659] PubMed: 37422594
Co-targeting BCL-XL and BCL-2 by PROTAC 753B eliminates leukemia cells and enhances efficacy of chemotherapy by targeting senescent cells [ Haematologica, 2023, 108(10):2626-2638] PubMed: 37078252
Spermatogenesis associated serine rich 2 like plays a prognostic factor and therapeutic target in acute myeloid leukemia by regulating the JAK2/STAT3/STAT5 axis [ J Transl Med, 2023, 21(1):115] PubMed: 36774517
The role of m6A demethylase FTO in chemotherapy resistance mediating acute myeloid leukemia relapse [ Cell Death Discov, 2023, 9(1):225] PubMed: 37402730
The role of m6A demethylase FTO in chemotherapy resistance mediating acute myeloid leukemia relapse [ Cell Death Discov, 2023, 9(1):225] PubMed: 37402730

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SHIPPING AND STORAGE
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