Cytarabine (Ara-C) is an antineoplastic and antileukemic agent in current clinical treatment. Cytarabine belongs to a class of nucleoside-analogue antimetabolite, which can enter into cells and be phosphorylated by deoxynucleoside salvage pathway and produce their activity by being incorporated into DNA during replication or repair, leading to inhibition of chain extension[1]. Cytarabine, combined with other drugs, is mainly used in the treatment for acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML) and chronic myelogenous leukemia (CML) (see https://www.fda.gov/), also can be used in treatment for other cancer. Cytarabine can inhibit DNA synthesis mainly through being incorporated into cellular DNA by both repair and replication synthesis[2]. Cytarabine can induce apoptosis, s phase arrest, as well as cell growth inhibition[3]. Cytarabine is usually used in long-term neuron culture to reduce glial cells and enhance neurons for its mitotic inhibition[4].
作用机制
Cytarabine, as nucleoside analogue, can inhibit DNA synthesis mainly through being incorporated into cellular DNA by both repair and replication synthesis.
Cytarabine/阿糖胞苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
AML stem and progenitor cells
100 pg/mL
24 h
The combination of IL-21 and cytarabine significantly reduced the colony-forming capacity of AML stem and progenitor cells
Cell Rep Med. 2024 Nov 19;5(11):101826.
MOLM-14 cells
250 nM
48 h
To evaluate the effect of araC on mitochondrial function and protein synthesis in MOLM-14 cells, results showed that araC enhanced mitochondrial membrane potential (MMP) but did not significantly affect protein synthesis.
J Exp Clin Cancer Res. 2022 Dec 9;41(1):340.
ML1 cells
2 μM
48 h
To evaluate the effect of exosomal miR92a on Ara-C resistance in ML1 cells, results showed that exosomal miR92a enhanced Ara-C resistance in ML1 cells.
Biomolecules. 2022 Oct 9;12(10):1448.
SKM1 cells
2 μM
48 h
To evaluate the effect of exosomal miR92a on Ara-C resistance in SKM1 cells, results showed that both high miR92a-Exos and low miR92a-Exos induced Ara-C resistance in SKM1 cells, with high miR92a-Exos having a stronger effect.
Biomolecules. 2022 Oct 9;12(10):1448.
Cytarabine/阿糖胞苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
MLL-AF9 AML model
Intraperitoneal injection
20 mg
Daily, 5 days on, 2 days off
Low-dose IL-21 treatment significantly prolonged the survival of AML mice
Cell Rep Med. 2024 Nov 19;5(11):101826.
NSG mice
MOLM-14 xenograft model
Intraperitoneally
50 mg/kg
Daily for 5 days
To evaluate the effect of araC on the growth of MOLM-14 cells in vivo, results showed that araC did not significantly inhibit the growth of MOLM-14 cells.
J Exp Clin Cancer Res. 2022 Dec 9;41(1):340.
Mice
CYT-induced cachexia model
Intravenous injection
100 mg/kg
Once a day for four consecutive days
To investigate the effect of CYT on energy balance and its role in cachexia, it was found that CYT exacerbates cachexia by inhibiting lipid absorption through increased zipper-like junctions in the lacteals of the small intestine
J Lipid Res. 2023 Jun;64(6):100387
NSG mice
SKM1 cell xenograft model
Intraperitoneal injection
80 mg/kg
3 times per week for 14 days
To evaluate the therapeutic effect of Ara-C on SKM1 cell xenografts. The results showed that the percentage of SKM1 cells in peripheral blood was significantly reduced in mice treated with Ara-C compared to untreated controls
Inhibit the replication of CCRF-CEM cell line in vitro, ED50=5 nM.
1995894
CCRF-CEM cell lines
Function assay
72 h
Concentration required to inhibit replication of CCRF-CEM cell lines by 50% after 72 hr incubation, ED50=6 nM.
1652024
CCRF-CEM human leukemic lymphoblastoid cell lines
Cytotoxic assay
Cytotoxicity against CCRF-CEM human leukemic lymphoblastoid cell lines, IC50=20 nM.
6827546
HeLa human cell lines
Function assay
144 h
The compound was tested in vitro for antitumor activity(50% inhibition of tumor cell growth) against HeLa human cell lines after 144 hr, ID50=0.1 μM
3625714
HL60 cells
Proliferation assay
In vitro inhibitory concentration against proliferation of HL60 cells, IC50=0.08 μM
12877593
human 2209-23 cells
Proliferation assay
Antiproliferative activity against human 2209-23 cells by [3H]thymidine incorporation scintillation proximity assay, IC50=0.029 μM
19055482
human 697 cell
Growth inhibition assay
Inhibition of human 697 cell growth in a cell viability assay, IC50=10.6 nM.
SANGER
human A427 cell
Growth inhibition assay
Inhibition of human A427 cell growth in a cell viability assay, IC50=34.49 nM.
SANGER
human A549 cell
Growth inhibition assay
Inhibition of human A549 cell growth in a cell viability assay, IC50=49.66 nM
SANGER
human BALL-1 cells
Growth inhibition assay
24 h
Growth inhibition of human BALL-1 cells after 24 hrs by WST-1 assay, GI50=0.08 μM
22264170
human BB65-RCC cell
Growth inhibition assay
Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=110.19 nM
SANGER
human BFTC-905 cell
Growth inhibition assay
Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=108.31 nM
SANGER
human BHT-101 cell
Growth inhibition assay
Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=41.76 nM
SANGER
human CAKI-1 cell
Growth inhibition assay
Growth inhibition of against human HCT116 cells after 24 hrs by WST-1 assay, GI50=0.12 μM
22264170
human CAKI-1 cell
Growth inhibition assay
Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=120 nM
SANGER
human CCRF-CEM cells
Cytotoxic assay
3 days
Cytotoxicity against deoxynucleoside analogue-sensitive human CCRF-CEM cells after 3 days by MTT assay, IC50=1 nM.
19674903
human CCRF-CEM cells
Cytotoxic assay
48 h
Cytotoxicity against human CCRF-CEM cells after 48 hrs by cell titer-blue assay, EC50=5.61 nM.
19743858
human CCRF-CEM cells
Cytotoxic assay
48 h
Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=6 nM.
22582991
human CCRF-CEM/C2 cells
Cytotoxic assay
48 h
Cytotoxicity against human CCRF-CEM/C2 cells after 48 hrs by cell titer-blue assay, EC50=22.8 nM.
19743858
human CEM cells
Cytotoxic assay
48 h
Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 48 hrs, IC50=0.024 μM.
20000418
human CHP-212 cell
Growth inhibition assay
Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=33.47 nM.
SANGER
human COR-L105 cell
Growth inhibition assay
Inhibition of human COR-L105 cell growth in a cell viability assay, IC50=160.39 nM
SANGER
human CTB-1 cell
Growth inhibition assay
Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=34.3 nM
SANGER
human CTV-1 cell
Growth inhibition assay
Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=84.74 nM
SANGER
human ES1 cell
Growth inhibition assay
Inhibition of human ES1 cell growth in a cell viability assay, IC50=12.97 nM.
SANGER
human ES8 cell
Growth inhibition assay
Inhibition of human ES8 cell growth in a cell viability assay, IC50=123.93 nM
SANGER
human EW-1 cell
Growth inhibition assay
Inhibition of human EW-1 cell growth in a cell viability assay, IC50=138.62 nM
SANGER
human GP5d cell
Growth inhibition assay
Inhibition of human GP5d cell growth in a cell viability assay, IC50=102 nM
SANGER
human H460 cells
Function assay
24 h
Antitumor activity against human H460 cells after 24 hrs by MTT assay
20211564
human HCT116 cells
Function assay
Antitumor activity against human HCT116 cells after 24 hrs by MTT assay, IC50=0.1 μM
20211564
human HEL cell
Growth inhibition assay
Inhibition of human HEL cell growth in a cell viability assay, IC50=20.52 nM.
SANGER
human H-EMC-SS cell
Growth inhibition assay
Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50=145.28 nM
SANGER
human HL60 cells
Cytotoxic assay
Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.049 μM.
22582991
human HL60 cells
Cytotoxic assay
48 h
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50=0.118 μM
19321234
human HMV-II cell
Growth inhibition assay
Inhibition of human HMV-II cell growth in a cell viability assay
SANGER
human HT-1080 cell
Growth inhibition assay
Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=114.47 nM
SANGER
human HT-29 cells
Proliferation assay
Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay, IC50=0.066 μM.
2778449
human J-RT3-T3-5 cell
Growth inhibition assay
Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay, IC50=68.42 nM
SANGER
human K5 cell
Growth inhibition assay
Inhibition of human K5 cell growth in a cell viability assay, IC50=43.2 nM
SANGER
human K562 cells
Cytotoxic assay
Cytotoxicity against human K562 cells by SRB assay, IC50=0.05 μM
24956556
human KE-37 cell
Growth inhibition assay
Inhibition of human KE-37 cell growth in a cell viability assay, IC50=110.85 nM
SANGER
human LB1047-RCC cell
Growth inhibition assay
Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=108.42 nM
SANGER
human LB2241-RCC cell
Growth inhibition assay
Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=55.34 nM
SANGER
human leukemia cell line(CCRF-CEM)
Cytotoxic assay
In vitro cytotoxicity of compounds were determined on Inhibition of human leukemia cell line(CCRF-CEM), IC50=0.09 μM.
8917645
human MCF7 1K cells
Cytotoxic assay
3 days
Cytotoxicity against deoxynucleoside analogue-resistant human MCF7 1K cells overexpressing ribonucleotide reductase after 3 days by MTT assay, IC50=40 nM.
19674903
human MCF7 cells
Cytotoxic assay
3 days
Cytotoxicity against deoxynucleoside analogue-sensitive human MCF7 cells after 3 days by MTT assay, IC50=4 nM.
19674903
human MC-IXC cell
Growth inhibition assay
Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=41.41 nM.
SANGER
human MEL-JUSO cell
Growth inhibition assay
Inhibition of human MEL-JUSO cell growth in a cell viability assay, IC50=85.76 nM
SANGER
human MLMA cell
Growth inhibition assay
Inhibition of human MLMA cell growth in a cell viability assay, IC50=55.51 nM
SANGER
human MOLT-16 cell
Growth inhibition assay
Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=36.07 nM.
SANGER
human MOLT-4 cell
Growth inhibition assay
Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=89.67 nM
SANGER
human NB69 cell
Growth inhibition assay
Inhibition of human NB69 cell growth in a cell viability assay, IC50=79.48 nM
SANGER
human NCI-H1703 cell
Growth inhibition assay
Inhibition of human NCI-H1703 cell growth in a cell viability assay, IC50=49.81 nM
SANGER
human NCI-H292 cell
Growth inhibition assay
Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=114.2 nM
SANGER
human NCI-H510A cell
Growth inhibition assay
Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=68.26 nM
SANGER
human NCI-SNU-1 cell
Growth inhibition assay
Inhibition of human NCI-SNU-1 cell growth in a cell viability assay， IC50=96.77 nM
SANGER
human NEC8 cell
Growth inhibition assay
Inhibition of human NEC8 cell growth in a cell viability assay, IC50=134.21 nM
SANGER
human P12-ICHIKAWA cell
Growth inhibition assay
Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=5.54 nM.
SANGER
human P30-OHK cell
Growth inhibition assay
Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=56.5 nM
SANGER
human SAS cell
Growth inhibition assay
Inhibition of human SAS cell growth in a cell viability assay, IC50=107.57 nM
SANGER
human SF268 cells
Cytotoxic assay
Cytotoxicity against human SF268 cells by MTT assay, IC50=7.68 nM.
19345581
human SNU638 cells
Cytotoxic assay
Cytotoxicity against human SNU638 cells by SRB assay, IC50=0.15 μM
24956556
human SW982 cell
Growth inhibition assay
Inhibition of human SW982 cell growth in a cell viability assay, IC50=91.23 nM
SANGER
human T-24 cell
Growth inhibition assay
Inhibition of human T-24 cell growth in a cell viability assay, IC50=78.56 nM
SANGER
human VA-ES-BJ cell
Growth inhibition assay
Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=71.65 nM
SANGER
L1210 cell lines
Function assay
Concentration required to inhibit replication of L1210 cell lines by 50% after 72 hr incubation, ED50=0.05 μM.
1652024
L1210 murine cell lines
Function assay
72 h
The compound was tested in vitro for antitumor activity(50% inhibition of tumor cell growth) against the L1210 murine cell lines after 72 hours, ID50=20 nM.
3625714
MOLT-4 human leukemic lymphoblastoid cell lines
Cytotoxic assay
Cytotoxicity against MOLT-4 human leukemic lymphoblastoid cell lines, IC50=10 nM.
6827546
mouse L1210 cells
Cytotoxic assay
3 days
Cytotoxicity against deoxynucleoside analogue-sensitive mouse L1210 cells after 3 days by MTT assay, IC50=0.4 nM.
19674903
mouse L1210 cells
Cytotoxic assay
48 h
Cytotoxicity against mouse L1210 cells assessed as inhibition of cell proliferation after 48 hrs, IC50=0.024 μM.
20000418
murine leukemia P388
Function assay
Anticancer activity carried out in vitro against murine leukemia P388, IC50=0.14 μM
11356110
P388 murine cell lines
Function assay
72 h
The compound was tested in vitro for antitumor activity(50% inhibition of tumor cell growth) against the P388 murine cell lines after 72 hours, ID50=20 nM.
3625714
parent promyelocytic leukemia cell line
Function assay
Anticancer activity was evaluated for the compound against parent promyelocytic leukemia cell line (HL-60-GHPRT+/dCK+), ED50=47 nM.
3027329
RPMI-6410 human leukemic lymphoblastoid cell lines
Cytotoxic assay
Cytotoxicity against RPMI-6410 human leukemic lymphoblastoid cell lines, IC50=0.06 μM
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