Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor - RNR inhibitor - Autophagy activator - Apoptosis related activator Clofarabine For research use only.

Clofarabine

Synonyms: Clolar

Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.

Clofarabine Chemical Structure

Clofarabine Chemical Structure

CAS: 123318-82-1

Selleck's Clofarabine has been cited by 20 Publications

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Purity & Quality Control

Batch: Purity: 99.90%
99.90

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Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K562 cell Cytotoxicity assay Compound was tested for cytotoxicity against K562 cell lines, IC50=0.003 μM 1732556
HEp-2 cell Cytotoxicity assay Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.012 μM 1732556
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.05 μM 1732556
L1210 cell Cytotoxicity assay Compound was tested for cytotoxicity against L1210 cell lines, IC50=2.3 μM 1732556
NCI-H23 Cytotoxicity assay 5 days Cytotoxicity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.04μM 19929004
PC3 Cytotoxicity assay 5 days Cytotoxicity against human PC3 cells after 5 days by SRB assay, GI50=0.063μM 19929004
BT549 Cytotoxicity assay 5 days Cytotoxicity against human BT549 cells after 5 days by SRB assay, GI50=0.065μM 19929004
HCT15 Cytotoxicity assay 5 days Cytotoxicity against human HCT15 cells after 5 days by SRB assay, GI50=0.18μM 19929004
NCI-H23 Cytostatic assay 5 days Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.04μM 21711054
MT4 Cytostatic assay 5 days Cytostatic activity against human MT4 cells after 5 days by SRB assay, GI50=0.051μM 21711054
PC3 Cytostatic assay 5 days Cytostatic activity against human PC3 cells after 5 days by SRB assay, GI50=0.063μM 21711054
BT549 Cytostatic assay 5 days Cytostatic activity against human BT549 cells after 5 days by SRB assay, GI50=0.065μM 21711054
A549 Cytostatic assay 5 days Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.086μM 21711054
HCT116 Cytostatic assay 5 days Cytostatic activity against human HCT116 cells after 5 days by SRB assay, GI50=0.106μM 21711054
DU145 Cytostatic assay 5 days Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.125μM 21711054
HCT15 Cytostatic assay 5 days Cytostatic activity against human HCT15 cells after 5 days by SRB assay, GI50=0.18μM 21711054
Hs578 Cytostatic assay 5 days Cytostatic activity against human Hs578 cells after 5 days by SRB assay, GI50=1.241μM 21711054
HL60 Cytostatic assay 48 hrs Cytostatic activity against human HL60 cells after 48 hrs by MTT assay, IC50=0.1μM 23820572
A549 Cytostatic assay 48 hrs Cytostatic activity against human A549 cells after 48 hrs by MTT assay, IC50=8μM 23820572
U373-MAGI Function assay 50 nM 2 hrs Potentiation of 5-Aza-C-induced antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as 5-Aza-C EC50 at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs and subsequent viral infection measu, EC50=30.4μM 27117260
U373-MAGI Antiviral assay 50 nM 4 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in viral infectivity at 50 nM incubated for 4 hrs prior to viral infection measured at 72 hrs post infection by flow cytometric analysis 27117260
U373-MAGI Function assay 200 nM 6 hrs Reduction in dGTP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis 27117260
U373-MAGI Function assay 200 nM 6 hrs Reduction in dCTP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis 27117260
U373-MAGI Function assay 200 nM 6 hrs Reduction in dATP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis 27117260
U373-MAGI Function assay 50 nM 2 hrs Reduction in dCTP level in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis 27117260
U373-MAGI Function assay 200 nM 2 hrs Reduction in dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-C 27117260
U373-MAGI Function assay 50 nM 2 hrs Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC 27117260
U373-MAGI Function assay 200 nM 2 hrs Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC 27117260
U373-MAGI Function assay 200 nM 2 hrs Reduction in dRGU-TP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis 27117260
U373-MAGI Function assay 200 nM 2 hrs Reduction in 5-aza-dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis 27117260
U373-MAGI Function assay 200 nM 2 hrs Reduction in dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC 27117260
U373-MAGI Function assay 50 nM 2 hrs Reduction in dCTP level in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC 27117260
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells 29435139
Granta Cytotoxicity assay 72 hrs Cytotoxicity against human Granta cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.017μM 30176535
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.04μM 30176535
CCRF-CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CCRF-CEM cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.044μM 30176535
RL Cytotoxicity assay 72 hrs Cytotoxicity against human RL cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.38μM 30176535
Click to View More Cell Line Experimental Data

Biological Activity

Description Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Targets
Ribonucleotide reductase [1]
(Cell-free assay)
65 nM
In vitro
In vitro Clofarabine is efficiently transported into cells via two facilitative or equilibrative nucleoside transporters, hENT1 and hENT2, and a concentrative nucleoside transporter, hCNT253. Clofarabine is phosphorylated in a stepwise manner by cytosolic kinases to the nucleotide analogues clofarabine 5′-mono-, di- and triphosphate following entry into cells, with Clofarabine triphosphate being the active form. Clofarabine 5′-mono-, di- and triphosphate are not substrates for nucleoside transporters and must be enzymatically converted by 5′-nucleotidase back to their dephosphorylated nucleoside form for transport out of the cell. Clofarabine triphosphate is a potent inhibitor of ribonucleotide reductase (IC50 = 65 nM), presumably by binding to the allosteric site on the regulatory subunit. Clofarabine has also been shown to act directly on mitochondria by altering the transmembrane potential with release of cytochrome c, apoptotic-inducing factor (AIF), apoptosis protease-activating factor 1 (APAF1) and caspase 9 into the cytosol. Clofarabine demonstrates strong in vitro growth inhibition and cytotoxic activity (IC50 values = 0.028–0.29 μM) in a wide variety of leukaemia and solid tumour cell lines. Clofarabine has been shown to increase the activity of dCK in HL60 cells, and increases the formation of the mono-, di-, and triphosphates of ara-C in K562 cells36. [1] Clofarabine (10 μM) inhibits the repair initiated by 4-hydroperoxycyclophosphamide (4-HC), with inhibition peaking at the intracellular concentrations of 5 μM in chronic lymphocytic leukemia (CLL) lymphocytes. Clofarabine (10 μM) combined with 4-hydroperoxycyclophosphamide (4-HC) produces more than additive apoptotic cell death than the sum of each alone. [2] Clofarabine (1 μM) combined with ara-C (10 μM) results in a biochemical modulation of ara-CTP and synergistic cell kill in K562 cells. [3]
In Vivo
In vivo Clofarabine administered intraperitoneally has significant activity against a wide variety of human tumour xenografts implanted subcutaneously in athymic nude or severe combined immune deficiency mice. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05917405 Recruiting
Acute Myeloid Leukemia in Remission
Nantes University Hospital
 September 14 2023 Phase 2
NCT03609814 Completed
Hematologic Malignancies|Nonmalignant Diseases|Immunodeficiencies|Hemoglobinopathies|Genetic Inborn Errors of Metabolism|Fanconi''s Anemia|Thalassemia|Sickle Cell Disease
University of California San Francisco
 January 26 2016 --

Chemical Information & Solubility

Molecular Weight 303.68 Formula

C10H11ClFN5O3
CAS No. 123318-82-1 SDF Download Clofarabine SDF
Smiles C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)F)Cl)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (197.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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