Clofarabine

Catalog No.S1218

Clofarabine Chemical Structure

Molecular Weight(MW): 303.68

Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
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1 Customer Review

  • Cancer Chemoth Pharm, 2015, 75:897-906.. Clofarabine purchased from Selleck.

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Biological Activity

Description Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.
Targets
Ribonucleotide reductase [1]
65 nM
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 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]

Protocol

Solubility (25°C)

In vitro DMSO 60 mg/mL (197.57 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 303.68
Formula

C10H11ClFN5O3

CAS No. 123318-82-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01629082 Completed Myeldysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia|Bone Marrow Diseases|Neutropenia|Acute Myeloid Leukemia (AML) National Heart, Lung, and Blood Institute (NHLBI)|Celgene Corporation|National Institutes of Health Clinical Center (CC) June 5, 2012 Phase 1
NCT02211755 Recruiting Neoplasms|Myelodysplastic Syndromes National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 30, 2014 Phase 1
NCT01701986 Recruiting Lymphoma M.D. Anderson Cancer Center October 25, 2012 Phase 1|Phase 2
NCT02727803 Recruiting Leukemia|Lymphoma|Myeloma|Myeloproliferative Diseases M.D. Anderson Cancer Center May 2016 Phase 2
NCT02686593 Recruiting Acute Myeloid Leukemia The University of Hong Kong February 2016 Phase 2
NCT02925351 Recruiting Autoimmune Disease|Crohn Disease|Inflammatory Disorder|Rheumatoid Arthritis|Systemic Lupus Erythematosus|Takayasu Arteritis Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) January 2016 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID