Molecular Weight(MW): 303.68
Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.
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|Description||Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.|
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.  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.  Clofarabine (1 μM) combined with ara-C (10 μM) results in a biochemical modulation of ara-CTP and synergistic cell kill in K562 cells. 
|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. |
|In vitro||DMSO||60 mg/mL (197.57 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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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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