Clofarabine

Catalog No.S1218

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

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Clofarabine Chemical Structure

Clofarabine Chemical Structure
Molecular Weight: 303.68

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Product Description

Biological Activity

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Bonate PL, et al. Nat Rev Drug Discov, 2006, 5(10), 855-863.

[2] Yamauchi T, et al. Clin Cancer Res, 2001, 7(11), 3580-3589.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
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
NCT02518750 Recruiting Acute Lymphoblastic Leukemia|Lymphoma, Non-Hodgkins|Leukemia, T-Cell|Leukemia, B-Cell St. Jude Childrens Research Hospital|Novartis Pharmaceuti  ...more St. Jude Childrens Research Hospital|Novartis Pharmaceuticals December 2015 Phase 2
NCT02441803 Recruiting Leukemia M.D. Anderson Cancer Center September 2015 Phase 2
NCT02425904 Recruiting Langerhans Cell Histiocytosis Dana-Farber Cancer Institute|Sanofi|St. Baldricks Foundat  ...more Dana-Farber Cancer Institute|Sanofi|St. Baldricks Foundation|Cookies for Kids Cancer April 2015 Phase 2

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Chemical Information

Download Clofarabine SDF
Molecular Weight (MW) 303.68
Formula

C10H11ClFN5O3

CAS No. 123318-82-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 60 mg/mL (197.57 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name  2-​chloro-​9-​(2-​deoxy-​2-​fluoro-​β-​D-​arabinofuranosyl)​-9H-​purin-​6-​amine

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