A ribonucleotide reductase and DNA polymerase-α inhibitor
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Clofarabine

Item No. 14125

Technical Information
Formal Name
2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
CAS Number
123318-82-1
Synonyms
  • Clolar
  • Evoltra
Molecular Formula
C10H11ClFN5O3
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
212, 263 nm
SMILES
OC[C@@H]1[C@@H](O)[C@H](F)[C@H](N2C=NC3=C2N=C(Cl)N=C3N)O1
InChi Code
InChI=1S/C10H11ClFN5O3/c11-10-15-7(13)5-8(16-10)17(2-14-5)9-4(12)6(19)3(1-18)20-9/h2-4,6,9,18-19H,1H2,(H2,13,15,16)/t3-,4+,6-,9-/m1/s1
InChi Key
WDDPHFBMKLOVOX-AYQXTPAHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Clofarabine is a nucleoside analog that inhibits ribonucleotide reductase and DNA polymerase-α (IC50s = 65 and 3.9 nM, respectively) and is cytotoxic to K562 myelogenous leukemia cells (IC50 = 5 nM).1 It induces apoptosis in primary chronic lymphocytic leukemia cells by directly altering mitochondrial transmembrane potential.2 Clofarabine demonstrates growth inhibition and cytotoxic activity in a variety of leukemias and solid tumors.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Parker, W.B., Shaddix, S.C., Chang, C.H., et alEffects of 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)adenine on K562 cellular metabolism and the inhibition of human ribonucleotide reductase and DNA polymerases by its 5'-triphosphate. Cancer Res. 51, 2386-2394 (1991).

    2. Genini, D., Adachi, S., Chao, Q., et alDeoxyadenosine analogs induce programmed cell death in chronic lymphocytic leukemia cells by damaging the DNA and by directly affecting the mitochondria. Blood 96(10), 3537-3543 (2000).

    3. Yamauchi, T., Nowak, B.J., Keating, M.J., et alDNA repair initiated in chronic lymphocytic leukemia lymphocytes by 4-hydroperoxycyclophosphamide is inhibited by fludarabine and clofarabine. Clin. Cancer Res. 7, 3580-3589 (2001).

    4. Chiarini, F., Lonetti, A., Teti, G., et alA combination of temsirolimus, an allosteric mTOR inhibitor, with clofarabine as a new therapeutic option for patients with acute myeloid leukemia. Oncotarget 3(12), 1615-1628 (2012).

    5. Lee, Y.J., Im, J.H., Lee, D.M., et alSynergistic inhibition of mesothelioma cell growth by the combination of clofarabine and resveratrol involves Nrf2 downregulation. BMB Rep. 45(11), 647-652 (2012).