PRODUCT INFORMATION

Cladribine
Item No. 12085

CAS Registry No.: 4291-63-8

Formal Name: 2-chloro-2-deoxy-adenosine N
Synonyms: Biodribin, 2-Chlorodeoxyadenosine, Jk 6251, N O
H2N
Leustatin, NSC 105014, RWJ 26251 OH
MF: C10H12ClN5O3
FW: 285.7 N N
OH
Purity: 98%
UV/Vis.: max: 212, 265 nm Cl
Supplied as: A crystalline solid
Storage: -20C
Stability: As supplied, 2 years from the QC date provided on the Certificate of Analysis, when
stored properly

Laboratory Procedures

Cladribine is supplied as a crystalline solid. A stock solution may be made by dissolving the cladribine in
the solvent of choice. Cladribine is soluble in organic solvents such as DMSO and dimethyl formamide, which
should be purged with an inert gas. The solubility of cladribine in these solvents is approximately 11 and
16 mg/ml, respectively.
Cladribine is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, cladribine
should first be dissolved in DMF and then diluted with the aqueous buffer of choice. Cladribine has a
solubility of approximately0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method. We do not
recommend storing the aqueous solution for more than one day.

Description

Cladribine is an adenosine analog which shows selective cytotoxicity against both proliferating and non-
dividing lymphocytes. Resistant to adenosine deaminase, cladribine is phosphorylated by deoxycytidine
kinase, resulting in its intracellular accumulation and inhibition of ribonucleotide reductase.1,2 It inhibits
lymphocyte growth with an IC50 value of 45 nM.3 The pharmacokinetics of clabridine in humans have been
published.4 After only a single course of treatment, clabridine eradicates hairy cell leukemia.5 It has potential
use in a variety of hematologic malignancies, but its use in treating multiple sclerosis is compromised by
serious adverse events.6,7

References

1. Tallman, M.S. and Hakimian, D. Blood 86(7), 2463-2474 (1995).

2. Seto, S., Carrera, C.J., Kubota, M., et al. J. Clin. Invest. 75, 377-383 (1985).
3. Huang, M.-C., Ashmun, R.A., Avery, T.L., et al. Cancer Res. 46, 2362-2368 (1986).
4. Liliemark, J. and Juliusson, G. Cancer Res. 51, 5570-5572 (1991).
5. Sigal, D.S., Sharpe, R., Burian, C., et al. Blood 115(10), 1893-1896 (2010).
6. Sigal, D.S., Miller, H.J., Schram, E.D., et al. Blood 116(16), 2884-2896 (2010).
7. Nicholas, R., Giannetti, P., Alsanousi, A., et al. Drug Des. Devel. Ther. 5, 255-274 (2011).

WARNING CAYMAN CHEMICAL

THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD
SAFETY DATA ANN ARBOR, MI 48108 USA
This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after
handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. PHONE: [800] 364-9897
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