Cladribine  (Synonyms: 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA)

Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis^[1][2].

Adenosine deaminase^[2]

Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation^[1].
? Cladribine (1-4 μM; 24 hours) induces G1 phase arrest via decreasing the expressions of Cyclin D1 and Cyclin E, and increasing the expressions of p21 and p27 in DLBCL cells^[1].
? Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells^[1].
? Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress^[1].
? Cladribine inhibits cell proliferation of multiple myeloma (MM) cells in a dose-dependent manner; with IC₅₀s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cladribine (10 μg/kg; i.p.; 3 times/week; for 2 weeks) may have benefits in the treatment of ischemia/reperfusion injury to the biochemical and histopathologic parameters^[3].
? Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice^[4].
? Cladribine exhibits C_max (rat 4.9 ng/mL) following intra-arterial injection^[5].
? Cladribine exhibits C_max (rat 1.1 ng/mL) following subcutaneous injection^[5].
? Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection^[5].
? Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection^[5].
? Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

285.69

C₁₀H₁₂ClN₅O₃

4291-63-8

Solid

White to off-white

OC[C@@H]1[C@@H](O)C[C@H](N2C=NC3=C2N=C(Cl)N=C3N)O1

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Linyan Xu, et al. Cladribine Induces ATF4 Mediated Apoptosis and Synergizes with SAHA in Diffuse Large B-Cell Lymphoma Cells. Int J Med Sci. 2020; 17(10): 1375–1384.  [Content Brief]

  [2]. Jian Ma, et al. Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer. 2011 Jun 16;11:255.  [Content Brief]

  [3]. Young Seop Chang, et al. MP28-10 COMBINED EFFECTS OF MELATONIN AND CLADRIBINE ON APOPTOSIS IN ISCHEMIA/REPERFUSION INJURY IN RAT BLADDER. THE JOURNAL OF UROLOGY. April 2016. 195 (4S): e375.

  [4]. Crystal D Hayes, et al. Chronic cladribine administration increases amyloid beta peptide generation and plaque burden in mice. PLoS One. 2012;7(10):e45841.  [Content Brief]

  [5]. Yeung, P. K. F., et al. Pharmacokinetics of Cladribine in a Rat Model Following Subcutaneous and Intra-arterial Injections. Drug Metabol Drug Interact. 2008;23(3-4):291-8.  [Content Brief]