Catalog No.S1199 Synonyms: 2-CdA, 2-chlorodeoxyadenosine
Molecular Weight(MW): 285.69
Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
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|Description||Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.|
|Features||Cladribine is primarily active in lymphoid tissues.|
Cladribine exerts remarkable activity in hairy cell leukemia (HCL), a chronic B-cell lymphoproliferative disorder, producing prolonged complete remissions. Cladribine induces accumulation of DNA strand breaks, and subsequently activates the tumor suppressor p53 in lymphocytes. Cladribine may modulate STAT3 activity in MM cells. Cladribine inhibits proliferation/survival of U266, RPMI8226 and MM1.S cells in a dose-dependent manner. While U266 is the least sensitive cell line, MM1.S is the most sensitive one to cladribine. Treatment with cladribine gradually increases the percentage of cells in the G1 phase of the cell cycle and reduces the percentage of cells in S phase. Cladribine appears to increase G2-M phase in U266 cells upon 24 hour-treatment. A dose-dependent increase in apoptosis induced by cladribine is seen in both RPMI8226 and MM1.S cells. Treatment with cladribine at 0.2 μM dramatically induces activation of caspase-3, -8, and -9 and PARP cleavage in a time-dependent manner in MM1.S. Cladribine significantly decreases the phospho-STAT3 (P-STAT3) levels in a dose-dependent manner, but has no effect on the total STAT3 protein levels.  Cladribine possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells.  Cladribine inhibits growth of primary mast cell (MC) and the MC line HMC-1 in a dose-dependent manner, with lower IC50 values recorded in HMC-1.2 cells harboring KIT D816V compared to HMC-1.1 cells lacking KIT D816V.  Cladribine decreases the migratory capacity of CD14+ monocytes, as well as of CD4+ and CD8+ T lymphocytes. 
|In vivo||Cladribine (0.7-3.5 mM) and/or diltiazem (2.4 mM), is injected intraperitoneally into adult zebrafish and red blood cell (RBC) lysates are assayed by HPLC for levels of purine nucleotides (e.g. ATP), potential biomarkers of cardiovascular health. Diltiazem increased RBC ATP concentrations, which are inhibited by co-injection of cladribine.  Plasma concentrations of Cladribine decreases rapidly following a biphasic decline after both ia and s.c. administrations. The AUC and t 1/2 beta after a single 1 mg/kg ia and 2 mg/kg s.c. injection of Cladribine are 0.66 vs 1.2 μg × h/mL and 3.5 vs 4.5 hours, respectively. |
-  Ma J, et al. BMC Cancer. 2011, 11, 255.
-  Guchelaar HJ, et al. Cancer Chemother Pharmacol. 1998, 42(1), 77-83.
-  B?hm A, et al. Exp Hematol. 2010, 38(9), 744-755.
|In vitro||DMSO||57 mg/mL (199.51 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+1% Tween 80+H2O
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04121065||Not yet recruiting||Procedure: Blood withdrawal||Relapsing Multiple Sclerosis||Neuromed IRCCS||January 2020||--|
|NCT03963375||Recruiting||Drug: Cladribine||Multiple Sclerosis|Multiple Sclerosis Relapsing-Remitting||Washington University School of Medicine|EMD Serono||October 2019||Phase 4|
|NCT03933202||Recruiting||Drug: Cladribine Tablets||Multiple Sclerosis||EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono||July 22 2019||--|
|NCT03933215||Recruiting||Drug: Cladribine Tablets||Multiple Sclerosis||EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono||May 21 2019||--|
|NCT03745144||Recruiting||Drug: Cladribine|Drug: Placebo|Drug: Microgynon®||Relapsing Multiple Sclerosis (RMS)||Merck KGaA Darmstadt Germany||January 17 2019||Phase 1|
|NCT03235973||Recruiting||Drug: Fludarabine-Cladribine-Busulfan conditioning regimen||Leukemia Myeloid Acute|Leukemia Lymphoblastic Acute||Institut Paoli-Calmettes||April 28 2018||Phase 1|
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