Cladribine

Alias: 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA; 2-CdA, 2-chlorodeoxyadenosine; Cladribina. Trade name: Leustatin; Leustat; Leustatine
Cat No.:V1456 Purity: ≥98%
Cladribine (also known as 2-CdA, 2-chlorodeoxyadenosine; Leustatin; Leustat; Leustatine), a purine nucleoside antimetabolite analogue and an approved medication used for treating hairy cell leukemia and B-cell chronic lymphocytic leukemia, is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50s of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
Cladribine Chemical Structure CAS No.: 4291-63-8
Product category: DNA(RNA) Synthesis
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cladribine (also known as 2-CdA, 2-chlorodeoxyadenosine; Leustatin; Leustat; Leustatine), a purine nucleoside antimetabolite analogue and an approved medication used for treating hairy cell leukemia and B-cell chronic lymphocytic leukemia, is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50s of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively. It is a well-known purine nucleoside analog that exhibits unique anti-lymphoma-proliferative activity against diseases like hairy cell leukemia (HCL). Cladribine exhibited dose-dependent inhibition of cell proliferation in U266, RPMI8226, and MM1.S cells, with IC50 values of 2.43, 0.75, and 0.18 μmol/L, in that order.

Biological Activity I Assay Protocols (From Reference)
Targets
Adenosine deaminase (MM1.S cells) ( IC50 = 0.18 μM )
Adenosine deaminase (RPMI8226 cells) ( IC50 = 0.75 μM )
Adenosine deaminase (U266 cells) ( IC50 = 2.43 μM )
ln Vitro

Cladribine exhibits exceptional efficacy in treating hairy cell leukemia (HCL), a chronic B-cell lymphoproliferative illness, resulting in extended, full remissions. Cladribine causes strand breaks in DNA to accumulate, which in turn triggers the activation of the tumor suppressor p53 in lymphocytes. In MM cells, cladribine may alter STAT3 activity. In a dose-dependent manner, cladribine inhibits the proliferation and survival of U266; RPMI8226; and MM1.S cells. The most cladribine-sensitive cell line is MM1.S, while U266 is the least. Cladribine treatment progressively raises the proportion of cells in the G1 phase and lowers the proportion of cells in the S phase of the cell cycle. After a 24-hour treatment, cladribine appears to lengthen the G2-M phase in U266 cells. Both RPMI8226 and MM1.S cells exhibit an increase in apoptosis brought on by cladribine that is dose-dependent. In MM1.S, 0.2 μM cladribine treatment significantly increases caspase-3, -8, and -9 activation as well as PARP cleavage in a time-dependent manner. While cladribine has no effect on the levels of total STAT3 protein, it dramatically reduces the levels of phospho-STAT3 (P-STAT3) in a dose-dependent manner. [1] In HSB2 cells, cladribine has the ability to induce apoptosis in a concentration-dependent manner. [2] Primary mast cell (MC) and the MC line HMC-1 are inhibited in growth by cladribine in a dose-dependent manner; IC50 values are lower in HMC-1.2 cells that carry KIT D816V than in HMC-1.1 cells that do not. [3] Cladribine inhibits CD4+ and CD8+ T lymphocyte migration as well as that of CD14+ monocytes. [4]

ln Vivo
Cladribine (0.7-3.5 mM) and/or diltiazem (2.4 mM), is injected intraperitoneally into adult zebrafish, and the levels of purine nucleotides (such as ATP), which may be biomarkers of cardiovascular health, are measured by HPLC in the lysates of the RBCs. RBC ATP concentrations were raised by diltiazem and are subsequently decreased by co-injecting cladribine.[5] Cladribine plasma concentrations drop quickly after both intraperitoneal and systemic administrations, with a biphasic decline. Following a single injection of 1 mg/kg ia and 2 mg/kg s.c. of Cladribine, the AUC and t 1/2 beta are 0.66 vs 1.2 μg × h/mL and 3.5 vs 4.5 hours, respectively.[6]
Cell Assay
The viability of the cells is assessed using the non-radioactive cell proliferation kit. To summarize, 0.1 mL of complete medium (5% FBS) is used as a control, or 0.1 mL of the same medium containing multiple doses of cladribine, is added to 96-well plates, and the cells are incubated for 72 hours. Reduction of MTS is used to calculate the percentages of surviving cells from each group in comparison to controls, which is defined as 100% survival, after reading all wells at 490 nm using a micro-plate reader.
Animal Protocol
Dissolved in saline; 0.7 mM - 3.5 mM; i.p. injection
Adult wild-type (AB) zebrafish
References

[1]. BMC Cancer . 2011 Jun 16:11:255.

[2]. Cancer Chemother Pharmacol . 1998;42(1):77-83.

[3]. Exp Hematol . 2010 Sep;38(9):744-55.

[4]. Eur J Neurol . 2009 Mar;16(3):409-12.

[5]. Biomarkers . 2009 Dec;14(8):554-9.

[6]. Drug Metabol Drug Interact . 2008;23(3-4):291-8.

[7]. Ann Hematol . 2002 Sep;81(9):508-13.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C10H12CLN5O3
Molecular Weight
285.69
Exact Mass
285.06
Elemental Analysis
C, 42.04; H, 4.23; Cl, 12.41; N, 24.51; O, 16.80
CAS #
4291-63-8
Appearance
Solid powder
SMILES
C1[C@@H]([C@H](O[C@H]1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O
InChi Key
PTOAARAWEBMLNO-KVQBGUIXSA-N
InChi Code
InChI=1S/C10H12ClN5O3/c11-10-14-8(12)7-9(15-10)16(3-13-7)6-1-4(18)5(2-17)19-6/h3-6,17-18H,1-2H2,(H2,12,14,15)/t4-,5+,6+/m0/s1
Chemical Name
(2R,3S,5R)-5-(6-amino-2-chloropurin-9-yl)-2-(hydroxymethyl)oxolan-3-ol
Synonyms
2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA; 2-CdA, 2-chlorodeoxyadenosine; Cladribina. Trade name: Leustatin; Leustat; Leustatine
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~57 mg/mL (~199.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
5% DMSO+ 30% PEG 300+ 1% Tween 80+ H2O: 10mg/mL (35.00mM) (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5003 mL 17.5015 mL 35.0030 mL
5 mM 0.7001 mL 3.5003 mL 7.0006 mL
10 mM 0.3500 mL 1.7501 mL 3.5003 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04239820 Active
Recruiting
Radiation: Imaging Multiple Sclerosis Turku University Hospital January 10, 2020 N/A
NCT04640818 Active
Recruiting
Drug: Cladribine Oral Tablet
Drug: Rituximab
Multiple Sclerosis Claudio Gobbi December 17, 2020 N/A
NCT03933215 Active
Recruiting
Drug: Cladribine Tablets Multiple Sclerosis EMD Serono Research & May 21, 2019 N/A
NCT03933202 Active
Recruiting
Drug: Cladribine Tablets Multiple Sclerosis EMD Serono Research &
Development Institute, Inc.
July 22, 2019 N/A
NCT04239820 Active
Recruiting
Radiation: Imaging Multiple Sclerosis Turku University Hospital January 10, 2020 N/A
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