Nutrabiotech Cladribine 98% 1G Powder, 98% high purity Cladribine powder, purine nucleoside analog, selective lymphocyte inhibitor, autoimmune neuroinflammation research raw material

High Purity Cladribine Powder CAS 4291-63-8

High-purity Cladribine powder CAS 4291-63-8, a synthetic purine nucleoside analog and bioactive antimetabolite compound. Widely utilized in biomedical research, cell metabolism study, pharmaceutical intermediate development and laboratory scientific research. Offers high stability, precise molecular activity and reliable bulk raw material supply for global research institutions.
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Cladribine (CAS 4291-63-8) Purine Nucleoside Analog | dCK-Dependent Lymphocyte Depletion, MS & HCL

Cladribine CAS 4291-63-8
Purine Nucleoside Analog & Lymphocyte-Depleting SIRT

A deoxyadenosine-mimic purine nucleoside analog, also known as 2-chlorodeoxyadenosine (2-CdA). Cladribine is resistant to adenosine deaminase (ADA) and acts as a prodrug: intracellular phosphorylation by deoxycytidine kinase (dCK) yields the active triphosphate CdATP, which preferentially accumulates in lymphocytes (high dCK, low 5'-nucleotidase) and disrupts DNA synthesis and repair, triggering apoptosis. FDA-approved (2019, brand Mavenclad) as an oral selective immune reconstitution therapy for relapsing multiple sclerosis; first-line in hairy cell leukemia with an 84% complete response rate.

Purine Nucleoside Analog dCK-Dependent Lymphocyte Depletion SIRT Multiple Sclerosis Hairy Cell Leukemia ADA-Resistant
Request a Quote Technical Specs
285.69
MW (C10H12ClN5O3)
84%
HCL Complete Response
≥98%
Purity (HPLC)

Molecular Information

Name: Cladribine
CAS: 4291-63-8
Formula: C10H12ClN5O3
MW: 285.69 g/mol
SMILES: C1C(C(OC1N2C=NC
  3=C(N=C(N=C32)Cl)N)CO)O
InChIKey: PTOAARAWEBMLNO
  -KVQBGUIXSA-N
Appearance: White to off-white crystalline
Synonyms: 2-CdA / 2CDA / Mavenclad
Storage: 0-4°C short, -20°C long term
🧪
CAS Number
4291-63-8
⚖️
Molecular Weight
285.69
🎯
Primary Activity
dCK / CdATP
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for Cladribine (CAS 4291-63-8)

📋 Physicochemical Properties

  • Product NameCladribine
  • IUPAC Name5-(6-Amino-2-chloropurin-9-yl)-2-(hydroxymethyl)oxolan-3-ol
  • CAS Number4291-63-8
  • Synonyms2-CdA / 2CDA / Mavenclad
  • Molecular FormulaC10H12ClN5O3
  • Molecular Weight285.69 g/mol
  • SMILESC1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O
  • InChIKeyPTOAARAWEBMLNO-KVQBGUIXSA-N
  • AppearanceWhite to off-white crystalline powder
  • HS Code2934.99
  • PubChem CID451164

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormCrystalline powder
  • ColorWhite to off-white
  • Bioavailability100% IV; 37-51% oral
  • Half-life5.4-19.7 h (dose route)
  • Protein Binding20-25%
  • SolubilityWater ~6.35 g/L; DMSO
  • Storage Condition0-4°C short; -20°C long term
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Enzyme Interactions

Cladribine's chlorinated deoxyadenosine scaffold engages nucleotide metabolism and DNA synthesis machinery with lymphocyte selectivity

🧬 Deoxycytidine Kinase (dCK) 🧪 DNA Polymerase ⚙️ Ribonucleotide Reductase 🛡️ Adenosine Deaminase (resistant) 🧫 DNA Repair 🩸 B / T Lymphocytes 💊 CdATP Incorporation 🧠 CNS Immune (MS) 🦠 Hairy Cell Leukemia 🔥 Apoptosis

How Cladribine Works: From dCK Activation to Lymphocyte Apoptosis

Cladribine acts as a prodrug whose selectivity arises from the cellular enzyme balance of lymphoid cells

1

ADA Resistance & Cellular Uptake

Cladribine mimics deoxyadenosine but is resistant to adenosine deaminase (ADA), so it is not rapidly degraded. It enters cells via nucleoside transporters and persists long enough to be metabolically activated.

2

dCK-Dependent Activation to CdATP

Within cells, deoxycytidine kinase (dCK) phosphorylates cladribine to its active triphosphate, CdATP. Lymphocytes have high dCK and low 5'-nucleotidase, so CdATP preferentially accumulates in B and T cells.

3

DNA Disruption & Apoptosis

Incorporated CdATP disrupts DNA synthesis and repair (inhibiting DNA polymerase, ribonucleotide reductase, and repair enzymes), triggering lymphocyte apoptosis and producing the selective immune reconstitution (SIRT) effect.

Research Applications & Disease Models

Cladribine's lymphoid selectivity spans neurology, hematology, oncology and immune-metabolism research

🧠

Multiple Sclerosis

FDA-approved (2019) oral selective immune reconstitution therapy (SIRT) for relapsing MS (brand Mavenclad). The CLARITY trial demonstrated reduced relapse rate and MRI activity via preferential B/T lymphocyte depletion.

CLARITY Trial
🩸

Hairy Cell Leukemia

First-line therapy with an ~84% complete response rate. Cladribine's durable lymphodepletion is highly effective against this indolent B-cell malignancy, establishing its foundational clinical profile.

84% CR
🧬

B-Cell CLL

Used as second-line therapy in chronic lymphocytic leukemia. Its dCK-dependent activation makes it active against proliferating and quiescent lymphoid clones alike.

Second-line
⚗️

Purine Metabolism

A classic tool for studying the dCK / 5'-nucleotidase ratio, nucleoside analog pharmacology, and the determinants of lymphoid versus myeloid sensitivity to antimetabolites.

Nucleoside Analog
🧫

DNA Damage Response

CdATP incorporation and inhibition of DNA repair enzymes make cladribine a model compound for investigating replication stress, mismatch repair, and apoptosis-linked DNA damage pathways.

DNA Repair
🛡️

Lymphocyte Biology

Enables selective B- and T-cell depletion and the study of immune reconstitution kinetics — foundational for SIRT concepts and tolerogenic immune remodeling.

Immune Reconstitution
🌀

Autoimmune Disease

Investigated in other autoimmune conditions where pathogenic lymphocyte clones drive disease, leveraging the same lymphoid-selective depletion validated in MS.

Investigational
🔬

Langerhans Cell Histiocytosis

Explored as an orphan indication given its activity against dendritic-cell lineage malignancies, reflecting the breadth of its antilymphoid spectrum.

Orphan Indication
⚖️

Nucleoside Analog Pharmacology

A benchmark compound for comparing chlorinated vs fluorinated deoxyadenosine analogs (e.g., vs fludarabine) and for optimizing lymphoid selectivity in drug design.

SAR Benchmark

Key Literature & Landmark Publications

Seminal papers on cladribine's discovery, mechanism, MS efficacy, and pharmacokinetics

Carson DA, Wasson DB, Taetle R, et al. Antileukemic and immunosuppressive activity of 2-chloro-2'-deoxyadenosine. Proceedings of the National Academy of Sciences USA. 1983;80(19):5951-5955.
doi: 10.1073/pnas.80.19.5951
Giovannoni G, Comi G, Cook S, et al. A placebo-controlled trial of oral cladribine for relapsing multiple sclerosis (CLARITY). New England Journal of Medicine. 2010;362(5):416-426.
doi: 10.1056/NEJMoa0902533
Leist TP, Comi G, Cree BA, et al. The Development of Cladribine Tablets for the Treatment of Multiple Sclerosis. Drugs. 2020;80(18):1859-1873.
PMC7708385
Liliemark J. Clinical pharmacokinetics of cladribine (2-chloro-2'-deoxyadenosine). Clinical Pharmacokinetics. 1997;32(2):120-131.
doi: 10.2165/00003088-199732020-00003

Available Sizes & Ordering

Research-grade Cladribine (CAS 4291-63-8) with full QC documentation; research packs and bulk custom quantities supported

TierPack SizeStock StatusSuitable ForLead Time
Standard1 gIn StockBiochemical / cell-based assaysSame/next-day ship
Medium5 gIn StockIn vivo pharmacology, long-term studiesSame/next-day ship
Large10 gIn StockMulti-lab collaborations, HTSSame/next-day ship
Bulk100 gIn StockProcess development, scale-upQuote to confirm
Industrial1 KGMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is Cladribine (CAS 4291-63-8), and what makes it unique?
Cladribine, also known as 2-chlorodeoxyadenosine (2-CdA), is a purine nucleoside analog that mimics deoxyadenosine. It is resistant to adenosine deaminase (ADA) and acts as a prodrug: deoxycytidine kinase (dCK) phosphorylates it to the active triphosphate CdATP, which disrupts DNA synthesis and repair and preferentially depletes lymphocytes. It is FDA-approved (2019, brand Mavenclad) as an oral selective immune reconstitution therapy (SIRT) for relapsing MS and is first-line in hairy cell leukemia (84% complete response). Molecular formula C10H12ClN5O3, MW 285.69.
How does Cladribine compare to fludarabine in potency?
Both are purine nucleoside analogs with distinct properties. Cladribine (2-CdA) is more potent and longer-lived in lymphocytes due to its ADA-resistant chloro-substituent and efficient dCK-mediated activation, producing durable lymphopenia. Fludarabine (2-F-Ara-A) is also dCK-activated but is not chlorinated and has somewhat different tissue distribution and toxicity. Cladribine's high potency underlies both its hairy cell leukemia efficacy and its careful risk-benefit management in MS.
Why is oral Cladribine bioavailable while many nucleotides are not?
Cladribine is a small, membrane-permeable nucleoside (not a charged nucleotide), enabling efficient cellular uptake followed by intracellular phosphorylation. Oral bioavailability is 37-51%, versus ~100% for IV/SC administration. Its passive diffusion plus transporter-mediated uptake and ADA resistance let it reach lymphoid compartments even after oral dosing — enabling the oral Mavenclad regimen.
What is the concept of selective immune reconstitution therapy (SIRT)?
SIRT describes cladribine's property of preferentially depleting pathogenic B and T lymphocytes while allowing gradual, endogenous immune reconstitution between courses, rather than continuous immunosuppression. This "hit-and-reconstitute" profile contrasts with chronic immunosuppressants and is the basis of the intermittent oral dosing schedule used in relapsing MS.
How does lymphocyte recovery occur after Cladribine treatment?
After cladribine-induced lymphocyte depletion, circulating lymphocyte counts gradually recover over months as bone-marrow output and peripheral repopulation resume. Recovery is monitored clinically; the intermittent Mavenclad dosing is designed so nadir immunosuppression is followed by reconstitution, minimizing cumulative risk while maintaining disease control.
How should Cladribine be dissolved and stored for research use?
Cladribine is soluble in water (~6.35 g/L) and DMSO. Prepare aqueous or DMSO stock solutions for cell-based assays, keeping osmolarity and DMSO limits appropriate. Store powder at 0-4°C short term, -20°C long term, protected from moisture. Always research-use-only; not for human or clinical consumption.
Is QC documentation provided with each batch?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity (≥98%), NMR structural confirmation, and MS data. MSDS/SDS, solubility datasheets, and Certificates of Origin are available on request. Qualified institutions may request sample evaluation — please contact us for details.

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Research-grade Cladribine (CAS 4291-63-8) — purity ≥98%, COA included
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