[CAS NO. 4291-63-8]  Cladribine

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PRODUCTS SPECIFICATIONS [4291-63-8]

Catelog
HY-13599
Brand
MCE
CAS
4291-63-8

DESCRIPTION [4291-63-8]

Overview

MDLMFCD00153939
Molecular Weight285.69
Molecular FormulaC10H12ClN5O3
SMILESOC[C@H]1O[C@@H](N2C=NC3=C2N=C(N=C3N)Cl)C[C@@H]1O

For research use only. We do not sell to patients.


Summary

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] .


IC50 & Target

Adenosine deaminase [2]


In Vitro

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 IC 50 s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively [2] .

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

Cell Proliferation Assay [1]

Cell Line: The human DLBCL cell lines (U2932, OCI-LY10, SUDHL2, WSU-DLCL2, DB)
Concentration: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours, 48 hours
Result: Exhibited notable suppression of cell proliferation in five DLBCL cells.

Western Blot Analysis [1]

Cell Line: U2932 cells, WSU-DLCL2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Decreased the expressions of Cyclin D1 and Cyclin E, and increased the expressions of p21 and p27.

Apoptosis Analysis [1]

Cell Line: U2932 cells, WSU-DLCL2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Induced apoptosis and activates exogenous and endogenous apoptotic signaling pathways.

Cell Cycle Analysis [1]

Cell Line: U2932 cells, WSU-DLCL2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Caused G1 phase arrest.

RT-PCR [1]

Cell Line: U2932 cells, WSU-DLCL2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Activated ER stress.

In Vivo

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] .

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

Animal Model: Male Sprague-Dawley rats, ischemic injury model [3]
Dosage: 10 μg/kg
Administration: Intraperitoneal injection, 3 times/week, for 2 weeks
Result: Might increase expression of Sphk1 and consecutively SphK1 suppressed HIF-1α.
Animal Model: Male Sprague Dawley rats (350-450 g) [5]
Dosage: 2 mg/kg for s.c., 1 mg/kg for i.a. (Pharmacokinetic Analysis)
Administration: Subcutaneous injection, intra-arterial
Result: C max (4.9 ng/mL i.a.; 1.1 ng/mL s.c.), T 1/2 β (3.5 h i.a.; 4.5 s.c.).

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04195945 Fred Hutchinson Cancer Center|Jazz Pharmaceuticals
Acute Myeloid Leukemia|Myeloid Neoplasm
March 11, 2020 Phase 2
NCT04550455 Keith Edwards, M.D.|EMD Serono|Multiple Sclerosis Center of Northeastern New York
Multiple Sclerosis
September 16, 2020 Phase 4
NCT03477500 Haukeland University Hospital
Multiple Sclerosis
March 21, 2018 Phase 3

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, protect from light

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


Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL ( 105.01 mM )

H 2 O : 10 mg/mL ( 35.00 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 25 mg/mL (87.51 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.


Synonyms

Adenosine, 2-chloro-2′-deoxy-
2-Chloro-2′-deoxyadenosine
2-Chloro-2′-deoxy-β-adenosine
2-Chloro-6-amino-9-(2-deoxy-β-D-erythro-pentofuranosyl)purine
2-Chlorodeoxyadenosine
NSC 105014-F
Cladribine
RWJ 26251
Leustatin
2-CdA
Cladarabine
NSC 105014
CldAdo
Jk 6251
Biodribin
Leustat
(2R,3S,5R)-5-(6-Amino-2-chloropurin-9-yl)-2-(hydroxymethyl)oxolan-3-ol
Vero-Cladribine
Mavenclad
Litak