Choose Your Country or Region

Cladribine

Name: Cladribine
Brand: Selleck Chemicals
SKU: S1199
Rating: 5 (25 reviews)

Synonyms: 2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251

Catalog No.S1199 Purity:99.99%

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.

Cladribine Chemical Structure

CAS No. 4291-63-8

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Cladribine Related Products

Related Compound Libraries	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
CCRF-CEM cell lines	Cytotoxicity assay		Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM	1732556
HEp-2 cell lines	Cytotoxicity assay		Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.03 μM	1732556
L1210 cell lines	Cytotoxicity assay		Compound was tested for cytotoxicity against L1210 cell lines, IC50=0.07 Μm	1732556
CCRF-CEM cells	Cytotoxicity assay	72 h	Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM	21840722
human Raji cells	Cytotoxicity assay	72 h	Cytotoxicity against human Raji cells after 72 hrs by MTT assay, IC50=0.009 μM	21840722
human HuH7 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay, IC50=1.8 μM	25462277
human T47D cells	Cytotoxicity assay	72 h	Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50=0.7 μM	25462277
human HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.3 μM	25462277
human K562 cells	Proliferation assay	48 h	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=10 μM	25960323
human SKHEP1 cells	Proliferation assay	48 h	Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=4 μM	25960323
human MOLT3 cells	Proliferation assay	48 h	Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2.3 μM	25960323
human KG1 cells	Proliferation assay	48 h	Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.2 μM	25960323
human RPMI8226 cells	Proliferation assay	48 h	Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM	25960323
human MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=45 μM	25960323
human SK-UT-1B cells	Proliferation assay	48 h	Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=1 μM	25960323
L1210 cell lines	Function assay		In vitro inhibitory effect was tested for cytostatic activity on the growth of murine leukemic L1210 cell lines, ID50=0.03 μM	2995666
P388 leukemic cell lines	Function assay		In vitro inhibitory effect was tested for cytostatic activity on the growth of lymphoid neoplasm P388 leukemic cell lines, ID50=0.03 μM	2995666
BV173	Cytotoxicity assay	3 days	Cytotoxicity against human BV173 cells after 3 days by MTT assay, IC50=0.0008μM	21711054
BT549	Cytotoxicity assay	3 days	Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123μM	21711054
CT26	Cytotoxicity assay	3 days	Cytotoxicity against mouse CT26 cells after 3 days by MTT assay, IC50=0.131μM	21711054
MES-SA	Cytotoxicity assay	3 days	Cytotoxicity against human MES-SA cells after 3 days by MTT assay, IC50=0.165μM	21711054
K562	Cytotoxicity assay	3 days	Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay, IC50=0.17μM	21711054
P388D1	Cytotoxicity assay	3 days	Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay, IC50=0.285μM	21711054
CEM-DNR-bulk	Cytotoxicity assay	3 days	Cytotoxicity against human CEM-DNR-bulk cells after 3 days by MTT assay, IC50=0.352μM	21711054
L1210	Cytotoxicity assay	3 days	Cytotoxicity against mouse L1210 cells after 3 days by MTT assay, IC50=0.393μM	21711054
EL4	Cytotoxicity assay	3 days	Cytotoxicity against mouse EL4 cells after 3 days by MTT assay, IC50=0.848μM	21711054
MCF7	Cytotoxicity assay	3 days	Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=2.35μM	21711054
K562	Cytotoxicity assay	3 days	Cytotoxicity against human K562 cells after 3 days by MTT assay, IC50=7.69μM	21711054
PC3	Cytotoxicity assay	3 days	Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=8.28μM	21711054
C6	Cytotoxicity assay	3 days	Cytotoxicity against rat C6 cells after 3 days by MTT assay, IC50=9.07μM	21711054
HPAC	Cytotoxicity assay	3 days	Cytotoxicity against human HPAC cells after 3 days by MTT assay, IC50=9.32μM	21711054
HCT116	Cytotoxicity assay	3 days	Cytotoxicity against human HCT116 cells after 3 days by MTT assay, IC50=9.43μM	21711054
HT-29	Cytotoxicity assay	3 days	Cytotoxicity against human HT-29 cells after 3 days by MTT assay, IC50=9.44μM	21711054
HCT116	Cytotoxicity assay	72 hrs	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=0.3μM	28219046
HuH7	Cytotoxicity assay	72 hrs	Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=1.8μM	28219046
MCF7	Cytotoxicity assay	72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=2μM	28219046
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Click to View More Cell Line Experimental Data

Biological Activity

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.

Targets

Adenosine deaminase (MM1.S cells) ^[1]	Adenosine deaminase (RPMI8226 cells) ^[1]	Adenosine deaminase (U266 cells) ^[1]
0.18 μM	0.75 μM	2.43 μM

In vitro
In vitro	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. ^[1] Cladribine possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells. ^[2] 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. ^[3] Cladribine decreases the migratory capacity of CD14⁺ monocytes, as well as of CD4⁺ and CD8⁺ T lymphocytes. ^[4]
Cell Research	Cell lines	U266, RPMI8226 and MM1.S
	Concentrations	0 μM - 32 μM
	Incubation Time	72 hours
	Method	The non-radioactive cell proliferation kit is used to determine cell viability. In brief, Human MM cell line U266, RPMI8226 and MM1.S are seeded onto 96-well plates with either 0.1 mL complete medium (5% FBS) as control, or 0.1 mL of the same medium containing a series of doses of cladribine, and incubated for 72 hours. After reading all wells at 490 nm with a micro-plate reader, the percentages of surviving cells from each group relative to controls, defined as 100% survival, are determined by reduction of MTS.

In Vivo
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. ^[5] 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. ^[6]
Animal Research	Animal Models	Adult wild-type (AB) zebrafish
	Dosages	0.7 mM - 3.5 mM
	Administration	Administered via i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05797740	Recruiting	Multiple Sclerosis	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany	August 3 2023	--
NCT04997148	Completed	Relapsing-Remitting Multiple Sclerosis	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany\|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany	August 11 2021	--

References

+ Expand

Chemical Information & Solubility

Molecular Weight	285.69	Formula	C₁₀H₁₂ClN₅O₃
CAS No.	4291-63-8	SDF	Download Cladribine SDF
Smiles	C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 57 mg/mL ( (199.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 30%PEG300 2 1%Tween80 3 64%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (35.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 10 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 640 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):