Home Neuronal Signaling Adenosine Deaminase inhibitor - DNA/RNA Synthesis inhibitor Cladribine For research use only.

Cladribine

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

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

Cladribine Chemical Structure

CAS No. 4291-63-8

Purity & Quality Control

Cladribine Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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
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 --

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)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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