Cat. No.: HY-13599

Cladribine

(Synonyms: 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA)

9 Cited Publications

Customer Review

Based on 9 publication(s) in Google Scholar

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.

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

Purity: 99.96%
CAS No.: 4291-63-8
Formula: C₁₀H₁₂ClN₅O₃
Molecular Weight:285.69

Storage:

4°C, protect from light

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

Cladribine Chemical Structure

CAS No.: 4291-63-8

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

Adenosine deaminase^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
BJ	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human BJ cells after 3 days by MTT assay Cytotoxicity against human BJ cells after 3 days by MTT assay	[PMID: 21711054]
BT-549	IC₅₀	0.123 μM Compound: Cladribine	Cytotoxicity against human BT549 cells after 3 days by MTT assay Cytotoxicity against human BT549 cells after 3 days by MTT assay	[PMID: 21711054]
BV-173	IC₅₀	0.0008 μM Compound: Cladribine	Cytotoxicity against human BV173 cells after 3 days by MTT assay Cytotoxicity against human BV173 cells after 3 days by MTT assay	[PMID: 21711054]
BV-173	IC₅₀	0.8 nM Compound: Cladribine	Cytotoxicity against human BV173 cells after 3 days by MTT assay Cytotoxicity against human BV173 cells after 3 days by MTT assay	[PMID: 21711054]
C6	IC₅₀	9.07 μM Compound: Cladribine	Cytotoxicity against rat C6 cells after 3 days by MTT assay Cytotoxicity against rat C6 cells after 3 days by MTT assay	[PMID: 21711054]
CCRF-CEM	IC₅₀	0.003 μM Compound: Table I Row 5	Compound was tested for cytotoxicity against CCRF-CEM cell lines Compound was tested for cytotoxicity against CCRF-CEM cell lines	[PMID: 1732556]
CCRF-CEM	IC₅₀	0.0005 μM Compound: Cladribine	Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay	[PMID: 21840722]
CCRF-CEM	IC₅₀	0.5 nM Compound: Cladribine	Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay	[PMID: 21840722]
CCRF-CEM	IC₅₀	0.003 μM Compound: 467	Anticancer activity against human CCRF-CEM cells Anticancer activity against human CCRF-CEM cells	[PMID: 34213340]
CT26	IC₅₀	0.131 μM Compound: Cladribine	Cytotoxicity against mouse CT26 cells after 3 days by MTT assay Cytotoxicity against mouse CT26 cells after 3 days by MTT assay	[PMID: 21711054]
EL4	IC₅₀	0.848 μM Compound: Cladribine	Cytotoxicity against mouse EL4 cells after 3 days by MTT assay Cytotoxicity against mouse EL4 cells after 3 days by MTT assay	[PMID: 21711054]
HCT-116	IC₅₀	9.43 μM Compound: Cladribine	Cytotoxicity against human HCT116 cells after 3 days by MTT assay Cytotoxicity against human HCT116 cells after 3 days by MTT assay	[PMID: 21711054]
HCT-116	IC₅₀	0.3 μM Compound: Cladribine	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 25462277]
HCT-116	IC₅₀	0.3 μM Compound: Cladribine	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 28219046]
HCT-116	IC₅₀	<0.1 μM Compound: Cladribine	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 29326016]
HCT-116	IC₅₀	<0.1 μM Compound: Cladribine	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
HCT-116	IC₅₀	<0.1 μM Compound: Cladribine	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
HeLa	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human HeLa cells after 3 days by MTT assay Cytotoxicity against human HeLa cells after 3 days by MTT assay	[PMID: 21711054]
Hep 3B2	IC₅₀	0.1 μM Compound: Cladribine	Cytotoxicity against human Hep3B cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human Hep3B cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
Hep 3B2	IC₅₀	0.1 μM Compound: Cladribine	Cytotoxicity against human Hep3B cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human Hep3B cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
HEp-2	IC₅₀	0.03 μM Compound: Table I Row 5	Compound was tested for cytotoxicity against HEp-2 cell lines Compound was tested for cytotoxicity against HEp-2 cell lines	[PMID: 1732556]
HEp-2	IC₅₀	0.03 μM Compound: 467	Anticancer activity against human HEp-2 cells Anticancer activity against human HEp-2 cells	[PMID: 34213340]
HepG2	IC₅₀	0.04 μM Compound: Cladribine	Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay	[PMID: 29326016]
HepG2	IC₅₀	0.4 μM Compound: Cladribine	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
HepG2	IC₅₀	0.4 μM Compound: Cladribine	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
HPAC	IC₅₀	9.32 μM Compound: Cladribine	Cytotoxicity against human HPAC cells after 3 days by MTT assay Cytotoxicity against human HPAC cells after 3 days by MTT assay	[PMID: 21711054]
HT-29	IC₅₀	9.44 μM Compound: Cladribine	Cytotoxicity against human HT-29 cells after 3 days by MTT assay Cytotoxicity against human HT-29 cells after 3 days by MTT assay	[PMID: 21711054]
Huh-7	IC₅₀	1.8 μM Compound: Cladribine	Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay	[PMID: 25462277]
Huh-7	IC₅₀	1.8 μM Compound: Cladribine	Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 28219046]
Huh-7	IC₅₀	0.4 μM Compound: Cladribine	Antiproliferative activity against human HuH7 cells after 72 hrs by SRB assay Antiproliferative activity against human HuH7 cells after 72 hrs by SRB assay	[PMID: 29326016]
Huh-7	IC₅₀	0.6 μM Compound: Cladribine	Cytotoxicity against human Huh-7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human Huh-7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
Huh-7	IC₅₀	0.9 μM Compound: Cladribine	Cytotoxicity against human Huh-7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human Huh-7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
K562	IC₅₀	0.17 μM Compound: Cladribine	Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay	[PMID: 21711054]
K562	IC₅₀	7.69 μM Compound: Cladribine	Cytotoxicity against human K562 cells after 3 days by MTT assay Cytotoxicity against human K562 cells after 3 days by MTT assay	[PMID: 21711054]
K562	IC₅₀	10 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
KG-1	IC₅₀	0.2 μM Compound: 1	Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
L1210	IC₅₀	0.07 μM Compound: Table I Row 5	Compound was tested for cytotoxicity against L1210 cell lines Compound was tested for cytotoxicity against L1210 cell lines	[PMID: 1732556]
L1210	IC₅₀	0.393 μM Compound: Cladribine	Cytotoxicity against mouse L1210 cells after 3 days by MTT assay Cytotoxicity against mouse L1210 cells after 3 days by MTT assay	[PMID: 21711054]
L1210	IC₅₀	0.07 μM Compound: 467	Anticancer activity against mouse L1210 cells Anticancer activity against mouse L1210 cells	[PMID: 34213340]
LNCaP	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human LNCAP cells after 3 days by MTT assay Cytotoxicity against human LNCAP cells after 3 days by MTT assay	[PMID: 21711054]
Mahlavu	IC₅₀	0.1 μM Compound: Cladribine	Antiproliferative activity against human Mahlavu cells after 72 hrs by SRB assay Antiproliferative activity against human Mahlavu cells after 72 hrs by SRB assay	[PMID: 29326016]
Mahlavu	IC₅₀	<0.1 μM Compound: Cladribine	Cytotoxicity against human Mahlavu cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human Mahlavu cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
Mahlavu	IC₅₀	<0.1 μM Compound: Cladribine	Cytotoxicity against human Mahlavu cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human Mahlavu cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
MCF7	IC₅₀	2.35 μM Compound: Cladribine	Cytotoxicity against human MCF7 cells after 3 days by MTT assay Cytotoxicity against human MCF7 cells after 3 days by MTT assay	[PMID: 21711054]
MCF7	IC₅₀	45 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
MCF7	IC₅₀	2 μM Compound: Cladribine	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 28219046]
MCF7	IC₅₀	2 μM Compound: Cladribine	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 29326016]
MCF7	IC₅₀	2 μM Compound: Cladribine	Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
MCF7	IC₅₀	2.4 μM Compound: Cladribine	Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
MDA-MB-231	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human MDA-MB-231 cells after 3 days by MTT assay Cytotoxicity against human MDA-MB-231 cells after 3 days by MTT assay	[PMID: 21711054]
MES-SA	IC₅₀	0.165 μM Compound: Cladribine	Cytotoxicity against human MES-SA cells after 3 days by MTT assay Cytotoxicity against human MES-SA cells after 3 days by MTT assay	[PMID: 21711054]
MOLT-3	IC₅₀	2.3 μM Compound: 1	Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
NCI-H146	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human NCI-H146 cells after 3 days by MTT assay Cytotoxicity against human NCI-H146 cells after 3 days by MTT assay	[PMID: 21711054]
P388D1	IC₅₀	0.285 μM Compound: Cladribine	Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay	[PMID: 21711054]
PC-3	IC₅₀	8.28 μM Compound: Cladribine	Cytotoxicity against human PC3 cells after 3 days by MTT assay Cytotoxicity against human PC3 cells after 3 days by MTT assay	[PMID: 21711054]
PLC	IC₅₀	9.1 μM Compound: Cladribine	Cytotoxicity against human PLC cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human PLC cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
PLC	IC₅₀	9.1 μM Compound: Cladribine	Cytotoxicity against human PLC cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human PLC cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
Raji	IC₅₀	0.009 μM Compound: Cladribine	Cytotoxicity against human Raji cells after 72 hrs by MTT assay Cytotoxicity against human Raji cells after 72 hrs by MTT assay	[PMID: 21840722]
RPMI-8226	IC₅₀	6 μM Compound: 1	Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
SAOS-2	IC₅₀	>=50 μM Compound: 2	Cytotoxicity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay Cytotoxicity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay	[PMID: 36917882]
SK-HEP1	IC₅₀	4 μM Compound: 1	Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
SK-MEL-2	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human SK-MEL-2 cells after 3 days by MTT assay Cytotoxicity against human SK-MEL-2 cells after 3 days by MTT assay	[PMID: 21711054]
SK-N-AS	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human SK-N-AS cells after 3 days by MTT assay Cytotoxicity against human SK-N-AS cells after 3 days by MTT assay	[PMID: 21711054]
SK-OV-3	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human SKOV3 cells after 3 days by MTT assay Cytotoxicity against human SKOV3 cells after 3 days by MTT assay	[PMID: 21711054]
Skut1B	IC₅₀	1 μM Compound: 1	Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]
SNU-182	IC₅₀	23.3 μM Compound: Cladribine	Cytotoxicity against human SNU-182 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-182 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
SNU-182	IC₅₀	23.3 μM Compound: Cladribine	Cytotoxicity against human SNU-182 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-182 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
SNU-387	IC₅₀	7.1 μM Compound: Cladribine	Cytotoxicity against human SNU-387 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-387 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
SNU-387	IC₅₀	7.1 μM Compound: Cladribine	Cytotoxicity against human SNU-387 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-387 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
SNU-398	IC₅₀	<0.1 μM Compound: Cladribine	Cytotoxicity against human SNU-398 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-398 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
SNU-398	IC₅₀	<0.1 μM Compound: Cladribine	Cytotoxicity against human SNU-398 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-398 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
SNU-423	IC₅₀	6.7 μM Compound: Cladribine	Cytotoxicity against human SNU-423 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-423 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
SNU-423	IC₅₀	6.7 μM Compound: Cladribine	Cytotoxicity against human SNU-423 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-423 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
SNU-449	IC₅₀	37.3 μM Compound: Cladribine	Cytotoxicity against human SNU-449 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-449 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
SNU-449	IC₅₀	37.3 μM Compound: Cladribine	Cytotoxicity against human SNU-449 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-449 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38688437]
SNU-475	IC₅₀	2.5 μM Compound: Cladribine	Cytotoxicity against human SNU-475 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Cytotoxicity against human SNU-475 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 38107180]
SNU-475	IC₅₀	2.5 μM Compound: Cladribine	Cytotoxicity against human SNU-475 cells assessed as cell growth inhibition by SRB assay Cytotoxicity against human SNU-475 cells assessed as cell growth inhibition by SRB assay	[PMID: 38688437]
T47D	IC₅₀	0.7 μM Compound: Cladribine	Cytotoxicity against human T47D cells after 72 hrs by SRB assay Cytotoxicity against human T47D cells after 72 hrs by SRB assay	[PMID: 25462277]
TC-32	IC₅₀	2.92 μM Compound: 2	Cytotoxicity against human TC-32 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay Cytotoxicity against human TC-32 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay	[PMID: 36917882]
U2OS	IC₅₀	>=50 μM Compound: 2	Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Blue reagent based luminescence assay	[PMID: 36917882]
U-87MG ATCC	IC₅₀	>10 μM Compound: Cladribine	Cytotoxicity against human U87MG cells after 3 days by MTT assay Cytotoxicity against human U87MG cells after 3 days by MTT assay	[PMID: 21711054]
ZR-75-1	IC₅₀	>100 μM Compound: 1	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 25960323]

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 IC₅₀s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively^[2].

MedChemExpress (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].

MedChemExpress (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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 4291-63-8
Appearance Solid
Molecular Weight 285.69
Formula C₁₀H₁₂ClN₅O₃
Color White to off-white
SMILES

OC[C@@H]1[C@@H](O)C[C@H](N2C=NC3=C2N=C(Cl)N=C3N)O1
Synonyms

2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Publications (9)

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Cell Stem Cell

Leukemic stem cell subtypes determine venetoclax resistance and therapeutic vulnerabilities in AML. [Abstract]

2026 Jun 4;33(6):982-999.e8. PMID: 42102807
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Nano Lett

Nanopore Signatures of Nucleoside Drugs. [Abstract]

2023 Oct 25;23(20):9437-9444. PMID: 37818841
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Molecules

Facilitating Anti-Cancer Combinatorial Drug Discovery by Targeting Epistatic Disease Genes. [Abstract]

2018 Mar 23;23(4). pii: E736. PMID: 29570606
Sci Rep

A novel human acute myeloid leukemia cell line SDEY-AML1 with KMT2A: MLLT3, IKZF1: EVX1 fusions exhibits high tumorigenicity in NSG mice. [Abstract]

2026 Feb 8;16(1):7792. PMID: 41656387

Cladribine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2026 Feb 8;16(1):7792. [Abstract]

Testing the sensitivity of Chidamide, LBH589, S63845, Olverembatinib, Cladribine, Afatinib to SDEY-AML1.
Chem Pharm Bull (Tokyo)

Synergistic Activity of an Antimetabolite Drug and Tyrosine Kinase Inhibitors against Breast Cancer Cells. [Abstract]

2017 Aug 1;65(8):768-775. PMID: 28539531

Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]

Changes in Bcl-2 protein expression in MCF-7 cells after treatment with Cladribine, Dasatinib or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]

Cladribine (0, 20, 40, 60, 80 μM; 48 h) showed cytotoxicity in MCF-7 cells.

Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]

Cladribine (15 µM; 48 h) induced apoptosis in MCF-7 Cells.

Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]

Cladribine (15 µM; 48 h) induced apoptosis in MCF-7 Cells. Nuclear morphology of apoptotic cells with condense/fragmented nuclei (shown with arrows).

Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]

Cladribine (15 µM; 12 h) increased intracellular Reactive Oxygen Species (ROS) generation in MCF-7 Cells.

Cladribine purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775. [Abstract]

Cladribine (15 µM; 12 h) decreased mitochondrial membrane potential (ΔΨm) in MCF-7 Cells.
Research Square Preprint

2024 Aug 19.

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (700.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (7.00 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (17.50 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 2 mg/mL (7.00 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 2 mg/mL (7.00 mM); Clear solution; Need ultrasonic and warming and heat to 50°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Linyan Xu, et al. Cladribine Induces ATF4 Mediated Apoptosis and Synergizes with SAHA in Diffuse Large B-Cell Lymphoma Cells. Int J Med Sci. 2020; 17(10): 1375–1384. [Content Brief]

[2]. Jian Ma, et al. Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer. 2011 Jun 16;11:255. [Content Brief]

[3]. Young Seop Chang, et al. MP28-10 COMBINED EFFECTS OF MELATONIN AND CLADRIBINE ON APOPTOSIS IN ISCHEMIA/REPERFUSION INJURY IN RAT BLADDER. THE JOURNAL OF UROLOGY. April 2016. 195 (4S): e375.

[4]. Crystal D Hayes, et al. Chronic cladribine administration increases amyloid beta peptide generation and plaque burden in mice. PLoS One. 2012;7(10):e45841. [Content Brief]

[5]. Yeung, P. K. F., et al. Pharmacokinetics of Cladribine in a Rat Model Following Subcutaneous and Intra-arterial Injections. Drug Metabol Drug Interact. 2008;23(3-4):291-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	3.5003 mL	17.5015 mL	35.0030 mL	87.5074 mL
H₂O / DMSO	5 mM	0.7001 mL	3.5003 mL	7.0006 mL	17.5015 mL
DMSO	10 mM	0.3500 mL	1.7501 mL	3.5003 mL	8.7507 mL
	15 mM	0.2334 mL	1.1668 mL	2.3335 mL	5.8338 mL
	20 mM	0.1750 mL	0.8751 mL	1.7501 mL	4.3754 mL
	25 mM	0.1400 mL	0.7001 mL	1.4001 mL	3.5003 mL
	30 mM	0.1167 mL	0.5834 mL	1.1668 mL	2.9169 mL
	40 mM	0.0875 mL	0.4375 mL	0.8751 mL	2.1877 mL
	50 mM	0.0700 mL	0.3500 mL	0.7001 mL	1.7501 mL
	60 mM	0.0583 mL	0.2917 mL	0.5834 mL	1.4585 mL
	80 mM	0.0438 mL	0.2188 mL	0.4375 mL	1.0938 mL
	100 mM	0.0350 mL	0.1750 mL	0.3500 mL	0.8751 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Cladribine

Apoptosis Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Nucleotide Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Endoplasmic Reticulum Stress Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Blood Cancer Compound Library

Rare Diseases Drug Library

Chemotherapy Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Withdrawn Drug Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

MCE Kinase Hinge Binder Fragment Library

Publications Citing Use of MedChemExpress (MCE) Cladribine

Biological Activity

Chemical Information

Publications (9)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Cladribine Related Classifications

Cat. No.: HY-13599