Cladribine

For research use only.

Catalog No.S1199 Synonyms: 2-CdA, 2-chlorodeoxyadenosine

8 publications

Cladribine Chemical Structure

CAS No. 4291-63-8

Cladribine (2-CdA, 2-chlorodeoxyadenosine) 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.

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Selleck's Cladribine has been cited by 8 publications

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Biological Activity

Description Cladribine (2-CdA, 2-chlorodeoxyadenosine) 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CCRF-CEM cell lines NYWxUGxsS3m2b4TvfIlkcXS7IHHzd4F6 MoLjR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgR2NTTi2FRV2gZ4VtdCCuaX7ld{whUUN3ME2wMlAxOyEQvF2= NV3kNYZjOTd|MkW1Oi=>
HEp-2 cell lines MXPDfZRwfG:6aXPpeJkh[XO|YYm= MV7Dc41xd3WwZDD3ZZMhfGW|dHXkJIZweiCleYTveI95cWOrdImgZYdicW6|dDDISZAuOiClZXzsJIxqdmW|LDDJR|UxRTBwMEOg{txO NFvORpIyPzN{NUW2
L1210 cell lines MoTtR5l1d3SxeHnjbZR6KGG|c3H5 NXjX[VVjS2:vcH;1coQhf2G|IITld5Rm\CCob4KgZ5l1d3SxeHnjbZR6KGGpYXnud5QhVDF{MUCgZ4VtdCCuaX7ld{whUUN3ME2wMlA4KM7ebR?= MYCxO|MzPTV4
human K562 cells NVnr[WJDS3m2b4TvfIlkcXS7IHHzd4F6 MWWzJIRigXN? MnjyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUeuOlkh|ryP M3LKT|IyPzFzMEW0
CEM-DNR-bulk cells NWr1doo5S3m2b4TvfIlkcXS7IHHzd4F6 Ml3iN{Bl[Xm| NH;sW|REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBETU1vRF7SMYJ2dGtiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlM2OiEQvF2= NIW5[2czOTdzMUC1OC=>
mouse L1210 cells NUP5dlhbS3m2b4TvfIlkcXS7IHHzd4F6 M3;NNFMh\GG7cx?= MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDMNVIyOCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN|k{KM7:TR?= M3THcVIyPzFzMEW0
mouse EL4 cells M1q1OGN6fG:2b4jpZ4l1gSCjc4PhfS=> NUWxSo9vOyCmYYnz NILzNXpEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBGVDRiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg1QCEQvF2= MmjWNlE4OTFyNUS=
human MCF7 cells M1PKdWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVXjPWRyOyCmYYnz NFrDS4VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9Nk4{PSEQvF2= NXL1VXYzOjF5MUGwOVQ>
BT549 cells NGTFdpVEgXSxdH;4bYNqfHliYYPzZZk> NV\SSXM{OyCmYYnz MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFU1QSClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNVI{KM7:TR?= M2K3RlIyPzFzMEW0
rat C6 cells M2fGS2N6fG:2b4jpZ4l1gSCjc4PhfS=> NVTifZpCOyCmYYnz NWDPSlNvS3m2b4TvfIlkcXS7IHHnZYlve3RicnH0JGM3KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;OT6wO{DPxE1? NXnycndmOjF5MUGwOVQ>
human HT-29 cells MlvSR5l1d3SxeHnjbZR6KGG|c3H5 NH3kbmE{KGSjeYO= MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUmuOFQh|ryP NH\0WI8zOTdzMUC1OC=>
human HCT116 cells MnTFR5l1d3SxeHnjbZR6KGG|c3H5 MnH6N{Bl[Xm| Mm\KR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9PU41OyEQvF2= M3vi[FIyPzFzMEW0
mouse CT26 cells Ml\GR5l1d3SxeHnjbZR6KGG|c3H5 M{\ZdVMh\GG7cx?= Mkj6R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgR3QzPiClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNVMyKM7:TR?= NU\TbFdPOjF5MUGwOVQ>
human PC3 cells MnuwR5l1d3SxeHnjbZR6KGG|c3H5 MYizJIRigXN? NF[5dWtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME24MlI5KM7:TR?= MUKyNVcyOTB3NB?=
MES-SA cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= NYLuWHZwOyCmYYnz NYPz[pd1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUWVLWPBJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XluIFnDOVA:OC5zNkWg{txO NVHhZpg4OjF5MUGwOVQ>
human HPAC cells NIrxTFdEgXSxdH;4bYNqfHliYYPzZZk> M2jKbVMh\GG7cx?= M2TUWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhRSUNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlMzKM7:TR?= MlfkNlE4OTFyNUS=
mouse P388D1 cells NXzQeGw4S3m2b4TvfIlkcXS7IHHzd4F6 M1LQUFMh\GG7cx?= MojGR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFM5QERzIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4zQDVizszN MUKyNVcyOTB3NB?=
CCRF-CEM cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= NHTWN3A4OiCq NVzHRVRRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0OURj3DSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCwNFUh|ryP M3OzbFIyQDRyN{Ky
human Raji cells NGHyUWlEgXSxdH;4bYNqfHliYYPzZZk> M{T6c|czKGh? MmH0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVoFrcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFA6KM7:TR?= NYSyOWxqOjF6NEC3NlI>
human HuH7 cells MnjRR5l1d3SxeHnjbZR6KGG|c3H5 NWPIVYFjPzJiaB?= NIfIV|REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NU45KM7:TR?= M{S5S|I2PDZ{Mke3
human T47D cells M4LIfGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{\XeFczKGh? MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD63JO69VQ>? M3vr[lI2PDZ{Mke3
human HCT116 cells MlvvR5l1d3SxeHnjbZR6KGG|c3H5 MnK2O|IhcA>? NYnVXllmS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5|IN88US=> M1W5blI2PDZ{Mke3
human K562 cells NUDhcpl7WHKxbHnm[ZJifGmxbjDhd5NigQ>? NYq4VlV3PDhiaB?= NHXyWFhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFyIN88US=> NFmwOGwzPTl4MEOyNy=>
human SKHEP1 cells NUXHZplpWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF;vXpM1QCCq MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONSFXQNUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PCEQvF2= NV[2Zo5rOjV7NkCzNlM>
human MOLT3 cells NXv1WW1zWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4S4ZVQ5KGh? NHXHfW5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{LkOg{txO NVz6cFdOOjV7NkCzNlM>
human KG1 cells NV3BeXpCWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWO0PEBp Mn;URY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNR{GgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOiEQvF2= M4q0PVI2QTZyM{Kz
human RPMI8226 cells Mlr3VJJwdGmoZYLheIlwdiCjc4PhfS=> MlHuOFghcA>? NU\CXJJYSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OkDPxE1? MYSyOVk3ODN{Mx?=
human MCF7 cells M1vpd3Bzd2yrZnXyZZRqd25iYYPzZZk> NWXpdXNHPDhiaB?= MmXlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01PSEQvF2= NETTTpYzPTl4MEOyNy=>
human SK-UT-1B cells NFnid21Rem:uaX\ldoF1cW:wIHHzd4F6 Ml7kOFghcA>? NXXDTXd5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1WXC1zQjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? Mnm4NlU6PjB|MkO=
L1210 cell lines MXzGeY5kfGmxbjDhd5NigQ>? MmHRTY4hfmm2cn:gbY5pcWKrdH;yfUBm\m[nY4Sge4F{KHSnc4Tl[EBnd3JiY4n0c5N1[XSrYzDhZ5Rqfmm2eTDvckB1cGViZ4Lve5RpKG:oIH31dolv\SCuZYXr[Y1q[yCOMUKxNEBk\WyuIHzpcoV{NCCLREWwQVAvODNizszN MnjONlk6PTZ4Nh?=
P388 leukemic cell lines M2O3SGZ2dmO2aX;uJIF{e2G7 NFvHTlhKdiC4aYTyc{BqdmirYnn0c5J6KGWoZnXjeEB4[XNidHXzeIVlKG[xcjDjfZRwe3SjdHnjJIFkfGm4aYT5JI9vKHSqZTDndo94fGhib3[gcJlueGixaXSgcoVweGyjc32gVFM5QCCuZYXr[Y1q[yClZXzsJIxqdmW|LDDJSFUxRTBwMEOg{txO MofQNlk6PTZ4Nh?=
human BV173 cells M2HiZ2N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml;aN{Bl[Xm| NFjtZY1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXjF5MzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODByODFOwG0> MVuyNVcyOTB3NB?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research:[1]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[5]
- Collapse
  • Animal Models: Adult wild-type (AB) zebrafish
  • Dosages: 0.7 mM - 3.5 mM
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (199.51 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+1% Tween 80+H2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 285.69
Formula

C10H12ClN5O3

CAS No. 4291-63-8
Storage powder
in solvent
Synonyms 2-CdA, 2-chlorodeoxyadenosine
Smiles C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04121065 Not yet recruiting Procedure: Blood withdrawal Relapsing Multiple Sclerosis Neuromed IRCCS January 2020 --
NCT03963375 Recruiting Drug: Cladribine Multiple Sclerosis|Multiple Sclerosis Relapsing-Remitting Washington University School of Medicine|EMD Serono October 28 2019 Phase 4
NCT03933202 Recruiting Drug: Cladribine Tablets Multiple Sclerosis EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono July 22 2019 --
NCT03933215 Recruiting Drug: Cladribine Tablets Multiple Sclerosis EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono May 21 2019 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID