Cladribine

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

Cladribine Chemical Structure

Molecular Weight(MW): 285.69

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.

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In DMSO USD 120 In stock
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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

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 Ml3YR5l1d3SxeHnjbZR6KGG|c3H5 M2fNU2NwdXCxdX7kJJdieyC2ZYP0[YQh\m:{IHP5eI91d3irY3n0fUBi\2GrboP0JGNEWkZvQ1XNJINmdGxibHnu[ZMtKEmFNUC9NE4xODNizszN Moj4NVc{OjV3Nh?=
HEp-2 cell lines M4H4UmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mof3R49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgTGVxNTJiY3XscEBtcW6nczygTWM2OD1yLkCzJO69VQ>? NFPmOlEyPzN{NUW2
L1210 cell lines MoXrR5l1d3SxeHnjbZR6KGG|c3H5 NIm5RolEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBNOTJzMDDj[YxtKGyrbnXzMEBKSzVyPUCuNFch|pyv MUSxO|MzPTV4
human K562 cells NV3nSpVWS3m2b4TvfIlkcXS7IHHzd4F6 MoTyN{Bl[Xm| M3TGXmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME23MlY6KM7:TR?= NFjVdFQzOTdzMUC1OC=>
CEM-DNR-bulk cells NWPqOI5VS3m2b4TvfIlkcXS7IHHzd4F6 NUTZPZRiOyCmYYnz MoH2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2VONUSQUj3ieYxsKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zOVIh|ryP M2LRflIyPzFzMEW0
mouse L1210 cells MmjiR5l1d3SxeHnjbZR6KGG|c3H5 M4rIRlMh\GG7cx?= M1fPfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGwyOjFyIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4{QTNizszN NXjTN4w1OjF5MUGwOVQ>
mouse EL4 cells NUjaW5lVS3m2b4TvfIlkcXS7IHHzd4F6 NVK0TlNGOyCmYYnz NUG5VItoS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhTUx2IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE45PDhizszN MlPNNlE4OTFyNUS=
human MCF7 cells MWfDfZRwfG:6aXPpeJkh[XO|YYm= M{frfFMh\GG7cx?= NIjGWmxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9Nk4{PSEQvF2= MWiyNVcyOTB3NB?=
BT549 cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= NEj1dpI{KGSjeYO= MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFU1QSClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNVI{KM7:TR?= NXzDeXhoOjF5MUGwOVQ>
rat C6 cells M1TNS2N6fG:2b4jpZ4l1gSCjc4PhfS=> MkT1N{Bl[Xm| MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBz[XRiQ{[gZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjB5IN88US=> M1;sOFIyPzFzMEW0
human HT-29 cells MVvDfZRwfG:6aXPpeJkh[XO|YYm= M1m4flMh\GG7cx?= M{HDWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9PU41PCEQvF2= M4TqUVIyPzFzMEW0
human HCT116 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= MlfUN{Bl[Xm| NFnFdWJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjR|IN88US=> NET4TG4zOTdzMUC1OC=>
mouse CT26 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= NX3TfZJTOyCmYYnz MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDDWFI3KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6xN|Eh|ryP NEjVeoczOTdzMUC1OC=>
human PC3 cells NV:wd4hXS3m2b4TvfIlkcXS7IHHzd4F6 M3TBVFMh\GG7cx?= NIrHSHNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME24MlI5KM7:TR?= MnXrNlE4OTFyNUS=
MES-SA cells NV64[otXS3m2b4TvfIlkcXS7IHHzd4F6 NV3lT2lSOyCmYYnz MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXMuW0FiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE3PSEQvF2= NGjpRWkzOTdzMUC1OC=>
human HPAC cells MWLDfZRwfG:6aXPpeJkh[XO|YYm= MXezJIRigXN? NHXWeYlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJWEGFIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9PU4{OiEQvF2= NFPZXFYzOTdzMUC1OC=>
mouse P388D1 cells NX;5RoNPS3m2b4TvfIlkcXS7IHHzd4F6 NUjUc285OyCmYYnz MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQN|g5TDFiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlI5PSEQvF2= M4PyRlIyPzFzMEW0
CCRF-CEM cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= M1vlWlczKGh? MnraR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjByMEWg{txO NHXDUJEzOTh2MEeyNi=>
human Raji cells M2qwWGN6fG:2b4jpZ4l1gSCjc4PhfS=> NInTRY04OiCq MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSZYpqKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNFkh|ryP NHTnU4UzOTh2MEeyNi=>
human HuH7 cells MXTDfZRwfG:6aXPpeJkh[XO|YYm= MmK2O|IhcA>? MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MT64JO69VQ>? NV71fog{OjV2NkKyO|c>
human T47D cells MUfDfZRwfG:6aXPpeJkh[XO|YYm= MWO3NkBp MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD63JO69VQ>? M1XBWFI2PDZ{Mke3
human HCT116 cells NWPDN2R5S3m2b4TvfIlkcXS7IHHzd4F6 NUfUeGc4PzJiaB?= Ml7WR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4{KM7:TR?= MlvCNlU1PjJ{N{e=
human K562 cells NXntVJNoWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2Kyd|Q5KGh? NUfXbnVuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zMDFOwG0> MW[yOVk3ODN{Mx?=
human SKHEP1 cells NH:0c2NRem:uaX\ldoF1cW:wIHHzd4F6 MkP5OFghcA>? NE\HVmdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLTGVROSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NDFOwG0> MWOyOVk3ODN{Mx?=
human MOLT3 cells M{fSPHBzd2yrZnXyZZRqd25iYYPzZZk> NFewb3Q1QCCq Ml3URY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi5|IN88US=> M3qzdFI2QTZyM{Kz
human KG1 cells M1K4PXBzd2yrZnXyZZRqd25iYYPzZZk> NYfNNollPDhiaB?= NWrMNZZ[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLS|Eh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMjFOwG0> MVOyOVk3ODN{Mx?=
human RPMI8226 cells MnO4VJJwdGmoZYLheIlwdiCjc4PhfS=> MVi0PEBp NY\1SnI5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OkDPxE1? NXjycXVuOjV7NkCzNlM>
human MCF7 cells M4\NdHBzd2yrZnXyZZRqd25iYYPzZZk> MYO0PEBp NVHmOnpoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12NTFOwG0> NX7tN5VyOjV7NkCzNlM>
human SK-UT-1B cells MoLpVJJwdGmoZYLheIlwdiCjc4PhfS=> NYfwVolJPDhiaB?= MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLWXUMVFDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zIN88US=> MV6yOVk3ODN{Mx?=
L1210 cell lines NGL3dIhHfW6ldHnvckBie3OjeR?= M2rSRmlvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDteZJqdmVibHX1b4VucWNiTEGyNVAh[2WubDDsbY5meyxiSVS1NF0xNjB|IN88US=> MnrYNlk6PTZ4Nh?=
P388 leukemic cell lines NEnVZoZHfW6ldHnvckBie3OjeR?= M1;kbGlvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDsfY1xcG:rZDDu[Y9xdGG|bTDQN|g5KGyndXvlcYlkKGOnbHygcIlv\XNuIFnEOVA:OC5yMzFOwG0> NX3sd2VyOjl7NU[2Oi=>
human BV173 cells NGLjVIFEgXSxdH;4bYNqfHliYYPzZZk> M1njbVMh\GG7cx?= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWlE4OyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFAxQCEQvF2= NXq1WXZjOjF5MUGwOVQ>

... 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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Adult wild-type (AB) zebrafish
  • Formulation: Saline
  • 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

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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 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 --
NCT03745144 Recruiting Drug: Cladribine|Drug: Placebo|Drug: Microgynon® Relapsing Multiple Sclerosis (RMS) Merck KGaA Darmstadt Germany January 17 2019 Phase 1
NCT03235973 Recruiting Drug: Fludarabine-Cladribine-Busulfan conditioning regimen Leukemia Myeloid Acute|Leukemia Lymphoblastic Acute Institut Paoli-Calmettes April 28 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID