Cladribine

For research use only.

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

4 publications

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 120 In stock
USD 97 In stock
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USD 490 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 MlHrR5l1d3SxeHnjbZR6KGG|c3H5 MmHiR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgR2NTTi2FRV2gZ4VtdCCuaX7ld{whUUN3ME2wMlAxOyEQvF2= Mm\MNVc{OjV3Nh?=
HEp-2 cell lines M1XBTmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn;KR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgTGVxNTJiY3XscEBtcW6nczygTWM2OD1yLkCzJO69VQ>? M4jlTVE4OzJ3NU[=
L1210 cell lines MX;DfZRwfG:6aXPpeJkh[XO|YYm= NFTpdXFEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBNOTJzMDDj[YxtKGyrbnXzMEBKSzVyPUCuNFch|pyv MXuxO|MzPTV4
human K562 cells MlT1R5l1d3SxeHnjbZR6KGG|c3H5 MofJN{Bl[Xm| M2fmPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME23MlY6KM7:TR?= M3TlWlIyPzFzMEW0
CEM-DNR-bulk cells Moq2R5l1d3SxeHnjbZR6KGG|c3H5 NUXZdpg4OyCmYYnz MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDSW0uTE6ULXL1cIsh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1yLkO1NkDPxE1? MoPpNlE4OTFyNUS=
mouse L1210 cells NYHGO21nS3m2b4TvfIlkcXS7IHHzd4F6 NUjGfXNROyCmYYnz M{jHd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGwyOjFyIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4{QTNizszN NEOxPXgzOTdzMUC1OC=>
mouse EL4 cells MnfDR5l1d3SxeHnjbZR6KGG|c3H5 M1rWeFMh\GG7cx?= MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDFUFQh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1yLki0PEDPxE1? MYWyNVcyOTB3NB?=
human MCF7 cells M3HVUWN6fG:2b4jpZ4l1gSCjc4PhfS=> NU\rT|dIOyCmYYnz NFjKUVlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9Nk4{PSEQvF2= NXXmNHM{OjF5MUGwOVQ>
BT549 cells M4mzfGN6fG:2b4jpZ4l1gSCjc4PhfS=> MoTON{Bl[Xm| NWjwemZrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR3NEmgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF{MzFOwG0> MoTUNlE4OTFyNUS=
rat C6 cells MmjlR5l1d3SxeHnjbZR6KGG|c3H5 NXvJR4pZOyCmYYnz MlHpR5l1d3SxeHnjbZR6KGGpYXnud5QhemG2IFO2JINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XluIFnDOVA:QS5yNzFOwG0> Moq3NlE4OTFyNUS=
human HT-29 cells MVnDfZRwfG:6aXPpeJkh[XO|YYm= M{X2UlMh\GG7cx?= NUTVUFNIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRvMkmgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjR2IN88US=> NVrVUY5DOjF5MUGwOVQ>
human HCT116 cells NYjJfIt1S3m2b4TvfIlkcXS7IHHzd4F6 M4jPXVMh\GG7cx?= NFT2OmJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjR|IN88US=> Ml7kNlE4OTFyNUS=
mouse CT26 cells MXHDfZRwfG:6aXPpeJkh[XO|YYm= M2TkUVMh\GG7cx?= NFGwb2lEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBEXDJ4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOzFizszN NYjDbHE1OjF5MUGwOVQ>
human PC3 cells M4X4O2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYmzJIRigXN? MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD16LkK4JO69VQ>? MnTUNlE4OTFyNUS=
MES-SA cells NUnzWWRFS3m2b4TvfIlkcXS7IHHzd4F6 M4TYSFMh\GG7cx?= M2fISGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GWy2VQTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTZ3IN88US=> NFrmclgzOTdzMUC1OC=>
human HPAC cells NXzTfpc5S3m2b4TvfIlkcXS7IHHzd4F6 Mn7vN{Bl[Xm| MnnjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHBCSyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUmuN|Ih|ryP MlvwNlE4OTFyNUS=
mouse P388D1 cells M{[x[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MYCzJIRigXN? Mn;MR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFM5QERzIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4zQDVizszN NV\LUngxOjF5MUGwOVQ>
CCRF-CEM cells NHP4fFNEgXSxdH;4bYNqfHliYYPzZZk> MVu3NkBp MmfsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjByMEWg{txO MWWyNVg1ODd{Mh?=
human Raji cells MlHRR5l1d3SxeHnjbZR6KGG|c3H5 MYi3NkBp MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSZYpqKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNFkh|ryP MWiyNVg1ODd{Mh?=
human HuH7 cells MX\DfZRwfG:6aXPpeJkh[XO|YYm= NHf6WoE4OiCq NHrqO4tEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NU45KM7:TR?= MYiyOVQ3OjJ5Nx?=
human T47D cells NVGwfZhTS3m2b4TvfIlkcXS7IHHzd4F6 NHLMcog4OiCq M{HSW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHQ1P0RiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlch|ryP M1XGd|I2PDZ{Mke3
human HCT116 cells NWXPNFVXS3m2b4TvfIlkcXS7IHHzd4F6 Ml7uO|IhcA>? M{XvWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOyEQvF2= Ml\ENlU1PjJ{N{e=
human K562 cells Ml\5VJJwdGmoZYLheIlwdiCjc4PhfS=> NIX2[mg1QCCq NGLldVVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFyIN88US=> MVWyOVk3ODN{Mx?=
human SKHEP1 cells NHnCUppRem:uaX\ldoF1cW:wIHHzd4F6 Mo\lOFghcA>? MmrHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1jFVFEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTRizszN MViyOVk3ODN{Mx?=
human MOLT3 cells NWnTZ4h{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MWe0PEBp NFy0VZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{LkOg{txO NIPv[Y4zPTl4MEOyNy=>
human KG1 cells NVrMRXNpWHKxbHnm[ZJifGmxbjDhd5NigQ>? NW\Ee|RYPDhiaB?= MmixRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNR{GgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOiEQvF2= M3XiZ|I2QTZyM{Kz
human RPMI8226 cells MnfuVJJwdGmoZYLheIlwdiCjc4PhfS=> NInrb5M1QCCq MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14IN88US=> M163XVI2QTZyM{Kz
human MCF7 cells MnvzVJJwdGmoZYLheIlwdiCjc4PhfS=> NIPuVFc1QCCq Ml;0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01PSEQvF2= NXy2UVJOOjV7NkCzNlM>
human SK-UT-1B cells NWTKbHV1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NWnVS3JxPDhiaB?= MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLWXUMVFDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zIN88US=> NWLwb41pOjV7NkCzNlM>
L1210 cell lines M4\QdmZ2dmO2aX;uJIF{e2G7 NGjDT3JKdiC4aYTyc{BqdmirYnn0c5J6KGWoZnXjeEB4[XNidHXzeIVlKG[xcjDjfZRwe3SjdHnjJIFkfGm4aYT5JI9vKHSqZTDndo94fGhib3[gcZVzcW6nIHzleYtmdWmlIFyxNlExKGOnbHygcIlv\XNuIFnEOVA:OC5yMzFOwG0> MoXtNlk6PTZ4Nh?=
P388 leukemic cell lines NITxfoNHfW6ldHnvckBie3OjeR?= NUTLUYI5UW5idnn0do8hcW6qaXLpeI9zgSCnZn\lZ5Qhf2G|IITld5Rm\CCob4KgZ5l1d3O2YYTpZ{Bi[3Srdnn0fUBwdiC2aHWg[5Jwf3SqIH;mJIx6dXCqb3nkJI5md3CuYYPtJHA{QDhibHX1b4VucWNiY3XscEBtcW6nczygTWQ2OD1yLkCzJO69VQ>? NFWxSWszQTl3Nk[2
human BV173 cells NH3sNGhEgXSxdH;4bYNqfHliYYPzZZk> M{GyOVMh\GG7cx?= M1vOTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJXOTd|IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4xODB6IN88US=> MV[yNVcyOTB3NB?=

... 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 NC1=NC(=NC2=C1N=C[N]2C3CC(O)C(CO)O3)Cl

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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 --
NCT03745144 Active not recruiting Drug: Cladribine|Drug: Placebo|Drug: Microgynon® Relapsing Multiple Sclerosis (RMS) Merck KGaA Darmstadt Germany January 17 2019 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID