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 NWjJRnlZS3m2b4TvfIlkcXS7IHHzd4F6 NEDTdmVEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBES1KILVPFUUBk\WyuIHzpcoV{NCCLQ{WwQVAvODB|IN88US=> NX;uc21HOTd|MkW1Oi=>
HEp-2 cell lines MV;DfZRwfG:6aXPpeJkh[XO|YYm= MlHuR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgTGVxNTJiY3XscEBtcW6nczygTWM2OD1yLkCzJO69VQ>? M3TNNFE4OzJ3NU[=
L1210 cell lines MU\DfZRwfG:6aXPpeJkh[XO|YYm= NUG4fWhjS2:vcH;1coQhf2G|IITld5Rm\CCob4KgZ5l1d3SxeHnjbZR6KGGpYXnud5QhVDF{MUCgZ4VtdCCuaX7ld{whUUN3ME2wMlA4KM7ebR?= NYPXNppNOTd|MkW1Oi=>
human K562 cells NVjSZmU1S3m2b4TvfIlkcXS7IHHzd4F6 NYrMWJJnOyCmYYnz M4jjRWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME23MlY6KM7:TR?= MXWyNVcyOTB3NB?=
CEM-DNR-bulk cells MX;DfZRwfG:6aXPpeJkh[XO|YYm= MknTN{Bl[Xm| MmDsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2VONUSQUj3ieYxsKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zOVIh|ryP NHXkWXEzOTdzMUC1OC=>
mouse L1210 cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= NFvDeHM{KGSjeYO= MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDMNVIyOCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN|k{KM7:TR?= MljqNlE4OTFyNUS=
mouse EL4 cells NYfGUZVtS3m2b4TvfIlkcXS7IHHzd4F6 NFfkVZI{KGSjeYO= M1TidWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGVNPCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuPFQ5KM7:TR?= MnLBNlE4OTFyNUS=
human MCF7 cells MUPDfZRwfG:6aXPpeJkh[XO|YYm= M171PVMh\GG7cx?= NYLafGV3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVIvOzVizszN NXP3eXg5OjF5MUGwOVQ>
BT549 cells NXT4SHRkS3m2b4TvfIlkcXS7IHHzd4F6 NYHr[mpROyCmYYnz MlPOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnQ2PDliY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlEzOyEQvF2= NF\WdGgzOTdzMUC1OC=>
rat C6 cells MUDDfZRwfG:6aXPpeJkh[XO|YYm= MlHJN{Bl[Xm| M{nqW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDDOkBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxRTlwMEeg{txO MXOyNVcyOTB3NB?=
human HT-29 cells NGXxPGdEgXSxdH;4bYNqfHliYYPzZZk> MXGzJIRigXN? NG[3NpFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDRizszN M{Xqe|IyPzFzMEW0
human HCT116 cells MlTNR5l1d3SxeHnjbZR6KGG|c3H5 NWf0ZnRWOyCmYYnz M33HZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDNizszN MV:yNVcyOTB3NB?=
mouse CT26 cells NFvFVGtEgXSxdH;4bYNqfHliYYPzZZk> MnvVN{Bl[Xm| MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDDWFI3KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6xN|Eh|ryP M4PFRVIyPzFzMEW0
human PC3 cells M2rwcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVizJIRigXN? NGXtOJlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME24MlI5KM7:TR?= MU[yNVcyOTB3NB?=
MES-SA cells M2DhbWN6fG:2b4jpZ4l1gSCjc4PhfS=> MojlN{Bl[Xm| M2TnNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GWy2VQTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTZ3IN88US=> NX7pdVFrOjF5MUGwOVQ>
human HPAC cells Mlz1R5l1d3SxeHnjbZR6KGG|c3H5 NH[zOo8{KGSjeYO= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIVGFEKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;OT6zNkDPxE1? M{\HcVIyPzFzMEW0
mouse P388D1 cells NIjqXI1EgXSxdH;4bYNqfHliYYPzZZk> MXyzJIRigXN? MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQN|g5TDFiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlI5PSEQvF2= NEPWWXMzOTdzMUC1OC=>
CCRF-CEM cells NGT2elhEgXSxdH;4bYNqfHliYYPzZZk> NEDoe4o4OiCq NV7X[3FOS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0OURj3DSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCwNFUh|ryP NYnNWZp1OjF6NEC3NlI>
human Raji cells NVr0cWhHS3m2b4TvfIlkcXS7IHHzd4F6 MonCO|IhcA>? MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSZYpqKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wNFkh|ryP MVmyNVg1ODd{Mh?=
human HuH7 cells M33UR2N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml;NO|IhcA>? NGLWTnJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NU45KM7:TR?= Mm\5NlU1PjJ{N{e=
human T47D cells NXTvSotES3m2b4TvfIlkcXS7IHHzd4F6 M1vZWFczKGh? NWr2UYo6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXDR5RDDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvPyEQvF2= MkPONlU1PjJ{N{e=
human HCT116 cells NH3sbGJEgXSxdH;4bYNqfHliYYPzZZk> NWKxXIdNPzJiaB?= MlnvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4{KM7:TR?= NG\lRXczPTR4MkK3Oy=>
human K562 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 MmrYOFghcA>? M4Gwe2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTBizszN NEPmRpczPTl4MEOyNy=>
human SKHEP1 cells NH\SbW9Rem:uaX\ldoF1cW:wIHHzd4F6 NI\nSHQ1QCCq M{KyU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vISXAyKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD12IN88US=> M{mwOlI2QTZyM{Kz
human MOLT3 cells NVHa[nNbWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3LMNlQ5KGh? NFvI[pBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{LkOg{txO NWjSc|J1OjV7NkCzNlM>
human KG1 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MlixOFghcA>? M4TobmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJizszN NWXUXFh1OjV7NkCzNlM>
human RPMI8226 cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 NETwVmM1QCCq Ml;2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NjFOwG0> Mnf3NlU6PjB|MkO=
human MCF7 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 MVi0PEBp MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2KM7:TR?= MUSyOVk3ODN{Mx?=
human SK-UT-1B cells M4DqfnBzd2yrZnXyZZRqd25iYYPzZZk> MkLlOFghcA>? NV;4d5g4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1WXC1zQjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? MnfjNlU6PjB|MkO=
L1210 cell lines MmHBSpVv[3Srb36gZZN{[Xl? MV3JckB3cXS{bzDpcohq[mm2b4L5JIVn\mWldDD3ZZMhfGW|dHXkJIZweiCleYTvd5RifGmlIHHjeIl3cXS7IH;uJJRp\SCpcn;3eIghd2ZibYXybY5mKGyndXvlcYlkKExzMkGwJINmdGxibHnu[ZMtKEmGNUC9NE4xOyEQvF2= Mlv3Nlk6PTZ4Nh?=
P388 leukemic cell lines M2ruN2Z2dmO2aX;uJIF{e2G7 MmrjTY4hfmm2cn:gbY5pcWKrdH;yfUBm\m[nY4Sge4F{KHSnc4Tl[EBnd3JiY4n0c5N1[XSrYzDhZ5Rqfmm2eTDvckB1cGViZ4Lve5RpKG:oIHz5cZBpd2mmIH7lc5Bt[XOvIGCzPFghdGW3a3XtbYMh[2WubDDsbY5meyxiSVS1NF0xNjB|IN88US=> MmfrNlk6PTZ4Nh?=
human BV173 cells NULNZXZUS3m2b4TvfIlkcXS7IHHzd4F6 M1:1d|Mh\GG7cx?= NEPYblVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXjF5MzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODByODFOwG0> NGPn[ngzOTdzMUC1OC=>

... 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03602131 Not yet recruiting Hodgkin Lymphoma|Non-hodgkin Lymphoma Sichuan University January 1 2019 Phase 2
NCT03745144 Recruiting Relapsing Multiple Sclerosis (RMS) Merck KGaA Darmstadt Germany January 17 2019 Phase 1
NCT03602131 Not yet recruiting Hodgkin Lymphoma|Non-hodgkin Lymphoma Sichuan University January 1 2019 Phase 2
NCT03745144 Recruiting Relapsing Multiple Sclerosis (RMS) Merck KGaA Darmstadt Germany January 17 2019 Phase 1
NCT03491579 Withdrawn AML|Relapse University Hospital Inselspital Berne December 2018 Phase 1
NCT03491579 Withdrawn AML|Relapse University Hospital Inselspital Berne December 2018 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID