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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USD 170 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 NU\odY8{S3m2b4TvfIlkcXS7IHHzd4F6 NEexcFVEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBES1KILVPFUUBk\WyuIHzpcoV{NCCLQ{WwQVAvODB|IN88US=> NX3rdXJEOTd|MkW1Oi=>
HEp-2 cell lines NID5dGZEgXSxdH;4bYNqfHliYYPzZZk> NIT6bWJEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBJTXBvMjDj[YxtKGyrbnXzMEBKSzVyPUCuNFMh|ryP MnflNVc{OjV3Nh?=
L1210 cell lines NGKyN3ZEgXSxdH;4bYNqfHliYYPzZZk> NEX0SVNEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBNOTJzMDDj[YxtKGyrbnXzMEBKSzVyPUCuNFch|pyv MXexO|MzPTV4
human K562 cells MVLDfZRwfG:6aXPpeJkh[XO|YYm= M{LDZVMh\GG7cx?= NVrKenFlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcvPjlizszN MVmyNVcyOTB3NB?=
CEM-DNR-bulk cells NHfWTW1EgXSxdH;4bYNqfHliYYPzZZk> NXPMTG0xOyCmYYnz MknRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2VONUSQUj3ieYxsKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zOVIh|ryP MlTNNlE4OTFyNUS=
mouse L1210 cells NYL5R2RWS3m2b4TvfIlkcXS7IHHzd4F6 MWmzJIRigXN? NH\BfllEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBNOTJzMDDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzl|IN88US=> MlSxNlE4OTFyNUS=
mouse EL4 cells Mo\aR5l1d3SxeHnjbZR6KGG|c3H5 NXLYSVYzOyCmYYnz MlnqR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgSWw1KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD64OFgh|ryP NI\JXGUzOTdzMUC1OC=>
human MCF7 cells NIrVV3pEgXSxdH;4bYNqfHliYYPzZZk> NGK1Tng{KGSjeYO= M{nlTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2yMlM2KM7:TR?= Mk\JNlE4OTFyNUS=
BT549 cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= MknzN{Bl[Xm| M37TPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJVPTR7IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOjNizszN MWCyNVcyOTB3NB?=
rat C6 cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= M3H2XlMh\GG7cx?= MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBz[XRiQ{[gZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjB5IN88US=> NVjlTFNPOjF5MUGwOVQ>
human HT-29 cells Mlj2R5l1d3SxeHnjbZR6KGG|c3H5 M1W5clMh\GG7cx?= NHLjSVFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDRizszN M3jNelIyPzFzMEW0
human HCT116 cells M2j6NGN6fG:2b4jpZ4l1gSCjc4PhfS=> MVKzJIRigXN? MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlQ{KM7:TR?= M1vXWlIyPzFzMEW0
mouse CT26 cells NUfq[5poS3m2b4TvfIlkcXS7IHHzd4F6 MWezJIRigXN? NHPVcZREgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBEXDJ4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOzFizszN MXeyNVcyOTB3NB?=
human PC3 cells M4nmSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NGG1PGo{KGSjeYO= NH;5dHNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME24MlI5KM7:TR?= MoDVNlE4OTFyNUS=
MES-SA cells MV;DfZRwfG:6aXPpeJkh[XO|YYm= MoW3N{Bl[Xm| M4\sV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1GWy2VQTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTZ3IN88US=> NWD1VY1kOjF5MUGwOVQ>
human HPAC cells NIDVcIhEgXSxdH;4bYNqfHliYYPzZZk> MYGzJIRigXN? NHvnc5VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJWEGFIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9PU4{OiEQvF2= MXWyNVcyOTB3NB?=
mouse P388D1 cells MXvDfZRwfG:6aXPpeJkh[XO|YYm= M2TGbFMh\GG7cx?= MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQN|g5TDFiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlI5PSEQvF2= M3PLZ|IyPzFzMEW0
CCRF-CEM cells NWK0SYpXS3m2b4TvfIlkcXS7IHHzd4F6 NGC1[FA4OiCq NFTXe3VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMECwOUDPxE1? Mkf5NlE5PDB5MkK=
human Raji cells M1;JTWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3uzT|czKGh? NGPYRm5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBT[WqrIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4xODlizszN NHv4R5IzOTh2MEeyNi=>
human HuH7 cells NGLIZ|JEgXSxdH;4bYNqfHliYYPzZZk> NWXj[GUxPzJiaB?= MmPnR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUGuPEDPxE1? MYiyOVQ3OjJ5Nx?=
human T47D cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= NVXMcodMPzJiaB?= NFfOUI9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE44KM7:TR?= NGrhTlEzPTR4MkK3Oy=>
human HCT116 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= MV[3NkBp M1vHVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOyEQvF2= MWOyOVQ3OjJ5Nx?=
human K562 cells NYjCc41MWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2qzUFQ5KGh? MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVExKM7:TR?= NXTweVViOjV7NkCzNlM>
human SKHEP1 cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 MVW0PEBp NFvVTHVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLTGVROSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NDFOwG0> M1rUS|I2QTZyM{Kz
human MOLT3 cells M3nQVnBzd2yrZnXyZZRqd25iYYPzZZk> NFXVeWI1QCCq M3P0UmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MWFMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJwMzFOwG0> Mn7kNlU6PjB|MkO=
human KG1 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 NWfzbFFjPDhiaB?= NXqydZNxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLS|Eh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMjFOwG0> NGfZOGczPTl4MEOyNy=>
human RPMI8226 cells NHPTenBRem:uaX\ldoF1cW:wIHHzd4F6 NIDBOo41QCCq M3jtOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[g{txO NYHqfoVkOjV7NkCzNlM>
human MCF7 cells MmeyVJJwdGmoZYLheIlwdiCjc4PhfS=> M{fzPVQ5KGh? MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2KM7:TR?= Mlm3NlU6PjB|MkO=
human SK-UT-1B cells MlLhVJJwdGmoZYLheIlwdiCjc4PhfS=> NGXP[GE1QCCq MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLWXUMVFDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zIN88US=> NWXHNoluOjV7NkCzNlM>
L1210 cell lines NIXYZY5HfW6ldHnvckBie3OjeR?= MWHJckB3cXS{bzDpcohq[mm2b4L5JIVn\mWldDD3ZZMhfGW|dHXkJIZweiCleYTvd5RifGmlIHHjeIl3cXS7IH;uJJRp\SCpcn;3eIghd2ZibYXybY5mKGyndXvlcYlkKExzMkGwJINmdGxibHnu[ZMtKEmGNUC9NE4xOyEQvF2= NIfLcokzQTl3Nk[2
P388 leukemic cell lines NYnHSJp2TnWwY4Tpc44h[XO|YYm= MUnJckB3cXS{bzDpcohq[mm2b4L5JIVn\mWldDD3ZZMhfGW|dHXkJIZweiCleYTvd5RifGmlIHHjeIl3cXS7IH;uJJRp\SCpcn;3eIghd2ZibIntdIhwcWRibnXvdIxie21iUEO4PEBt\XWtZX3pZ{Bk\WyuIHzpcoV{NCCLREWwQVAvODNizszN Mn3ENlk6PTZ4Nh?=
human BV173 cells NIHz[m9EgXSxdH;4bYNqfHliYYPzZZk> NY[wemRWOyCmYYnz NWHFclZES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlZzN{OgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjByMEig{txO MViyNVcyOTB3NB?=

... 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
NCT00980395 Active not recruiting Lymphoma|Mantle Cell Lymphoma|Indolent Lymphoma|SLL University of Arizona|National Cancer Institute (NCI) July 7 2009 Phase 2
NCT00923013 Recruiting Hairy Cell Leukemia National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 7 2008 Phase 2
NCT03586609 Not yet recruiting Acute Myeloid Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) October 31 2018 Phase 2
NCT00725985 Completed Multiple Sclerosis EMD Serono December 31 2008 Phase 3
NCT03012672 Recruiting Acute Leukemia of Ambiguous Lineage|Acute Myeloid Leukemia|Myeloid Neoplasm Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) December 30 2016 Phase 2
NCT01013350 Active not recruiting Multiple Sclerosis EMD Serono November 30 2009 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID