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 MXXDfZRwfG:6aXPpeJkh[XO|YYm= NFL5WoFEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBES1KILVPFUUBk\WyuIHzpcoV{NCCLQ{WwQVAvODB|IN88US=> NWHod3BIOTd|MkW1Oi=>
HEp-2 cell lines NHOyPYZEgXSxdH;4bYNqfHliYYPzZZk> NU[5T2lOS2:vcH;1coQhf2G|IITld5Rm\CCob4KgZ5l1d3SxeHnjbZR6KGGpYXnud5QhUEWyLUKgZ4VtdCCuaX7ld{whUUN3ME2wMlA{KM7:TR?= NWjLUnNLOTd|MkW1Oi=>
L1210 cell lines NXjPPFRHS3m2b4TvfIlkcXS7IHHzd4F6 NWSzPW5pS2:vcH;1coQhf2G|IITld5Rm\CCob4KgZ5l1d3SxeHnjbZR6KGGpYXnud5QhVDF{MUCgZ4VtdCCuaX7ld{whUUN3ME2wMlA4KM7ebR?= MXWxO|MzPTV4
human K562 cells NFTFRWpEgXSxdH;4bYNqfHliYYPzZZk> NWTvcpJiOyCmYYnz MkLpR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUeuOlkh|ryP MmmwNlE4OTFyNUS=
CEM-DNR-bulk cells MlToR5l1d3SxeHnjbZR6KGG|c3H5 NGS2RYQ{KGSjeYO= MnPER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2VONUSQUj3ieYxsKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zOVIh|ryP MXmyNVcyOTB3NB?=
mouse L1210 cells NXfxfIdLS3m2b4TvfIlkcXS7IHHzd4F6 MYKzJIRigXN? MoDzR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgUFEzOTBiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlM6OyEQvF2= NXLhZW42OjF5MUGwOVQ>
mouse EL4 cells MVLDfZRwfG:6aXPpeJkh[XO|YYm= MVOzJIRigXN? NEG0eIVEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBGVDRiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg1QCEQvF2= MUWyNVcyOTB3NB?=
human MCF7 cells M2PYcWN6fG:2b4jpZ4l1gSCjc4PhfS=> NG\5U5g{KGSjeYO= MoHjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUKuN|Uh|ryP NUXLSVhTOjF5MUGwOVQ>
BT549 cells MnzNR5l1d3SxeHnjbZR6KGG|c3H5 MVqzJIRigXN? NILoVmNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDV2OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTJ|IN88US=> M4fqZVIyPzFzMEW0
rat C6 cells NYPnV4ExS3m2b4TvfIlkcXS7IHHzd4F6 MmLLN{Bl[Xm| M{nTRWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDDOkBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxRTlwMEeg{txO M4XzSVIyPzFzMEW0
human HT-29 cells NX3HUZlYS3m2b4TvfIlkcXS7IHHzd4F6 NFfrW3U{KGSjeYO= MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUmuOFQh|ryP M4Xpb|IyPzFzMEW0
human HCT116 cells NF73[YVEgXSxdH;4bYNqfHliYYPzZZk> NV;yb5IyOyCmYYnz MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlQ{KM7:TR?= MlWzNlE4OTFyNUS=
mouse CT26 cells Ml\KR5l1d3SxeHnjbZR6KGG|c3H5 MnXtN{Bl[Xm| NFm0e2dEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBEXDJ4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOzFizszN M1nIVFIyPzFzMEW0
human PC3 cells M{DPXmN6fG:2b4jpZ4l1gSCjc4PhfS=> MmCwN{Bl[Xm| MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD16LkK4JO69VQ>? MmXoNlE4OTFyNUS=
MES-SA cells NHXBUI5EgXSxdH;4bYNqfHliYYPzZZk> MVezJIRigXN? MnrHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWVUNVODIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yPjVizszN NH3mV3UzOTdzMUC1OC=>
human HPAC cells M13OemN6fG:2b4jpZ4l1gSCjc4PhfS=> NVu4RVRMOyCmYYnz M13ld2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhRSUNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlMzKM7:TR?= NGTZSm0zOTdzMUC1OC=>
mouse P388D1 cells NVjse4l5S3m2b4TvfIlkcXS7IHHzd4F6 M4LnW|Mh\GG7cx?= NUX6dZUxS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhWDN6OFSxJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{OEWg{txO MUSyNVcyOTB3NB?=
CCRF-CEM cells M1O4eGN6fG:2b4jpZ4l1gSCjc4PhfS=> NWq2O4xuPzJiaB?= NIm5OY9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMECwOUDPxE1? MknwNlE5PDB5MkK=
human Raji cells NFHScmxEgXSxdH;4bYNqfHliYYPzZZk> M{jJSlczKGh? M3e0e2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJicmliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxQSEQvF2= NH[xVlAzOTh2MEeyNi=>
human HuH7 cells NXL5NoJiS3m2b4TvfIlkcXS7IHHzd4F6 M4\rfVczKGh? NITkbpJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NU45KM7:TR?= NX;oT3liOjV2NkKyO|c>
human T47D cells NYXnWVRLS3m2b4TvfIlkcXS7IHHzd4F6 NWWwWFVPPzJiaB?= MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD63JO69VQ>? NFnNeIUzPTR4MkK3Oy=>
human HCT116 cells MoDyR5l1d3SxeHnjbZR6KGG|c3H5 NYnhcZlUPzJiaB?= NU\CNm5zS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5|IN88US=> MYKyOVQ3OjJ5Nx?=
human K562 cells MWTQdo9tcW[ncnH0bY9vKGG|c3H5 MlW4OFghcA>? MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVExKM7:TR?= M3LNb|I2QTZyM{Kz
human SKHEP1 cells NGnmR3FRem:uaX\ldoF1cW:wIHHzd4F6 M4CwV|Q5KGh? NUfoOlBOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSg{txO MnK4NlU6PjB|MkO=
human MOLT3 cells NFTIcFhRem:uaX\ldoF1cW:wIHHzd4F6 MX60PEBp MnH5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi5|IN88US=> MWKyOVk3ODN{Mx?=
human KG1 cells NYKxO5BjWHKxbHnm[ZJifGmxbjDhd5NigQ>? NID1dmg1QCCq NVzTbmpbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLS|Eh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMjFOwG0> M{[z[VI2QTZyM{Kz
human RPMI8226 cells M3nZcXBzd2yrZnXyZZRqd25iYYPzZZk> MmTjOFghcA>? MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14IN88US=> M1nn[lI2QTZyM{Kz
human MCF7 cells M4nqd3Bzd2yrZnXyZZRqd25iYYPzZZk> NIXtV5I1QCCq NE\kbHpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTR3IN88US=> MVuyOVk3ODN{Mx?=
human SK-UT-1B cells M{fXZnBzd2yrZnXyZZRqd25iYYPzZZk> MoHSOFghcA>? Mn33RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3VWE0ySiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MTFOwG0> MlH6NlU6PjB|MkO=
L1210 cell lines NFu3NZdHfW6ldHnvckBie3OjeR?= MUTJckB3cXS{bzDpcohq[mm2b4L5JIVn\mWldDD3ZZMhfGW|dHXkJIZweiCleYTvd5RifGmlIHHjeIl3cXS7IH;uJJRp\SCpcn;3eIghd2ZibYXybY5mKGyndXvlcYlkKExzMkGwJINmdGxibHnu[ZMtKEmGNUC9NE4xOyEQvF2= NX22eYRDOjl7NU[2Oi=>
P388 leukemic cell lines M1\Nc2Z2dmO2aX;uJIF{e2G7 NYnsOXFlUW5idnn0do8hcW6qaXLpeI9zgSCnZn\lZ5Qhf2G|IITld5Rm\CCob4KgZ5l1d3O2YYTpZ{Bi[3Srdnn0fUBwdiC2aHWg[5Jwf3SqIH;mJIx6dXCqb3nkJI5md3CuYYPtJHA{QDhibHX1b4VucWNiY3XscEBtcW6nczygTWQ2OD1yLkCzJO69VQ>? MXuyPVk2PjZ4
human BV173 cells MW\DfZRwfG:6aXPpeJkh[XO|YYm= MmrRN{Bl[Xm| MnTUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnYyPzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxODhizszN NYKyVnMzOjF5MUGwOVQ>

... 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:
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
Synonyms 2-CdA, 2-chlorodeoxyadenosine

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00923013 Recruiting Hairy Cell Leukemia National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 3, 2008 Phase 2
NCT02250937 Recruiting Acute Myeloid Leukemia|Myelodysplastic Syndrome M.D. Anderson Cancer Center October 27, 2014 Phase 2
NCT02728050 Recruiting Acute Biphenotypic Leukemia|Acute Myeloid Leukemia|de Novo Myelodysplastic Syndrome|Myeloproliferative Neoplasm University of Washington|National Cancer Institute (NCI) December 2016 Phase 1|Phase 2
NCT03012672 Recruiting Acute Myeloid Leukemia|Myeloid Neoplasm Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) December 2016 --
NCT02921061 Recruiting de Novo Myelodysplastic Syndrome|Mixed Phenotype Acute Leukemia|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) November 2016 Phase 1
NCT02756572 Recruiting Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Recurrent Childhood Acute Myeloid Leukemia University of Washington|National Cancer Institute (NCI) September 2016 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID