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 MmnWR5l1d3SxeHnjbZR6KGG|c3H5 MVXDc41xd3WwZDD3ZZMhfGW|dHXkJIZweiCleYTveI95cWOrdImgZYdicW6|dDDDR3JHNUOHTTDj[YxtKGyrbnXzMEBKSzVyPUCuNFA{KM7:TR?= NYTVTXR7OTd|MkW1Oi=>
HEp-2 cell lines NUjafYNxS3m2b4TvfIlkcXS7IHHzd4F6 MWnDc41xd3WwZDD3ZZMhfGW|dHXkJIZweiCleYTveI95cWOrdImgZYdicW6|dDDISZAuOiClZXzsJIxqdmW|LDDJR|UxRTBwMEOg{txO MUKxO|MzPTV4
L1210 cell lines M1HubWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUPvcI9zS2:vcH;1coQhf2G|IITld5Rm\CCob4KgZ5l1d3SxeHnjbZR6KGGpYXnud5QhVDF{MUCgZ4VtdCCuaX7ld{whUUN3ME2wMlA4KM7ebR?= Mn3GNVc{OjV3Nh?=
human K562 cells NInzU4REgXSxdH;4bYNqfHliYYPzZZk> NHjIO5Q{KGSjeYO= NH3t[2tEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9O{43QSEQvF2= NFHOXXozOTdzMUC1OC=>
CEM-DNR-bulk cells Ml33R5l1d3SxeHnjbZR6KGG|c3H5 NUPSTVQzOyCmYYnz MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDSW0uTE6ULXL1cIsh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1yLkO1NkDPxE1? NUP1[5ZYOjF5MUGwOVQ>
mouse L1210 cells MlTxR5l1d3SxeHnjbZR6KGG|c3H5 M4LV[FMh\GG7cx?= NE\VW|dEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBNOTJzMDDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzl|IN88US=> NEXqZnczOTdzMUC1OC=>
mouse EL4 cells M3vYO2N6fG:2b4jpZ4l1gSCjc4PhfS=> MnXCN{Bl[Xm| NGHSPGhEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBGVDRiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg1QCEQvF2= M1P6bFIyPzFzMEW0
human MCF7 cells MorDR5l1d3SxeHnjbZR6KGG|c3H5 NVjQSlFQOyCmYYnz MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6zOUDPxE1? MkHNNlE4OTFyNUS=
BT549 cells M1GyS2N6fG:2b4jpZ4l1gSCjc4PhfS=> MnHzN{Bl[Xm| NG\IdWZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDV2OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTJ|IN88US=> Mn;vNlE4OTFyNUS=
rat C6 cells M3fCTGN6fG:2b4jpZ4l1gSCjc4PhfS=> NG\PeVg{KGSjeYO= NGi1cm1EgXSxdH;4bYNqfHliYXfhbY5{fCC{YYSgR|Yh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD17LkC3JO69VQ>? MXqyNVcyOTB3NB?=
human HT-29 cells MmXhR5l1d3SxeHnjbZR6KGG|c3H5 NV[2XGs4OyCmYYnz NGriepREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDRizszN NWjleoVnOjF5MUGwOVQ>
human HCT116 cells M2TVcWN6fG:2b4jpZ4l1gSCjc4PhfS=> MlT3N{Bl[Xm| MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlQ{KM7:TR?= NHn3UG0zOTdzMUC1OC=>
mouse CT26 cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= NHTGbJg{KGSjeYO= M3PIdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGNVOjZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE{OSEQvF2= NH3QNJAzOTdzMUC1OC=>
human PC3 cells NXn1T4dlS3m2b4TvfIlkcXS7IHHzd4F6 M4LtPFMh\GG7cx?= NWPKdpl2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9PE4zQCEQvF2= MWSyNVcyOTB3NB?=
MES-SA cells NIH2VXVEgXSxdH;4bYNqfHliYYPzZZk> M3nIXlMh\GG7cx?= NIHhenpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTVNvU1GgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF4NTFOwG0> MkC3NlE4OTFyNUS=
human HPAC cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= MlTEN{Bl[Xm| MoDrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHBCSyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUmuN|Ih|ryP MXGyNVcyOTB3NB?=
mouse P388D1 cells MnTaR5l1d3SxeHnjbZR6KGG|c3H5 M2fVVlMh\GG7cx?= NFv0d4FEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBROzh6REGgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJ6NTFOwG0> MVyyNVcyOTB3NB?=
CCRF-CEM cells NVnSWI9YS3m2b4TvfIlkcXS7IHHzd4F6 NEnySmc4OiCq MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDR3JHNUOHTTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODByNTFOwG0> NY\l[I5QOjF6NEC3NlI>
human Raji cells MmjYR5l1d3SxeHnjbZR6KGG|c3H5 NYXkfJdRPzJiaB?= NXvETYQ{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWmGsaTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODB7IN88US=> MWeyNVg1ODd{Mh?=
human HuH7 cells MkfTR5l1d3SxeHnjbZR6KGG|c3H5 NHTY[pc4OiCq Mm\ER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUGuPEDPxE1? NHfPb|MzPTR4MkK3Oy=>
human T47D cells M4DEcmN6fG:2b4jpZ4l1gSCjc4PhfS=> NIHNXJI4OiCq M2Do[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHQ1P0RiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlch|ryP MlSyNlU1PjJ{N{e=
human HCT116 cells NGD1Z3ZEgXSxdH;4bYNqfHliYYPzZZk> Ml;CO|IhcA>? NYX2b5pwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5|IN88US=> MV:yOVQ3OjJ5Nx?=
human K562 cells MlrnVJJwdGmoZYLheIlwdiCjc4PhfS=> M1\ySVQ5KGh? M1TIW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTBizszN M3nHWlI2QTZyM{Kz
human SKHEP1 cells MnfPVJJwdGmoZYLheIlwdiCjc4PhfS=> NGXFTnI1QCCq NUHhV3EySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSg{txO MnfENlU6PjB|MkO=
human MOLT3 cells Mm\5VJJwdGmoZYLheIlwdiCjc4PhfS=> MmL5OFghcA>? M{Cz[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MWFMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJwMzFOwG0> M4HpV|I2QTZyM{Kz
human KG1 cells M4PTeXBzd2yrZnXyZZRqd25iYYPzZZk> M3rmUFQ5KGh? M2nzZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJizszN NHfqc|czPTl4MEOyNy=>
human RPMI8226 cells MV7Qdo9tcW[ncnH0bY9vKGG|c3H5 Mnf2OFghcA>? M1zNU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[g{txO NF:zOFgzPTl4MEOyNy=>
human MCF7 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NELzUJk1QCCq Mlj2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01PSEQvF2= NITEO48zPTl4MEOyNy=>
human SK-UT-1B cells NGm1R4FRem:uaX\ldoF1cW:wIHHzd4F6 M2\UWFQ5KGh? NIj0fVdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMXVVNTGEIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? Mne1NlU6PjB|MkO=
L1210 cell lines NITz[FJHfW6ldHnvckBie3OjeR?= NVizRYozUW5idnn0do8hcW6qaXLpeI9zgSCnZn\lZ5Qhf2G|IITld5Rm\CCob4KgZ5l1d3O2YYTpZ{Bi[3Srdnn0fUBwdiC2aHWg[5Jwf3SqIH;mJI12emmwZTDs[ZVs\W2rYzDMNVIyOCClZXzsJIxqdmW|LDDJSFUxRTBwMEOg{txO MWGyPVk2PjZ4
P388 leukemic cell lines NInjTGNHfW6ldHnvckBie3OjeR?= Ml7ITY4hfmm2cn:gbY5pcWKrdH;yfUBm\m[nY4Sge4F{KHSnc4Tl[EBnd3JiY4n0c5N1[XSrYzDhZ5Rqfmm2eTDvckB1cGViZ4Lve5RpKG:oIHz5cZBpd2mmIH7lc5Bt[XOvIGCzPFghdGW3a3XtbYMh[2WubDDsbY5meyxiSVS1NF0xNjB|IN88US=> NHi5d2czQTl3Nk[2
human BV173 cells M4fTeWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWC4PYlSOyCmYYnz NFvmc3JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXjF5MzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODByODFOwG0> MUmyNVcyOTB3NB?=

... 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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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