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 M1K4OGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHS5WGhEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBES1KILVPFUUBk\WyuIHzpcoV{NCCLQ{WwQVAvODB|IN88US=> NYTScXdJOTd|MkW1Oi=>
HEp-2 cell lines MXvDfZRwfG:6aXPpeJkh[XO|YYm= NGDCelVEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBJTXBvMjDj[YxtKGyrbnXzMEBKSzVyPUCuNFMh|ryP M3vIelE4OzJ3NU[=
L1210 cell lines MnrBR5l1d3SxeHnjbZR6KGG|c3H5 MonBR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgUFEzOTBiY3XscEBtcW6nczygTWM2OD1yLkC3JO6ddQ>? MnSzNVc{OjV3Nh?=
human K562 cells MoXBR5l1d3SxeHnjbZR6KGG|c3H5 M1nk[|Mh\GG7cx?= NHHndGREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9O{43QSEQvF2= NU\0UZhSOjF5MUGwOVQ>
CEM-DNR-bulk cells NY[3eIdbS3m2b4TvfIlkcXS7IHHzd4F6 NWjYV3ExOyCmYYnz NI\JOoxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBETU1vRF7SMYJ2dGtiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlM2OiEQvF2= MoKzNlE4OTFyNUS=
mouse L1210 cells M4PjVGN6fG:2b4jpZ4l1gSCjc4PhfS=> M4ftWFMh\GG7cx?= MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDMNVIyOCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN|k{KM7:TR?= M2L0RlIyPzFzMEW0
mouse EL4 cells MmnER5l1d3SxeHnjbZR6KGG|c3H5 NXPIVFQ2OyCmYYnz MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDFUFQh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1yLki0PEDPxE1? MV2yNVcyOTB3NB?=
human MCF7 cells M1TRdGN6fG:2b4jpZ4l1gSCjc4PhfS=> MVSzJIRigXN? MkjoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUKuN|Uh|ryP Mn25NlE4OTFyNUS=
BT549 cells MlXQR5l1d3SxeHnjbZR6KGG|c3H5 M2PtNVMh\GG7cx?= NHzIOYdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDV2OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTJ|IN88US=> NWrpVZp[OjF5MUGwOVQ>
rat C6 cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= MnLnN{Bl[Xm| M{DxeGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDDOkBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxRTlwMEeg{txO M1H4R|IyPzFzMEW0
human HT-29 cells MUXDfZRwfG:6aXPpeJkh[XO|YYm= NXrIXmJoOyCmYYnz NH3m[4tEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDRizszN MWmyNVcyOTB3NB?=
human HCT116 cells NFf4VZNEgXSxdH;4bYNqfHliYYPzZZk> MnXIN{Bl[Xm| M3rNe2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDNizszN MUSyNVcyOTB3NB?=
mouse CT26 cells M3X2PGN6fG:2b4jpZ4l1gSCjc4PhfS=> M2r1PVMh\GG7cx?= NEn1Zo5EgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBEXDJ4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOzFizszN MkXjNlE4OTFyNUS=
human PC3 cells NX6y[Y1YS3m2b4TvfIlkcXS7IHHzd4F6 M4n3Z|Mh\GG7cx?= MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD16LkK4JO69VQ>? M3\nWlIyPzFzMEW0
MES-SA cells M1zrRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MXqzJIRigXN? MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXMuW0FiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE3PSEQvF2= NH:4NVEzOTdzMUC1OC=>
human HPAC cells NIexNodEgXSxdH;4bYNqfHliYYPzZZk> NHPaZWw{KGSjeYO= M1fBXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhRSUNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlMzKM7:TR?= MljjNlE4OTFyNUS=
mouse P388D1 cells NVzpUmF6S3m2b4TvfIlkcXS7IHHzd4F6 M1LGSFMh\GG7cx?= NGTxO2dEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBROzh6REGgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJ6NTFOwG0> MXeyNVcyOTB3NB?=
CCRF-CEM cells NGPTOI5EgXSxdH;4bYNqfHliYYPzZZk> NYXtdVFkPzJiaB?= NV7jb2MyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0OURj3DSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkCwNFUh|ryP MUSyNVg1ODd{Mh?=
human Raji cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= Mn75O|IhcA>? MlTaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVoFrcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFA6KM7:TR?= MnriNlE5PDB5MkK=
human HuH7 cells NHq3VFNEgXSxdH;4bYNqfHliYYPzZZk> Mo\XO|IhcA>? MnjzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPyClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUGuPEDPxE1? NUX4[GlyOjV2NkKyO|c>
human T47D cells NET4c2ZEgXSxdH;4bYNqfHliYYPzZZk> MUO3NkBp NIq4VYNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE44KM7:TR?= MmPRNlU1PjJ{N{e=
human HCT116 cells MX7DfZRwfG:6aXPpeJkh[XO|YYm= M4TuNVczKGh? NEHSeFFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjNizszN NFLMbFkzPTR4MkK3Oy=>
human K562 cells NFj3c3BRem:uaX\ldoF1cW:wIHHzd4F6 M1PZUFQ5KGh? M4P4bWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTBizszN MWKyOVk3ODN{Mx?=
human SKHEP1 cells MlHPVJJwdGmoZYLheIlwdiCjc4PhfS=> MlvSOFghcA>? NVjyXoh5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSg{txO M3nxdlI2QTZyM{Kz
human MOLT3 cells M3\5VHBzd2yrZnXyZZRqd25iYYPzZZk> NYHRc3pQPDhiaB?= MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGSzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zNjNizszN MYqyOVk3ODN{Mx?=
human KG1 cells NGP3[pVRem:uaX\ldoF1cW:wIHHzd4F6 NWXwRVdSPDhiaB?= MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuJMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4zKM7:TR?= MWeyOVk3ODN{Mx?=
human RPMI8226 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 NXu2NJV1PDhiaB?= M3va[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[g{txO NXrzSmhOOjV7NkCzNlM>
human MCF7 cells NEC1[WhRem:uaX\ldoF1cW:wIHHzd4F6 NV36XJhKPDhiaB?= MmTCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01PSEQvF2= MVmyOVk3ODN{Mx?=
human SK-UT-1B cells M3;0ZnBzd2yrZnXyZZRqd25iYYPzZZk> M1\CcVQ5KGh? Mkn3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3VWE0ySiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MTFOwG0> MUmyOVk3ODN{Mx?=
L1210 cell lines NHPPd4ZHfW6ldHnvckBie3OjeR?= M1;wTGlvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDteZJqdmVibHX1b4VucWNiTEGyNVAh[2WubDDsbY5meyxiSVS1NF0xNjB|IN88US=> NGjpeo4zQTl3Nk[2
P388 leukemic cell lines NWDEbpBXTnWwY4Tpc44h[XO|YYm= M3r6XmlvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDsfY1xcG:rZDDu[Y9xdGG|bTDQN|g5KGyndXvlcYlkKGOnbHygcIlv\XNuIFnEOVA:OC5yMzFOwG0> MoDPNlk6PTZ4Nh?=
human BV173 cells Mkj1R5l1d3SxeHnjbZR6KGG|c3H5 Mm\5N{Bl[Xm| NWrETVRsS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlZzN{OgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjByMEig{txO MX: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]
+ 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
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