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 NVf1VWczS3m2b4TvfIlkcXS7IHHzd4F6 Mn30R49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgR2NTTi2FRV2gZ4VtdCCuaX7ld{whUUN3ME2wMlAxOyEQvF2= MVSxO|MzPTV4
HEp-2 cell lines NFPzWGREgXSxdH;4bYNqfHliYYPzZZk> MVfDc41xd3WwZDD3ZZMhfGW|dHXkJIZweiCleYTveI95cWOrdImgZYdicW6|dDDISZAuOiClZXzsJIxqdmW|LDDJR|UxRTBwMEOg{txO MVGxO|MzPTV4
L1210 cell lines M{nVOGN6fG:2b4jpZ4l1gSCjc4PhfS=> NEGzU|NEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBNOTJzMDDj[YxtKGyrbnXzMEBKSzVyPUCuNFch|pyv MoXYNVc{OjV3Nh?=
human K562 cells NHXBcItEgXSxdH;4bYNqfHliYYPzZZk> M{nOXFMh\GG7cx?= M{LuNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME23MlY6KM7:TR?= MWqyNVcyOTB3NB?=
CEM-DNR-bulk cells M3PEO2N6fG:2b4jpZ4l1gSCjc4PhfS=> NHPzOoQ{KGSjeYO= Mm\SR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2VONUSQUj3ieYxsKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zOVIh|ryP MViyNVcyOTB3NB?=
mouse L1210 cells MkDmR5l1d3SxeHnjbZR6KGG|c3H5 NIWz[I4{KGSjeYO= NYK2cJVZS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhVDF{MUCgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjN7MzFOwG0> NVr5OWJpOjF5MUGwOVQ>
mouse EL4 cells NVnWZoVES3m2b4TvfIlkcXS7IHHzd4F6 NXezNodROyCmYYnz MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDFUFQh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1yLki0PEDPxE1? MnLqNlE4OTFyNUS=
human MCF7 cells Mn\sR5l1d3SxeHnjbZR6KGG|c3H5 NGHVNo0{KGSjeYO= MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6zOUDPxE1? MWeyNVcyOTB3NB?=
BT549 cells NVLPVHFpS3m2b4TvfIlkcXS7IHHzd4F6 NXHYXoRGOyCmYYnz NGHSRZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDV2OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTJ|IN88US=> NYr6U4NoOjF5MUGwOVQ>
rat C6 cells MlfxR5l1d3SxeHnjbZR6KGG|c3H5 M2THZ|Mh\GG7cx?= M{mzdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDDOkBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxRTlwMEeg{txO Mnj4NlE4OTFyNUS=
human HT-29 cells MnnVR5l1d3SxeHnjbZR6KGG|c3H5 NYjSeGprOyCmYYnz NFHpZm1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvPDRizszN MYeyNVcyOTB3NB?=
human HCT116 cells Ml3zR5l1d3SxeHnjbZR6KGG|c3H5 M1nHb|Mh\GG7cx?= MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlQ{KM7:TR?= MV:yNVcyOTB3NB?=
mouse CT26 cells NX3JfWh3S3m2b4TvfIlkcXS7IHHzd4F6 MVSzJIRigXN? MlPjR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgR3QzPiClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNVMyKM7:TR?= M1;LSlIyPzFzMEW0
human PC3 cells M4Tad2N6fG:2b4jpZ4l1gSCjc4PhfS=> MoHUN{Bl[Xm| MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD16LkK4JO69VQ>? MkjyNlE4OTFyNUS=
MES-SA cells M13qcWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUjnbWRCOyCmYYnz MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXMuW0FiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE3PSEQvF2= Mo[xNlE4OTFyNUS=
human HPAC cells M37BcmN6fG:2b4jpZ4l1gSCjc4PhfS=> M17sXFMh\GG7cx?= NIK4VYdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJWEGFIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9PU4{OiEQvF2= NGX4OpAzOTdzMUC1OC=>
mouse P388D1 cells NXPxdohqS3m2b4TvfIlkcXS7IHHzd4F6 MkjxN{Bl[Xm| NWDWWFY{S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhWDN6OFSxJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{OEWg{txO NFfsbW4zOTdzMUC1OC=>
CCRF-CEM cells NV7Ke49JS3m2b4TvfIlkcXS7IHHzd4F6 M{i0W|czKGh? MoHyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2NTTi2FRV2gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjByMEWg{txO M1vyWFIyQDRyN{Ky
human Raji cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= NYrPXodZPzJiaB?= MoDlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVoFrcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFA6KM7:TR?= M325VVIyQDRyN{Ky
human HuH7 cells M{HlW2N6fG:2b4jpZ4l1gSCjc4PhfS=> MoCxO|IhcA>? MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MT64JO69VQ>? NHL4bnYzPTR4MkK3Oy=>
human T47D cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MYG3NkBp MonRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWFQ4TCClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuO{DPxE1? MUCyOVQ3OjJ5Nx?=
human HCT116 cells NXy4OVJLS3m2b4TvfIlkcXS7IHHzd4F6 NYm2bHZQPzJiaB?= M3LndWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOyEQvF2= M4jrRlI2PDZ{Mke3
human K562 cells NFzOOWZRem:uaX\ldoF1cW:wIHHzd4F6 MnfHOFghcA>? MoDPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yOCEQvF2= NHT4XnYzPTl4MEOyNy=>
human SKHEP1 cells M2fyTXBzd2yrZnXyZZRqd25iYYPzZZk> MWO0PEBp NIm2N2FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLTGVROSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NDFOwG0> M4DYPVI2QTZyM{Kz
human MOLT3 cells M2LPe3Bzd2yrZnXyZZRqd25iYYPzZZk> NFPUVYU1QCCq NE\vXYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{LkOg{txO MVeyOVk3ODN{Mx?=
human KG1 cells M2TZfXBzd2yrZnXyZZRqd25iYYPzZZk> MmLpOFghcA>? MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuJMTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4zKM7:TR?= NH;TdJQzPTl4MEOyNy=>
human RPMI8226 cells NEfhO5hRem:uaX\ldoF1cW:wIHHzd4F6 NFm1OG41QCCq NVXWWIRrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OkDPxE1? MVqyOVk3ODN{Mx?=
human MCF7 cells NHTpWpFRem:uaX\ldoF1cW:wIHHzd4F6 Mk\OOFghcA>? MlLaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01PSEQvF2= MlfHNlU6PjB|MkO=
human SK-UT-1B cells Mn\ZVJJwdGmoZYLheIlwdiCjc4PhfS=> MlXPOFghcA>? NUO1TopNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1WXC1zQjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? Ml;YNlU6PjB|MkO=
L1210 cell lines M1\pPWZ2dmO2aX;uJIF{e2G7 NUjVdohHUW5idnn0do8hcW6qaXLpeI9zgSCnZn\lZ5Qhf2G|IITld5Rm\CCob4KgZ5l1d3O2YYTpZ{Bi[3Srdnn0fUBwdiC2aHWg[5Jwf3SqIH;mJI12emmwZTDs[ZVs\W2rYzDMNVIyOCClZXzsJIxqdmW|LDDJSFUxRTBwMEOg{txO NXPhXGZROjl7NU[2Oi=>
P388 leukemic cell lines NXrLdZNsTnWwY4Tpc44h[XO|YYm= M2P5SWlvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDsfY1xcG:rZDDu[Y9xdGG|bTDQN|g5KGyndXvlcYlkKGOnbHygcIlv\XNuIFnEOVA:OC5yMzFOwG0> NUDDZpF6Ojl7NU[2Oi=>
human BV173 cells NVL5RmRjS3m2b4TvfIlkcXS7IHHzd4F6 M2XvfFMh\GG7cx?= NWnXOHR{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlZzN{OgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjByMEig{txO NH;XTXMzOTdzMUC1OC=>

... 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 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