Cladribine

For research use only. Not for use in humans.

Catalog No.S1199 Synonyms: 2-CdA, 2-chlorodeoxyadenosine

2 publications

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 120 In stock
USD 97 In stock
USD 170 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

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 NVzEVXRRS3m2b4TvfIlkcXS7IHHzd4F6 M4rMVGNwdXCxdX7kJJdieyC2ZYP0[YQh\m:{IHP5eI91d3irY3n0fUBi\2GrboP0JGNEWkZvQ1XNJINmdGxibHnu[ZMtKEmFNUC9NE4xODNizszN MVGxO|MzPTV4
HEp-2 cell lines MUDDfZRwfG:6aXPpeJkh[XO|YYm= M{LZOWNwdXCxdX7kJJdieyC2ZYP0[YQh\m:{IHP5eI91d3irY3n0fUBi\2GrboP0JGhGeC1{IHPlcIwhdGmwZYOsJGlEPTB;MD6wN{DPxE1? M3W0XlE4OzJ3NU[=
L1210 cell lines NIDuSHBEgXSxdH;4bYNqfHliYYPzZZk> MoTQR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgUFEzOTBiY3XscEBtcW6nczygTWM2OD1yLkC3JO6ddQ>? M3e0d|E4OzJ3NU[=
human K562 cells MVHDfZRwfG:6aXPpeJkh[XO|YYm= MUezJIRigXN? NWHFbYRsS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcvPjlizszN MoXCNlE4OTFyNUS=
CEM-DNR-bulk cells NGnKcGVEgXSxdH;4bYNqfHliYYPzZZk> M2XxVlMh\GG7cx?= NFPY[WpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBETU1vRF7SMYJ2dGtiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlM2OiEQvF2= NV;yNWQ{OjF5MUGwOVQ>
mouse L1210 cells MYPDfZRwfG:6aXPpeJkh[XO|YYm= Mn7sN{Bl[Xm| M1KxRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGwyOjFyIHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4{QTNizszN MWiyNVcyOTB3NB?=
mouse EL4 cells NYPPfXduS3m2b4TvfIlkcXS7IHHzd4F6 NX:xc4hqOyCmYYnz NXXwU|V7S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhTUx2IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE45PDhizszN MlvRNlE4OTFyNUS=
human MCF7 cells M3[zSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWjhdXJ7OyCmYYnz MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6zOUDPxE1? M3LyZ|IyPzFzMEW0
BT549 cells MmjhR5l1d3SxeHnjbZR6KGG|c3H5 MlXmN{Bl[Xm| NUi5V4dKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR3NEmgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF{MzFOwG0> MkfFNlE4OTFyNUS=
rat C6 cells MoPmR5l1d3SxeHnjbZR6KGG|c3H5 M1nQVFMh\GG7cx?= MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBz[XRiQ{[gZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF06NjB5IN88US=> MnTXNlE4OTFyNUS=
human HT-29 cells NWHaeIRjS3m2b4TvfIlkcXS7IHHzd4F6 M1jVWlMh\GG7cx?= MnT1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlQ1KM7:TR?= MXyyNVcyOTB3NB?=
human HCT116 cells M3fKcWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVexN|gxOyCmYYnz MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME25MlQ{KM7:TR?= NYLUdIZxOjF5MUGwOVQ>
mouse CT26 cells MVnDfZRwfG:6aXPpeJkh[XO|YYm= NVjrXW9JOyCmYYnz NGjsPZdEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBEXDJ4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOzFizszN NYLKVI5jOjF5MUGwOVQ>
human PC3 cells MUXDfZRwfG:6aXPpeJkh[XO|YYm= NETYRmk{KGSjeYO= NGXhTW9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME24MlI5KM7:TR?= NV;MXXJzOjF5MUGwOVQ>
MES-SA cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= NVnJT29SOyCmYYnz MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXMuW0FiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE3PSEQvF2= NGi0ToozOTdzMUC1OC=>
human HPAC cells NV7OZ3JQS3m2b4TvfIlkcXS7IHHzd4F6 MY[zJIRigXN? Ml\TR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHBCSyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUmuN|Ih|ryP MkG4NlE4OTFyNUS=
mouse P388D1 cells M2Xye2N6fG:2b4jpZ4l1gSCjc4PhfS=> MoXyN{Bl[Xm| MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQN|g5TDFiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlI5PSEQvF2= NI\ZemUzOTdzMUC1OC=>
CCRF-CEM cells NELYU5VEgXSxdH;4bYNqfHliYYPzZZk> M3PxNFczKGh? NFv5cYNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMECwOUDPxE1? NYLRUndTOjF6NEC3NlI>
human Raji cells MkO0R5l1d3SxeHnjbZR6KGG|c3H5 MkHmO|IhcA>? MnvXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVoFrcSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFA6KM7:TR?= MWiyNVg1ODd{Mh?=
human HuH7 cells NW\q[5AxS3m2b4TvfIlkcXS7IHHzd4F6 NGjEZpE4OiCq MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MT64JO69VQ>? MY[yOVQ3OjJ5Nx?=
human T47D cells NXz2dnlYS3m2b4TvfIlkcXS7IHHzd4F6 MWi3NkBp MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD63JO69VQ>? M{jjV|I2PDZ{Mke3
human HCT116 cells M2LKNGN6fG:2b4jpZ4l1gSCjc4PhfS=> MnW2O|IhcA>? NH3yNnhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjNizszN NX3xTm5POjV2NkKyO|c>
human K562 cells MkO4VJJwdGmoZYLheIlwdiCjc4PhfS=> NW\JUnd2PDhiaB?= M4P1XGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTBizszN MnjsNlU6PjB|MkO=
human SKHEP1 cells MULQdo9tcW[ncnH0bY9vKGG|c3H5 MWi0PEBp NVHuUmZKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSg{txO NV7iTWFXOjV7NkCzNlM>
human MOLT3 cells NYHYXGsxWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUTudGlHPDhiaB?= NG\nVJFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1{LkOg{txO NUn5cXNHOjV7NkCzNlM>
human KG1 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 NUXFdWZwPDhiaB?= NUe3T4l5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLS|Eh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMjFOwG0> MmPQNlU6PjB|MkO=
human RPMI8226 cells NFHQdY9Rem:uaX\ldoF1cW:wIHHzd4F6 M{jBeVQ5KGh? NIrl[JhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLQUWk5OjJ4IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22JO69VQ>? NX3sVWhZOjV7NkCzNlM>
human MCF7 cells NGnoWmJRem:uaX\ldoF1cW:wIHHzd4F6 M1K1[lQ5KGh? MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ2KM7:TR?= NYTQV29xOjV7NkCzNlM>
human SK-UT-1B cells NWfRb|FOWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFy1OYQ1QCCq MnPERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3VWE0ySiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MTFOwG0> MWGyOVk3ODN{Mx?=
L1210 cell lines NEHDN2dHfW6ldHnvckBie3OjeR?= NW\zdGVjUW5idnn0do8hcW6qaXLpeI9zgSCnZn\lZ5Qhf2G|IITld5Rm\CCob4KgZ5l1d3O2YYTpZ{Bi[3Srdnn0fUBwdiC2aHWg[5Jwf3SqIH;mJI12emmwZTDs[ZVs\W2rYzDMNVIyOCClZXzsJIxqdmW|LDDJSFUxRTBwMEOg{txO NV7VNHlKOjl7NU[2Oi=>
P388 leukemic cell lines Mni2SpVv[3Srb36gZZN{[Xl? M3vmT2lvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDsfY1xcG:rZDDu[Y9xdGG|bTDQN|g5KGyndXvlcYlkKGOnbHygcIlv\XNuIFnEOVA:OC5yMzFOwG0> MWWyPVk2PjZ4
human BV173 cells M135[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NVjYTIRsOyCmYYnz MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWlE4OyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFAxQCEQvF2= MWGyNVcyOTB3NB?=

... 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]
- Collapse
  • 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]
- Collapse
  • 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
Smiles NC1=NC(=NC2=C1N=C[N]2C3CC(O)C(CO)O3)Cl

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04121065 Not yet recruiting Procedure: Blood withdrawal Relapsing Multiple Sclerosis Neuromed IRCCS January 2020 --
NCT03963375 Recruiting Drug: Cladribine Multiple Sclerosis|Multiple Sclerosis Relapsing-Remitting Washington University School of Medicine|EMD Serono October 2019 Phase 4
NCT03933202 Recruiting Drug: Cladribine Tablets Multiple Sclerosis EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono July 22 2019 --
NCT03933215 Recruiting Drug: Cladribine Tablets Multiple Sclerosis EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono May 21 2019 --
NCT03745144 Recruiting Drug: Cladribine|Drug: Placebo|Drug: Microgynon® Relapsing Multiple Sclerosis (RMS) Merck KGaA Darmstadt Germany January 17 2019 Phase 1
NCT03235973 Recruiting Drug: Fludarabine-Cladribine-Busulfan conditioning regimen Leukemia Myeloid Acute|Leukemia Lymphoblastic Acute Institut Paoli-Calmettes April 28 2018 Phase 1

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

DNA/RNA Synthesis Signaling Pathway Map

Related DNA/RNA Synthesis Products

Tags: buy Cladribine | Cladribine supplier | purchase Cladribine | Cladribine cost | Cladribine manufacturer | order Cladribine | Cladribine distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID