Cladribine (Synonyms: 2-Chlorodeoxyadenosine, Jk 6251, NSC 105014, RWJ 26251) |
| Katalog-Nr.GC10509 |
Cladribin (2-Chlor-2′-desoxyadenosin), ein Purin-Nukleosid-Analogon, ist ein oral wirksamer Adenosin-Desaminase-Hemmer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 4291-63-8
Sample solution is provided at 25 µL, 10mM.
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Cladribine is an adenosine deaminase inhibitor.Adenosine deaminase is an enzyme that involved in purine metabolism.
Cladribine is a well-known purine nucleoside analog with particular activity against lymphoproliferative disorders, such as hairy cell leukemia (HCL). In U266, RPMI8226 and MM1.S cells, Cladribine inhibited cell proliferation in a dose-dependant way with IC50 value of 2.43, 0.75 and 0.18 μmol/L, respectively. Apoptosis assays showed that Cladribine induced apoptosis of U266, RPMI8226 and MM1.S cells in a dose-dependant way [1]. In MM1.S cells, Cladribine (0.2uM) induces activation of caspase-3, -8, and -9 and PARP cleavage in a time-dependent way and reduces the phospho-STAT3 levels in a dose-dependent way. Also, Cladribine induces accumulation of DNA strand breaks and then activates the tumor suppressor p53 in lymphocytes [1].
In the treatment of indolent lymphoid malignancies, lower doses of Cladribine (5 mg/m2/week) are highly active and possibly better tolerated than standard doses [2].
References:
[1]. Ma J, Wang S, Zhao M, et al. Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer, 2011, 11: 255.
[2]. Robak T, Korycka A, Robak E. Older and new formulations of cladribine. Pharmacology and clinical efficacy in hematological malignancies. Recent Pat Anticancer Drug Discov, 2006, 1(1): 23-38.
| Cas No. | 4291-63-8 | SDF | |
| Überlieferungen | 2-Chlorodeoxyadenosine, Jk 6251, NSC 105014, RWJ 26251 | ||
| Chemical Name | (2R,3S,5R)-5-(6-amino-2-chloropurin-9-yl)-2-(hydroxymethyl)oxolan-3-ol | ||
| Canonical SMILES | C1C(C(OC1N2C=NC3=C2N=C(N=C3N)Cl)CO)O | ||
| Formula | C10H12ClN5O3 | M.Wt | 285.69 |
| Löslichkeit | ≥ 41.7mg/mL in DMSO with gentle warming | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5003 mL | 17.5015 mL | 35.003 mL |
| 5 mM | 0.7001 mL | 3.5003 mL | 7.0006 mL |
| 10 mM | 0.35 mL | 1.7501 mL | 3.5003 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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