| CAS |
4291-63-8 |
| Chinese Name |
克拉屈滨 |
| English Name |
Cladribine |
| Synonyms |
2-CdA;2-chlorodeoxyadenosine;CldAdo;2-Chloro-2-deoxyadenosine |
| Molecular Formula |
C10H12ClN5O3 |
| Molecular Weight |
285.69 |
| Solubility |
Soluble in DMSO |
| Purity |
HPLC≥99% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 224-427-9 |
| MDL |
MFCD00153939 |
| SMILES |
OC[C@@H]1[C@H](C[C@H](N2C=NC3=C2N=C(Cl)N=C3N)O1)O |
| InChIKey |
PTOAARAWEBMLNO-KVQBGUIXSA-N |
| InChI |
InChI=1S/C10H12ClN5O3/c11-10-14-8(12)7-9(15-10)16(3-13-7)6-1-4(18)5(2-17)19-6/h3-6,17-18H,1-2H2,(H2,12,14,15)/t4-,5+,6+/m0/s1 |
| PubChem CID |
20279 |
| Target Point |
Adenosine Deaminase |
| Passage |
Metabolic Enzyme&Protease |
| Background |
Cladribine is an adenosine deaminase inhibitor. |
| Biological Activity |
Cladribine is a well-known purine nucleoside analog with particular activity against lymphoproliferative disorders, such as hairy cell leukemia (HCL).[1] |
| IC50 |
Adenosine deaminase(MM1.S cells): 0.18μM;Adenosine deaminase(RPMI8226 cells): 0.75μM;Adenosine deaminase(U266 cells): 2.43μM [1] |
| In Vitro |
Cladribine exhibited inhibitory effects on MM cells in vitro. Cladribine inhibited cell proliferation of MM cells in a dose-dependent manner，although the three MM cell lines exhibited a remarkably different responsiveness to cladribine. The IC50 of cladribine for U266，RPMI8226，or MM1.S cells was approximately 2.43，0.75，or 0.18 μmol/L，respectively. Treatment with cladribine resulted in a significant G1 arrest in U266 and RPMI8226 cells，but only a minor increase in the G1 phase for MM1.S cells. Cladribine induced apoptosis of U266 cells in a dose-dependent manner. Cladribine induced PARP cleavage and activation of caspase-8 and caspase-3. Meanwhile，treatment with cladribine led to a remarkable reduction of the phosphorylated STAT3(P-STAT3). [1] |
| In Vivo |
Cladribine(0.7-3.5 mM)and/or diltiazem(2.4 mM)，was injected intraperitoneally into adult zebrafish and red blood cell(RBC)lysates were assayed by HPLC for levels of purine nucleotides(e.g. ATP)，potential biomarkers of cardiovascular health. Diltiazem increased RBC ATP concentrations，which were inhibited by co-injection of cladribine.[2] |
| Data Literature Source |
[1]. Ma J，Wang S，Zhao M，Deng XS，Lee CK，Yu XD，Liu B. Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer. 2011 Jun 16;11:255.
[2]. Klein LC，Yeung PK，Berman JN. Cladribine inhibits a diltiazem-induced increase in red blood cell purine nucleotide concentrations in a zebrafish model. Biomarkers. 2009 Dec;14(8):554-9. |
| Unit |
Bottle |
| Specification |
10mg 50mg 100mg |
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