| 应用 |
It is a chlorinated purine nucleoside with activity against lymphoproliferative disorders, such as hairy cell leukemia (HCL) and multiple myeloma (MM). 2-CdA resists ADA degradation and is phosphorylated to CdATP in lymphocytes. CdATP incorporation into DNA induces strand breaks and the activation of apoptosis. 2-CdA may also be used in studies involving the inhibition of DNA polymerase(s).
Cladribiane, like fludarabine, is a prodrug that is must be phosphorylated intracellularly to the monophosphate by the nuclear/cytosol enzyme deoxycytidine kinase (dCK) and possibly by the mitochondrial enzyme deoxyguanosine kinase (dGK). |
| 产品介绍 |
Cladribine是一种腺苷脱氨酶抑制剂，作用于U266， RPMI8226，和MM1.S细胞，IC50分别约为2.43 μM， 0.75 μM，和0.18 μM。 |
| 备注 |
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. |
| 生化机理 |
2-Chloro-2'-deoxyadenosine is a deoxyadenosine analog that induces apoptosis in chronic lymphocytic leukemia (CLL) cells. Studies show that 2-chloro-2′-deoxyadenosine can be produced from intact cells of Escherichia coli that produce B-2194 thermostable purine-nucleoside phosphorylase II. In addition, in vitro studies show that 2-Chloro-2′-deoxyadenosine can inhibit human T and B cell lymphoproliferative responses possibly by inhibiting DNA repair. Furthermore, Staphylococcus aureus Cowan-induced expression of CD25 on B-cells is suppressed by 2-Chloro-2′-deoxyadenosine. 2-Chloro-2′-deoxyadenosine is an inhibitor of Adenosine deaminase. |
| 别名 |
CdA;克拉利宾;克拉屈滨;2-氯-2'-脱氧腺嘌呤核苷;2-氯-9-(2-脱氧-β-D-呋喃阿拉伯糖基)腺嘌呤;CdA;2CdA;CldAdo; Leustat; Leustatin; 2-Chloro-2'-deoxyadenosine;2-Chloro-9-(2-deoxy-β-D-arabinofuranosyl)adenine |
