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。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 prodrμg 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).
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, respectivelyIt 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).
CAS编号：4291-63-8
敏感性：对热敏感

熔点
220°C
溶解性：Soluble in DMSO ( ≥57 mg/ml), water (<1 mg/ml), ethanol (<1 mg/ml), and methanol.
储存温度：2-8°C储存
Reaxys-RN：624220
RTECS：AU7357560

MDL号：MFCD00153939
分子量：285.69
分子式：C10H12ClN5O3
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PubChem CID：20279