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Cladribine

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Chemical Structure| 4291-63-8 同义名 : 克拉屈滨 ;2-Chloro-2′-deoxyadenosine;CldAdo;* 2chlorodeoxyadenosine.;2CdA. Code name: RWJ26251. Chemical structure names: * 2chloro2deoxyadenosine;Leustatine. Abbreviations: 2CDA;Cladribina. US brand name: Leustatin. Foreign brand names: Leustat;NSC 105014;Jk 6251;​2-Chlorodeoxyadenosine;RWJ 26251;2CdA
CAS号 : 4291-63-8
货号 : A410468
分子式 : C10H12ClN5O3
纯度 : 98%
分子量 : 285.687
MDL号 : MFCD00153939
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(105.01 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 10 mg/mL(35 mM)，配合低频超声助溶
动物实验配方：

5% DMSO+30% PEG 300+1% Tween 80+water 10 mg/mL

生物活性
描述 Adenosine Deaminase (ADA) is a housekeeping enzyme in purine metabolism that is unique and essential in the differentiation and maturation of the immune system and thus can be the cause of human severe combined immune deficiency. Cladribine is a well-known ADA inhibitor against lymphoproliferative disorders with IC50 for U266, RPMI8226, or MM1.S cells approximately 2.43, 0.75, or 0.18 μM respectively. In U266 cells, cladribine treatment gradually increased the percentage of cells in the G1 phase from 42% to 45%, 62%, 66% at 24, 48, 72 hrs, respectively. And the percentage of cells in S phase reduced from 50% to 36%, 26%, 23% at 24, 48, 72 hrs, respectively. The percentage of cells in G2/M phase increased from 8% to 19% at 24 hrs and then decreased to 11% at 72 hrs. Cladribine also induced the cells’ apoptosis with percentages of 5%, 15%, 21% and 33% when U266 cells were untreated or treated with 2, 5, 10 μM of cladribine, respectively. In RPMI8226 cells, 2μM cladribine treatment led to 14% increasing of cells in G1 phase and 18% decreasing in S phase at 24 hrs. And the percentages of apoptosis cells were improved in a dose-dependent manner when treated with 0.5, 1, 2 μM of cladribine, respectively. Similar cell cycle induction results with treatment of 0.5μM cladribine and apoptosis induction results with treatment of 0.1, 0.2, 0.5μM cladribine were observed in MM1.S cells. Furthermore, treatment of 0.2μM cladribine could be effective in reducing P-STAT3 in MM1.S cells while the concentrations were 1 μM in RPMI8226 and 2 μM in U266 cells[1]. When applied the cladribine in four patients with systemic mastocytosis (SM), the IC50 for HMC-1.1 and HMC-1.2 cells were 300 nM and 10 nM respectively, suggesting that the codon 816 mutant may improve the responses to this drug. Cell apoptosis were also induced when treated with 0.5 and 1 μM of cladribine, the survival of HMC-1.2 cells was much stronger. The expression of apoptosis related CD95 in HMC-1.2 cells were also substantially promoted by 0.5 μM cladribine with stimulation index (SI) raised from 1 to 3 and with that of CD164 raised from 1 to 2. The expression SI of CD87 only in HMC-1.1 cells were raised from 1 to 5, while no effect on CD87 was observed in HMC-1.2 cells[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
BT549 cells Cytotoxicity assay 3 days Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123 μM 21711054
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM 1732556
CCRF-CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM 21840722
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02096055 Leukemia Phase 2 Active, not recruiting April 2026 United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00691652 Lymphoma Phase 1 Phase 2 Terminated - United States, Oregon ... 展开 >> Knight Cancer Institute at Oregon Health and Science University Portland, Oregon, United States, 97239-3098 收起 <<
NCT00117598 Lymphoma Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.50mL

0.70mL

0.35mL

17.50mL

3.50mL

1.75mL

35.00mL

7.00mL

3.50mL
参考文献

[1]Ma J. Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer. 2011 Jun 16;11:255. doi: 10.1186/1471-2407-11-255.

[2]Guchelaar HJ, Vermes I, et al. Apoptosis-and necrosis-inducing potential of cladribine, cytarabine, cisplatin, and 5-fluorouracil in vitro: a quantitative pharmacodynamic model. Cancer Chemother Pharmacol. 1998;42(1):77-83.

[3]Scheible H, Laisney M, et al. Comparison of the in vitro and in vivo metabolism of Cladribine (Leustatin, Movectro) in animals and human. Xenobiotica. 2013 Dec;43(12):1084-94.

[4]Hayes CD, Dey D, et al. Chronic cladribine administration increases amyloid beta peptide generation and plaque burden in mice. PLoS One. 2012;7(10):e45841.

[5]Cladribine

[6]Böhm A. In vitro and in vivo growth-inhibitory effects of cladribine on neoplastic mast cells exhibiting the imatinib-resistant KIT mutation D816V. Exp Hematol. 2010 Sep;38(9):744-55. doi: 10.1016/j.exphem.2010.05.006. Epub 2010 May 27.