Home Neuronal Signaling Adenosine Deaminase inhibitor - DNA/RNA Synthesis inhibitor Cladribine 仅限科研使用

Cladribine

别名: 2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251 中文名称：克拉利宾

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。

Cladribine Chemical Structure

Cladribine Chemical Structure

CAS: 4291-63-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) 979.91 现货
25mg 792.01 现货
50mg 1382.86 现货
1g 7944.3 现货
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Cladribine相关产品

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息(PMID)
CT26 Cytotoxicity assay 3 days Cytotoxicity against mouse CT26 cells after 3 days by MTT assay, IC50=0.131μM 21711054
BT549 Cytotoxicity assay 3 days Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123μM 21711054
BV173 Cytotoxicity assay 3 days Cytotoxicity against human BV173 cells after 3 days by MTT assay, IC50=0.0008μM 21711054
human SK-UT-1B cells Proliferation assay 48 h Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=1 μM 25960323
human MCF7 cells Proliferation assay 48 h Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=45 μM 25960323
human RPMI8226 cells Proliferation assay 48 h Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM 25960323
human KG1 cells Proliferation assay 48 h Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.2 μM 25960323
human MOLT3 cells Proliferation assay 48 h Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2.3 μM 25960323
human SKHEP1 cells Proliferation assay 48 h Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=4 μM 25960323
human K562 cells Proliferation assay 48 h Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=10 μM 25960323
human HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.3 μM 25462277
human T47D cells Cytotoxicity assay 72 h Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50=0.7 μM 25462277
human HuH7 cells Cytotoxicity assay 72 h Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay, IC50=1.8 μM 25462277
human Raji cells Cytotoxicity assay 72 h Cytotoxicity against human Raji cells after 72 hrs by MTT assay, IC50=0.009 μM 21840722
CCRF-CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM 21840722
MES-SA Cytotoxicity assay 3 days Cytotoxicity against human MES-SA cells after 3 days by MTT assay, IC50=0.165μM 21711054
K562 Cytotoxicity assay 3 days Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay, IC50=0.17μM 21711054
P388D1 Cytotoxicity assay 3 days Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay, IC50=0.285μM 21711054
CEM-DNR-bulk Cytotoxicity assay 3 days Cytotoxicity against human CEM-DNR-bulk cells after 3 days by MTT assay, IC50=0.352μM 21711054
L1210 Cytotoxicity assay 3 days Cytotoxicity against mouse L1210 cells after 3 days by MTT assay, IC50=0.393μM 21711054
EL4 Cytotoxicity assay 3 days Cytotoxicity against mouse EL4 cells after 3 days by MTT assay, IC50=0.848μM 21711054
MCF7 Cytotoxicity assay 3 days Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=2.35μM 21711054
K562 Cytotoxicity assay 3 days Cytotoxicity against human K562 cells after 3 days by MTT assay, IC50=7.69μM 21711054
PC3 Cytotoxicity assay 3 days Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=8.28μM 21711054
C6 Cytotoxicity assay 3 days Cytotoxicity against rat C6 cells after 3 days by MTT assay, IC50=9.07μM 21711054
HPAC Cytotoxicity assay 3 days Cytotoxicity against human HPAC cells after 3 days by MTT assay, IC50=9.32μM 21711054
HCT116 Cytotoxicity assay 3 days Cytotoxicity against human HCT116 cells after 3 days by MTT assay, IC50=9.43μM 21711054
HT-29 Cytotoxicity assay 3 days Cytotoxicity against human HT-29 cells after 3 days by MTT assay, IC50=9.44μM 21711054
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=0.3μM 28219046
HuH7 Cytotoxicity assay 72 hrs Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=1.8μM 28219046
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=2μM 28219046
P388 leukemic cell lines Function assay In vitro inhibitory effect was tested for cytostatic activity on the growth of lymphoid neoplasm P388 leukemic cell lines, ID50=0.03 μM 2995666
L1210 cell lines Function assay In vitro inhibitory effect was tested for cytostatic activity on the growth of murine leukemic L1210 cell lines, ID50=0.03 μM 2995666
L1210 cell lines Cytotoxicity assay Compound was tested for cytotoxicity against L1210 cell lines, IC50=0.07 Μm 1732556
HEp-2 cell lines Cytotoxicity assay Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.03 μM 1732556
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM 1732556
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 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。
特性 Cladribine主要在淋巴组织中具有活性。
靶点
Adenosine deaminase (MM1.S cells) Adenosine deaminase (RPMI8226 cells) Adenosine deaminase (U266 cells)
0.18 μM 0.75 μM 2.43 μM
体外研究(In Vitro)
体外研究活性 Cladribine对毛细胞白血病(HCL)，一种慢性B淋巴细胞增生疾病发挥显著的活性，延长完全缓解期。Cladribine诱导DNA链断裂累积，随后激活淋巴细胞中抑癌基因p53。Cladribine可能调节MM细胞中STAT3活性。Cladribine剂量依赖性抑制U266，RPMI8226和MM1.S细胞的增殖/存活。其中U266对cladribine敏感性最低，而对MM1.S敏感性最高。Cladribine治疗逐渐增加细胞周期中G1期的细胞比例，并减少S期细胞。Cladribine处理24小时后似乎能够增加U266细胞中G2-M期的比例。在RPMI8226和MM1.S细胞中都能观察到cladribine诱导的细胞凋亡剂量依赖性增加。0.2 μM cladribine治疗时间依赖性显著诱导MM1.S 中caspase-3，-8，和-9激活和PARP裂解。Cladribine剂量依赖性显著降低磷酸STAT3 (P-STAT3)水平，但是不影响总STAT3蛋白质水平。 Cladribine在HSB2细胞中具有浓度依赖性诱导细胞凋亡的潜能。 Cladribine以剂量依赖的方式抑制原代肥大细胞(MC)和MC系HMC-1生长，含有KIT D816V的HMC-1.2细胞与KIT D816V缺失的HMC-1.1细胞相比，具有较低的IC50值。 Cladribine降低CD14+单核细胞，以及CD4+和CD8+ T淋巴细胞的迁移能力。
细胞实验 细胞系 U266，RPMI8226 和 MM1.S
浓度 0 μM - 32 μM
孵育时间 72小时
方法 非放射性细胞增殖试剂盒用于测定细胞活性。简而言之，人MM细胞系U266，RPMI8226和MM1.S接种到96孔板，0.1 mL完全培养基(5% FBS)为对照组，0.1 mL包含一系列剂量cladribine的相同培养基为试验组，培养72小时。使用微板读书器在490 nm下读取所有孔中的细胞数量，每组相对于100%存活率对照组的存活细胞百分数，通过MTS的减少测定。
体内研究(In Vivo)
体内研究活性 Cladribine (0.7-3.5 mM)和/或diltiazem (2.4 mM)，腹腔注射到成年斑马鱼，通过HPLC分析心血管健康的潜在标志物，红血球(RBC)裂解物嘌呤核苷酸(例如ATP)的水平。Diltiazem增加RBC ATP浓度，该作用被共注射cladribine所抑制。 Ia 和s.c.给药后，伴随双相下降，Cladribine血浆浓度急速减少。单剂Cladribine 以1 mg/kg ia 和 2 mg/kg s.c. 注射后，AUC和t 1/2β分别为0.66: 1.2 μg ×h/mL和3.5: 4.5小时。
动物实验 Animal Models 成年野生型(AB)斑马鱼
Dosages 0.7 mM - 3.5 mM
Administration 腹腔注射给药
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05797740 Recruiting
Multiple Sclerosis
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 August 3 2023 --
NCT04997148 Completed
Relapsing-Remitting Multiple Sclerosis
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany
 August 11 2021 --
  • [1]https://pubmed.ncbi.nlm.nih.gov/21679466/
  • [2]https://pubmed.ncbi.nlm.nih.gov/9619762/
  • [3]https://pubmed.ncbi.nlm.nih.gov/20553795/
  • [4]https://pubmed.ncbi.nlm.nih.gov/19175384/
  • [5]https://pubmed.ncbi.nlm.nih.gov/20001707/
  • [6]https://pubmed.ncbi.nlm.nih.gov/19326772/
  • [7]https://pubmed.ncbi.nlm.nih.gov/12373351/

化学信息&溶解度

分子量 285.69 分子式

C10H12ClN5O3
CAS号 4291-63-8 SDF Download Cladribine SDF
Smiles C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 57 mg/mL ( (199.51 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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