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
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
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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) [1] Adenosine deaminase (RPMI8226 cells) [1] Adenosine deaminase (U266 cells) [1]
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。[1] Cladribine在HSB2细胞中具有浓度依赖性诱导细胞凋亡的潜能。[2] 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。[3] Cladribine降低CD14+单核细胞,以及CD4+和CD8+ T淋巴细胞的迁移能力。[4]
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。[5] 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。[6]
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 --

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

体内溶解度
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

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,: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: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: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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