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
CAS: 4291-63-8
产品质控
批次：
纯度：
99.99%
99.99
Cladribine相关产品
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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 | ||
| 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 |
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| 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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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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