Clofarabine
别名: Clolar 中文名称：克罗拉滨,氯法拉滨
Clofarabine (Clolar)抑制 ribonucleotide reductase (RNR) (IC50 = 65 nM)和 DNA polymerase 的酶活性。Clofarabine 可诱导自噬和凋亡。
Clofarabine Chemical Structure
CAS: 123318-82-1
客户使用Selleck的Clofarabine发表文献20篇
客户使用该产品的2个实验数据
产品质控
批次：
纯度：
99.90%
99.90
Clofarabine相关产品
| 相关靶点 | tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase | 点击展开 |
|---|---|---|
| 相关化合物库 | FDA药物库 天然产物库 凋亡分子化合物库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
相关信号通路图
DNA/RNA Synthesis抑制剂选择性比较
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 |
|---|---|---|---|---|---|
| U373-MAGI | Function assay | 50 nM | 2 hrs | Potentiation of 5-Aza-C-induced antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as 5-Aza-C EC50 at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs and subsequent viral infection measu, EC50=30.4μM | 27117260 |
| U373-MAGI | Antiviral assay | 50 nM | 4 hrs | Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in viral infectivity at 50 nM incubated for 4 hrs prior to viral infection measured at 72 hrs post infection by flow cytometric analysis | 27117260 |
| U373-MAGI | Function assay | 200 nM | 6 hrs | Reduction in dGTP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis | 27117260 |
| U373-MAGI | Function assay | 200 nM | 6 hrs | Reduction in dCTP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis | 27117260 |
| U373-MAGI | Function assay | 200 nM | 6 hrs | Reduction in dATP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis | 27117260 |
| U373-MAGI | Function assay | 50 nM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis | 27117260 |
| U373-MAGI | Function assay | 200 nM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-C | 27117260 |
| U373-MAGI | Function assay | 50 nM | 2 hrs | Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 |
| U373-MAGI | Function assay | 200 nM | 2 hrs | Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 |
| U373-MAGI | Function assay | 200 nM | 2 hrs | Reduction in dRGU-TP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis | 27117260 |
| U373-MAGI | Function assay | 200 nM | 2 hrs | Reduction in 5-aza-dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis | 27117260 |
| U373-MAGI | Function assay | 200 nM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 |
| U373-MAGI | Function assay | 50 nM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 |
| MT4 | Cytostatic assay | 5 days | Cytostatic activity against human MT4 cells after 5 days by SRB assay, GI50=0.051μM | 21711054 | |
| NCI-H23 | Cytostatic assay | 5 days | Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.04μM | 21711054 | |
| HCT15 | Cytotoxicity assay | 5 days | Cytotoxicity against human HCT15 cells after 5 days by SRB assay, GI50=0.18μM | 19929004 | |
| BT549 | Cytotoxicity assay | 5 days | Cytotoxicity against human BT549 cells after 5 days by SRB assay, GI50=0.065μM | 19929004 | |
| PC3 | Cytotoxicity assay | 5 days | Cytotoxicity against human PC3 cells after 5 days by SRB assay, GI50=0.063μM | 19929004 | |
| NCI-H23 | Cytotoxicity assay | 5 days | Cytotoxicity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.04μM | 19929004 | |
| PC3 | Cytostatic assay | 5 days | Cytostatic activity against human PC3 cells after 5 days by SRB assay, GI50=0.063μM | 21711054 | |
| BT549 | Cytostatic assay | 5 days | Cytostatic activity against human BT549 cells after 5 days by SRB assay, GI50=0.065μM | 21711054 | |
| A549 | Cytostatic assay | 5 days | Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.086μM | 21711054 | |
| HCT116 | Cytostatic assay | 5 days | Cytostatic activity against human HCT116 cells after 5 days by SRB assay, GI50=0.106μM | 21711054 | |
| DU145 | Cytostatic assay | 5 days | Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.125μM | 21711054 | |
| HCT15 | Cytostatic assay | 5 days | Cytostatic activity against human HCT15 cells after 5 days by SRB assay, GI50=0.18μM | 21711054 | |
| Hs578 | Cytostatic assay | 5 days | Cytostatic activity against human Hs578 cells after 5 days by SRB assay, GI50=1.241μM | 21711054 | |
| HL60 | Cytostatic assay | 48 hrs | Cytostatic activity against human HL60 cells after 48 hrs by MTT assay, IC50=0.1μM | 23820572 | |
| A549 | Cytostatic assay | 48 hrs | Cytostatic activity against human A549 cells after 48 hrs by MTT assay, IC50=8μM | 23820572 | |
| Granta | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Granta cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.017μM | 30176535 | |
| HL60 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.04μM | 30176535 | |
| CCRF-CEM | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CCRF-CEM cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.044μM | 30176535 | |
| RL | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RL cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.38μM | 30176535 | |
| L1210 cell | Cytotoxicity assay | Compound was tested for cytotoxicity against L1210 cell lines, IC50=2.3 μM | 1732556 | ||
| CCRF-CEM cell lines | Cytotoxicity assay | Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.05 μM | 1732556 | ||
| HEp-2 cell | Cytotoxicity assay | Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.012 μM | 1732556 | ||
| K562 cell | Cytotoxicity assay | Compound was tested for cytotoxicity against K562 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 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 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 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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: Orthogonal 3D viability 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 | Clofarabine (Clolar)抑制 ribonucleotide reductase (RNR) (IC50 = 65 nM)和 DNA polymerase 的酶活性。Clofarabine 可诱导自噬和凋亡。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Clofarabine通过两种促进型和平衡型核苷转运蛋白，hENT1 和 hENT2，以及一种集中型核苷转运蛋白，hCNT253，有效地转运到细胞内。Clofarabine被细胞溶质中的激酶逐步磷酸化为核苷类似物Clofarabine 5′-单-，双-和三磷酸盐，然后进入细胞，Clofarabine三磷酸盐为活性形式。Clofarabine 5′-单-，双-和三磷酸盐不是核苷转运蛋白的底物，必须被5′-核苷酸酶酶促转化为它们的去磷酸化形式转运出细胞。Clofarabine三磷酸盐是核苷酸还原酶(IC50 = 65 nM)的有效抑制剂，推测通过调节亚基结合到变构位点。Clofarabine直接作用于线粒体，通过改变跨膜电位，将细胞色素C，凋亡诱导因子(AIF)，凋亡蛋白酶活化因子1 (APAF1)和caspase 9释放到细胞质。在多种白血病和实体肿瘤细胞系中，Clofarabine在体外表现出强的生长抑制作用和细胞毒性(IC50值= 0.028–0.29 μM)。Clofarabine能够增加HL6细胞中dCK的活性，也能增加K562细胞中ara-C单-，双-和三磷酸盐的形成。[1] Clofarabine (10 μM)抑制4-过氧氢环磷酰胺(4-HC)引起的修复，在慢性淋巴细胞白血病(CLL)淋巴细胞中，抑制峰值为5 μM细胞内浓度。Clofarabine (10 μM)与4-过氧氢环磷酰胺(4-HC)结合比各自单独使用能够产生更多的额外凋亡性细胞死亡。[2] Clofarabine (1 μM)与ara-C (10 μM)结合产生ara-CTP的生化调节作用，并协同杀死K562细胞。[3] | |||
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| 体内研究(In Vivo) | ||
| 体内研究活性 | 在无胸腺裸鼠或重症联合免疫缺陷小鼠体内，Clofarabine腹腔内给药对各种皮下移植的人肿瘤移植物具有显著的活性。[1] | |
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05917405 | Recruiting | Acute Myeloid Leukemia in Remission |
Nantes University Hospital |
September 14 2023 | Phase 2 |
| NCT03609814 | Completed | Hematologic Malignancies|Nonmalignant Diseases|Immunodeficiencies|Hemoglobinopathies|Genetic Inborn Errors of Metabolism|Fanconi''s Anemia|Thalassemia|Sickle Cell Disease |
University of California San Francisco |
January 26 2016 | -- |
化学信息&溶解度
| 分子量 | 303.68 | 分子式 | C10H11ClFN5O3 |
| CAS号 | 123318-82-1 | SDF | Download Clofarabine SDF |
| Smiles | C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)F)Cl)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 60 mg/mL ( (197.57 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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