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

Clofarabine Chemical Structure

CAS: 123318-82-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) 743.68 现货
10mg 581.27 现货
50mg 2224.02 现货
1g 11850.93 现货
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Clofarabine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
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
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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
Ribonucleotide reductase [1]
(Cell-free assay)
65 nM
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]
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)

体外溶解度
批次:

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

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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