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Clofarabine

別名: Clolar 中文名稱：克羅拉濱,氯法拉濱

Clofarabine (Clolar)抑制 ribonucleotide reductase (RNR) (IC50 = 65 nM)和 DNA polymerase 的酶活性。Clofarabine 可誘導(dǎo)自噬和凋亡。

Clofarabine Chemical Structure

Clofarabine Chemical Structure

CAS: 123318-82-1

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 743.68 現(xiàn)貨
10mg 581.27 現(xiàn)貨
50mg 2224.02 現(xiàn)貨
1g 11850.93 現(xiàn)貨
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Clofarabine相關(guān)產(chǎn)品

相關(guān)信號通路圖

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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

產(chǎn)品描述 Clofarabine (Clolar)抑制 ribonucleotide reductase (RNR) (IC50 = 65 nM)和 DNA polymerase 的酶活性。Clofarabine 可誘導(dǎo)自噬和凋亡。
靶點
Ribonucleotide reductase [1]
(Cell-free assay)
65 nM
體外研究(In Vitro)
體外研究活性 Clofarabine通過兩種促進型和平衡型核苷轉(zhuǎn)運蛋白，hENT1 和 hENT2，以及一種集中型核苷轉(zhuǎn)運蛋白，hCNT253，有效地轉(zhuǎn)運到細(xì)胞內(nèi)。Clofarabine被細(xì)胞溶質(zhì)中的激酶逐步磷酸化為核苷類似物Clofarabine 5′-單-，雙-和三磷酸鹽，然后進入細(xì)胞，Clofarabine三磷酸鹽為活性形式。Clofarabine 5′-單-，雙-和三磷酸鹽不是核苷轉(zhuǎn)運蛋白的底物，必須被5′-核苷酸酶酶促轉(zhuǎn)化為它們的去磷酸化形式轉(zhuǎn)運出細(xì)胞。Clofarabine三磷酸鹽是核苷酸還原酶(IC50 = 65 nM)的有效抑制劑，推測通過調(diào)節(jié)亞基結(jié)合到變構(gòu)位點。Clofarabine直接作用于線粒體，通過改變跨膜電位，將細(xì)胞色素C，凋亡誘導(dǎo)因子(AIF)，凋亡蛋白酶活化因子1 (APAF1)和caspase 9釋放到細(xì)胞質(zhì)。在多種白血病和實體腫瘤細(xì)胞系中，Clofarabine在體外表現(xiàn)出強的生長抑制作用和細(xì)胞毒性(IC50值= 0.028–0.29 μM)。Clofarabine能夠增加HL6細(xì)胞中dCK的活性，也能增加K562細(xì)胞中ara-C單-，雙-和三磷酸鹽的形成。[1] Clofarabine (10 μM)抑制4-過氧氫環(huán)磷酰胺(4-HC)引起的修復(fù)，在慢性淋巴細(xì)胞白血病(CLL)淋巴細(xì)胞中，抑制峰值為5 μM細(xì)胞內(nèi)濃度。Clofarabine (10 μM)與4-過氧氫環(huán)磷酰胺(4-HC)結(jié)合比各自單獨使用能夠產(chǎn)生更多的額外凋亡性細(xì)胞死亡。[2] Clofarabine (1 μM)與ara-C (10 μM)結(jié)合產(chǎn)生ara-CTP的生化調(diào)節(jié)作用，并協(xié)同殺死K562細(xì)胞。[3]
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 在無胸腺裸鼠或重癥聯(lián)合免疫缺陷小鼠體內(nèi)，Clofarabine腹腔內(nèi)給藥對各種皮下移植的人腫瘤移植物具有顯著的活性。[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 --

化學(xué)信息&溶解度

分子量 303.68 分子式

C10H11ClFN5O3
CAS號 123318-82-1 SDF Download Clofarabine SDF
Smiles C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)F)Cl)N
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 60 mg/mL ( (197.57 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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