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DNA Damage/DNA Repair
DNA/RNA Synthesis inhibitor
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RNR inhibitor
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Autophagy activator
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Apoptosis related activator
Clofarabine
僅限科研使用
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
CAS: 123318-82-1
產(chǎn)品質(zhì)控
批次：
純度：
99.90%
99.90
Clofarabine相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) RK-33 Triapine (3-AP) Carmofur BMH-21 B02 YK-4-279 Bergapten Azaguanine-8 Halofuginone Adenine HCl Tegafur (FT-207) Mizoribine Cyclocytidine HCl Thymidine Nedaplatin APX-3330 Flupirtine maleate Pritelivir (BAY 57-1293) 6-Thio-dG JH-RE-06 TK216 CRT0044876 Adenine Tubercidin Amenamevir Madrasin ML216 PFM01 BC-LI-0186 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫 細(xì)胞周期化合物庫 | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
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(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | Clofarabine通過兩種促進(jìn)型和平衡型核苷轉(zhuǎn)運(yùn)蛋白，hENT1 和 hENT2，以及一種集中型核苷轉(zhuǎn)運(yùn)蛋白，hCNT253，有效地轉(zhuǎn)運(yùn)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(jìn)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(yùn)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(yùn)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(diǎn)。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(shí)體腫瘤細(xì)胞系中，Clofarabine在體外表現(xiàn)出強(qiáng)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(dú)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(hào) | 123318-82-1 | SDF | Download Clofarabine SDF |
| Smiles | C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)F)Cl)N | ||
| 儲(chǔ)存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 60 mg/mL ( (197.57 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 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(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請輸入動(dòng)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(jì)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(jìn)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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