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Fludarabine

別名: FaraA, Fludarabinum, NSC 118218 中文名稱：氟達拉濱

Fludarabine在血管平滑肌細胞中是一種STAT1活化抑制劑，特異性降低STAT1蛋白質水平（和mRNA水平） ，而對其他STATs無此作用。它還是一種DNA合成抑制劑。Fludarabine可誘導凋亡。

Fludarabine Chemical Structure

Fludarabine Chemical Structure

CAS: 21679-14-1

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1032.75 現(xiàn)貨
10mg 810.59 現(xiàn)貨
50mg 2525.07 現(xiàn)貨
200mg 5651.1 現(xiàn)貨
1g 7950.08 現(xiàn)貨
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Fludarabine相關產(chǎn)品

相關信號通路圖

STAT Signaling Pathways

STAT信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
EHEB Apoptosis Assay 40 μM 24 h induces apoptosis 23497075
HEC50B Apoptosis Assay 20/100 μM 24 h induces apoptosis slightly 23595697
AN3CA Apoptosis Assay 20/100 μM 24 h induces apoptosis in a dose-dependent manner 23595697
HEC1A Apoptosis Assay 20/100 μM 24 h induces apoptosis in a dose-dependent manner 23595697
HEC50B Growth Inhibition Assay 100-500 μM 24 h inhibits cell growth slightly 23595697
AN3CA Growth Inhibition Assay 100-500 μM 24 h inhibits cell growth in a dose-dependent manner 23595697
HEC1A Growth Inhibition Assay 100-500 μM 24 h inhibits cell growth in a dose-dependent manner 23595697
Reh Function Assay 10?μM 1/2/4 h induces autophagy 23681223
Nalm-6 Function Assay 10?μM 1/2/4 h induces autophagy 23681223
DU-145 Growth Inhibition Assay 0-10 μg/ml 48 h? inhibits cell growth in a dose-dependent manner 23734815
NALM6 Apoptosis Assay 5?μM 24 h induces cell apoptosis 24057147
I-83 Apoptosis Assay 5?μM 24 h induces cell apoptosis 24057147
BJAB Apoptosis Assay 5?μM 24 h induces cell apoptosis 24057147
HMECs? Function Assay 100?μM? 36?h inhibits IFNα?mediated phosphorylation of STAT1 and STAT3, but not of STAT2 24211327
HMECs Function Assay 100?μM? 36?h inhibits IFNγ?and LPS induced STAT1 phosphorylation and IRF1 expression 24211327
624.38mel? Function Assay 50-200 μM 24 h inhibits IDO activity independently of mRNA levels 24911872
MDA-231 Function Assay 50-200 μM 24 h inhibits IDO activity independently of mRNA levels 24911872
624.38mel? Function Assay 50 μM 24 h decreases IDO expression 24911872
MDA-231 Function Assay 100 μM 24 h decreases IDO expression 24911872
PBMC Function Assay 50/100 μM 24 h inhibits STAT1 phosphorylation 24911872
Raji? Function Assay 3?μM 24/48/72 h induces accumulations of p53, p63 and p73? 24940695
KBM3/Bu2506 Apoptosis Assay 2.5 μM 48 h induces apoptosis slightly 25111583
MOLM 13 Apoptosis Assay 2.5 μM 48 h induces apoptosis slightly 25111583
THP-1 Apoptosis Assay 2.5 μM 48 h induces apoptosis slightly 25111583
MV-4-11 Apoptosis Assay 2.5 μM 48 h induces apoptosis slightly 25111583
Jeko-1? Function Assay 20 μM 24 h inhibits expression of IDO 25940712
CLL? Apoptosis Assay 10 μM? 24-96 h induces apoptotic cell death 22207686
MEC1 Apoptosis Assay 100?μM 72 h induces apoptosis significantly 22132973
U937? Apoptosis Assay 0.8 μM 4-48 h induces apoptosis slightly 22074700
U937? Apoptosis Assay 1 μM 96 h induces apoptosis slightly 22023523
Daudi Apoptosis Assay 20 μM 96 h induces apoptosis slightly 22023523
J45.01 Apoptosis Assay 1 μM 96 h induces apoptosis slightly 22023523
NALM-6 Apoptosis Assay 10 μM? 24 h induces cell apoptosis slightly 21699383
JMV-3 Apoptosis Assay 10 μM? 24 h induces cell apoptosis slightly 21699383
EHEB Function Assay 5-50 μM 24 h decreases p21 expression significantly 21168391
JVM-2? Function Assay 30 μM 24 h decreases p21 expression 21168391
KBM3/Bu2506 Growth Inhibition Assay 0.6 μM 24 h increases the cell fraction in S-phase 20933509
HLE-B3? Function Assay 25 μM 48 h blocks IFN-γ–induced STAT1 phosphorylation and IDO expression 20435158
SKW6.4 Apoptosis Assay 0.01-10 μM 24/48 h induces cell death in both time- and dose- dependent manner 18092340
CCRF-CEM Function assay 10 uM 1 to 60 mins Drug transport in human CCRF-CEM cells assessed as ENT1-mediated uptake at 10 uM after 1 to 60 mins by liquid scintillation counting analysis 23388705
K562 Growth Inhibition Assay 72 h IC50=3.3 nM 20307198
RPMI 8226 Growth Inhibition Assay 24 h IC50=1.54?μM 17976186
MM.1S Growth Inhibition Assay 48 h IC50=13.48?μM 17976186
MM.1R Growth Inhibition Assay 48 h IC50=33.79 μM 17976186
CLL5 Antitumor assay 48 hrs Antitumor activity against CLL5 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 0.16 μM. 24673739
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human paclitaxel-resistant K562 cells after 72 hrs by MTT assay, IC50 = 0.26 μM. 20605656
CLL3 Antitumor assay 48 hrs Antitumor activity against CLL3 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 0.35 μM. 24673739
CLL4 Antitumor assay 48 hrs Antitumor activity against CLL4 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 0.64 μM. 24673739
CEM-DNR-B Cytotoxicity assay 72 hrs Cytotoxicity against human CEM-DNR-B cells after 72 hrs by MTT assay, IC50 = 1.01 μM. 20605656
CLL6 Antitumor assay 48 hrs Antitumor activity against CLL6 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 1.6 μM. 24673739
CLL2 Antitumor assay 48 hrs Antitumor activity against CLL2 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 2.66 μM. 24673739
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 6.6 μM. 25462277
PBMC Cytotoxicity assay 48 hrs Cytotoxicity against patient PBMC after 48 hrs by CellTitre-Blue assay in presenc of mouse M210B4 cells, IC50 = 10 μM. 25562417
CLL1 Antitumor assay 48 hrs Antitumor activity against CLL1 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 17.1 μM. 24673739
CEM Cytotoxicity assay 72 hrs Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50 = 19.49 μM. 20605656
T47D Cytotoxicity assay 72 hrs Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50 = 46.2 μM. 25462277
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 47.44 μM. 20605656
Reh Growth Inhibition Assay IC50 ～10?μM 23681223
Nalm-6 Growth Inhibition Assay IC50 ～10?μM 23681223
Nalm-6-FluR Growth Inhibition Assay IC50=250 μM 25061101
Molt-4 Growth Inhibition Assay IC50=180 μM 25061101
RPMI-8226 Growth Inhibition Assay IC50=500 μM 25061101
Mec-1 Growth Inhibition Assay IC50＞500 μM 25061101
U2937 Growth Inhibition Assay IC50=16 μM 25061101
Reh Growth Inhibition Assay IC50=30 μM 25061101
Nalm-6 Growth Inhibition Assay IC50=18 μM 25061101
A549 Growth Inhibition Assay IC50=15.7±2.8 μM 23377192
A549 GAPDH-deficient Growth Inhibition Assay IC50=18.5±2.3 μM 23377192
RPMI 8226 Growth Inhibition Assay IC50=25.9?±?3.7 μM 21948264
CEM Growth Inhibition Assay IC50=2.4?±?0.4 μM 21948264
Raji Growth Inhibition Assay IC50=0.47?±?0.04 μM 21948264
U937 Growth Inhibition Assay IC50=0.24?±?0.04 μM 21948264
K562 Growth Inhibition Assay IC50=0.44?±?0.05 μM 21948264
KBM3/Bu2506 Growth Inhibition Assay IC20=0.67 μM 20933509
MDA-MB-231 Growth Inhibition Assay IC50=4.0 μM 20447390
MCF-7 Growth Inhibition Assay IC50=15.0 μM 20447390
BW-225 Growth Inhibition Assay IC20=1.37 ×10?8?μM? 18661380
OH-65 Growth Inhibition Assay IC20=1.37 ×10?8?μM? 18661380
GR-145 Growth Inhibition Assay IC20=2.74 × 10?8 μM? 18661380
A549 Growth Inhibition Assay IC20=5.48 × 10?8 μM? 18661380
CaSki? Growth Inhibition Assay IC20=1.37 × 10?7 μM? 18661380
ZMK-1 Growth Inhibition Assay IC20=1.37 × 10?6 μM? 18661380
U937 Growth Inhibition Assay IC50=3,200 ± 560 nM 15930361
primary CLL Cytotoxicity assay Cytotoxicity against human primary CLL cells, LD50 = 1.1 μM. 25148392
CHO Function assay Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor, Ki = 10.4 μM. 7707320
JVM2 Antitumor assay Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis, EC50 = 10.4 μM. 24673739
HeLa Antitumor assay Antitumor activity against human HeLa cells assessed as cell viability by MTT assay, EC50 = 16 μM. 24673739
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
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
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Daoy qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 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
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 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
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 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
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells 29435139
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生物活性

產(chǎn)品描述 Fludarabine在血管平滑肌細胞中是一種STAT1活化抑制劑，特異性降低STAT1蛋白質水平（和mRNA水平） ，而對其他STATs無此作用。它還是一種DNA合成抑制劑。Fludarabine可誘導凋亡。
靶點
STAT1 [5]
(Vascular smooth muscle cells)
體外研究(In Vitro)
體外研究活性

Fludarabine有效抑制RPMI8226細胞增殖,呈時間濃度依賴性。Fludarabine處理MM.1S和MM.1R細胞48小時的IC50分別為13.48μg/mL和33.79μg/mL。而Fludarabine處理U266細胞48小時的IC 50為222.2μg/mL。Fludarabine處理可增加處于細胞周期G 1期的細胞數(shù)量，并伴隨著處于細胞周期S期細胞數(shù)量的減少，對細胞周期的影響呈時間依賴性。Fludarabine在MM細胞中誘導細胞周期阻滯和細胞凋亡。Fludarabine時間依賴性的誘導caspase，-8，- 9和- 3，- 7的剪切，繼而誘導PARP的剪切 。氟達拉濱以時間梯度增加Bax基因表達，而Bak基因表達量不變。RPMI 8226細胞用Fludarabine處理12小時，處理后細胞膜電位降低，61.05%的細胞表達低熒光羅丹明123，而未處理的對照組細胞僅為8.62%[1]。為提高溶解度，F(xiàn)ludarabine可制為一磷酸鹽形式(F-ara-AMP, fudarabine)，在靜脈滴注后即可即時、定量的從母核上去磷酸化。細胞內重磷酸化修飾導致Fludarabine-阿糖胞苷三磷酸（(F-ara-ATP）。該代謝產(chǎn)物抑制了DNA復制的幾個關鍵過程，如DNA合成所需酶，比如核糖核酸還原酶，DNA引發(fā)酶，DNA聚合酶，具有3 ' - 5 '外切酶活性的脫氧核糖核酸聚合酶δ和ε和DNA連接酶[2]。通過檢測ICAM - 1的表達和IL - 8釋放，表明Fludarabine還可以誘導前炎癥刺激單核細胞的增加[3]。Fludarabine對卵巢癌細胞系生長無影響，而它對黑色素瘤細胞系有明顯的劑量依賴性抑制[4]。Fludarabine是一種STAT1抑制劑，可特異性降低STAT1而不影響STAT1家族的其他成員[5]。除了細胞質積累外，重復低劑量順鉑(RLDC)還誘導HMGB1表達，該表達被STAT1敲除明顯抑制。Fludarabine在RLDC治療的腎小管細胞中始終呈劑量依賴性地抑制HMGB1的表達[5]。
細胞實驗 細胞系 地塞米松敏感(MM.1S) 和耐受 (MM.1R) 的人MM 細胞系, RPMI8226和 U266 細胞系
濃度 2 μg/mL
孵育時間 24 小時
方法

對地塞米松敏感(MM.1S) 和耐受 (MM.1R) 的人MM 細胞系, RPMI8226和 U266 細胞系以5 × 105細胞密度鋪板，實驗組均包括氟達拉濱處理和空白對照組。處理后細胞用PBS清洗兩次然后用70%冰乙醇固定，離心后用含100μg/mL核糖核酸酶PBS重懸浮，37ºC孵育30分鐘。樣品重懸于25μg/mL碘化吡啶中，用流式細胞儀檢測。根據(jù)產(chǎn)品說明用Annexin V-FITC試劑盒檢測細胞凋亡。利用TUNEL（末端脫氧核苷酸轉移酶介導脫氧核苷酸缺口末端標記）法和原位細胞凋亡檢測試劑盒處理細胞，最后用流式細胞儀分析。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot procaspase-9 / procaspase-3

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