Fludarabine
别名: FaraA, Fludarabinum, NSC 118218 中文名称：氟达拉滨
Fludarabine在血管平滑肌细胞中是一种STAT1活化抑制剂，特异性降低STAT1蛋白质水平（和mRNA水平） ，而对其他STATs无此作用。它还是一种DNA合成抑制剂。Fludarabine可诱导凋亡。
Fludarabine Chemical Structure
CAS: 21679-14-1
产品质控
批次：
纯度：
99.95%
99.95
Fludarabine相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Fludarabine在血管平滑肌细胞中是一种STAT1活化抑制剂，特异性降低STAT1蛋白质水平（和mRNA水平） ，而对其他STATs无此作用。它还是一种DNA合成抑制剂。Fludarabine可诱导凋亡。 | |
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Fludarabine有效抑制RPMI8226细胞增殖,呈时间浓度依赖性。Fludarabine处理MM.1S和MM.1R细胞48小时的IC50分别为13.48μg/mL和33.79μg/mL。而Fludarabine处理U266细胞48小时的IC 50为222.2μg/mL。Fludarabine处理可增加处于细胞周期G 1期的细胞数量，并伴随着处于细胞周期S期细胞数量的减少，对细胞周期的影响呈时间依赖性。Fludarabine在MM细胞中诱导细胞周期阻滞和细胞凋亡。Fludarabine时间依赖性的诱导caspase，-8，- 9和- 3，- 7的剪切，继而诱导PARP的剪切 。氟达拉滨以时间梯度增加Bax基因表达，而Bak基因表达量不变。RPMI 8226细胞用Fludarabine处理12小时，处理后细胞膜电位降低，61.05%的细胞表达低荧光罗丹明123，而未处理的对照组细胞仅为8.62%[1]。为提高溶解度，Fludarabine可制为一磷酸盐形式(F-ara-AMP, fudarabine)，在静脉滴注后即可即时、定量的从母核上去磷酸化。细胞内重磷酸化修饰导致Fludarabine-阿糖胞苷三磷酸（(F-ara-ATP）。该代谢产物抑制了DNA复制的几个关键过程，如DNA合成所需酶，比如核糖核酸还原酶，DNA引发酶，DNA聚合酶，具有3 ' - 5 '外切酶活性的脱氧核糖核酸聚合酶δ和ε和DNA连接酶[2]。通过检测ICAM - 1的表达和IL - 8释放，表明Fludarabine还可以诱导前炎症刺激单核细胞的增加[3]。Fludarabine对卵巢癌细胞系生长无影响，而它对黑色素瘤细胞系有明显的剂量依赖性抑制[4]。Fludarabine是一种STAT1抑制剂，可特异性降低STAT1而不影响STAT1家族的其他成员[5]。除了细胞质积累外，重复低剂量顺铂(RLDC)还诱导HMGB1表达，该表达被STAT1敲除明显抑制。Fludarabine在RLDC治疗的肾小管细胞中始终呈剂量依赖性地抑制HMGB1的表达[5]。 |
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| 细胞实验 | 细胞系 | 地塞米松敏感(MM.1S) 和耐受 (MM.1R) 的人MM 细胞系, RPMI8226和 U266 细胞系 | ||
| 浓度 | 2 μg/mL | |||
| 孵育时间 | 24 小时 | |||
| 方法 | 对地塞米松敏感(MM.1S) 和耐受 (MM.1R) 的人MM 细胞系, RPMI8226和 U266 细胞系以5 × 105细胞密度铺板，实验组均包括氟达拉滨处理和空白对照组。处理后细胞用PBS清洗两次然后用70%冰乙醇固定，离心后用含100μg/mL核糖核酸酶PBS重悬浮，37ºC孵育30分钟。样品重悬于25μg/mL碘化吡啶中，用流式细胞仪检测。根据产品说明用Annexin V-FITC试剂盒检测细胞凋亡。利用TUNEL（末端脱氧核苷酸转移酶介导脱氧核苷酸缺口末端标记）法和原位细胞凋亡检测试剂盒处理细胞，最后用流式细胞仪分析。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | procaspase-9 / procaspase-3 p-p53 / p53 STAT1 |
|
27223263 | |
| Immunofluorescence | α-SMA / Vimentin |
|
28322315 | |
| Growth inhibition assay | Cell viability |
|
24956101 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | PBS对照组中肿瘤细胞增长迅速，25天内扩增为10倍。而用40mg/kgFludarabine处理的肿瘤扩增不超过5倍。40mg/kgFludarabine对RPMI 8226细胞有明显的抗肿瘤效果。RPMI 8226处理肿瘤细胞十天后增加凋亡细胞核数量。[1] Fludarabine可在免疫缺陷小鼠中有效抑制RPMI 8226细胞的骨髓转移。 |
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|---|---|---|
| 动物实验 | Animal Models | 携带RPMI 8226肿瘤细胞的免疫缺陷型小鼠 |
| Dosages | 40 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05390814 | Recruiting | Primary Central Nervous System Lymphoma |
Assistance Publique - Hôpitaux de Paris |
December 18 2023 | Phase 1 |
| NCT05201183 | Withdrawn | Acute Myeloid Leukemia|Chronic Myeloid Leukemia|Acute Lymphocytic Leukemia|Myelodysplastic Syndromes |
Naoyuki G. Saito M.D. Ph.D.|Indiana University |
October 2023 | Phase 1|Phase 2 |
| NCT05917405 | Recruiting | Acute Myeloid Leukemia in Remission |
Nantes University Hospital |
September 14 2023 | Phase 2 |
化学信息&溶解度
| 分子量 | 285.23 | 分子式 | C10H12FN5O4 |
| CAS号 | 21679-14-1 | SDF | Download Fludarabine SDF |
| Smiles | C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)O)F)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 57 mg/mL ( (199.83 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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体内溶解配方 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。
技术支持
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常见问题及建议解决方法
问题 1:
how to re-suspend and deliver the inhibitor for in vivo experiments?
回答：
For S1491, Fludarabine, we tested a vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W that you can resuspend the compound in at up to 30mg/ml. It's a suspension and can only be given via oral gavage.
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