Pemetrexed disodium
别名: LY-231514 disodium 中文名称：培美曲塞二钠
Pemetrexed disodium是一种新型抗叶酸和抗代谢药物，作用于TS，DHFR和GARFT，无细胞试验中Ki分别为1.3 nM，7.2 nM 和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。
Pemetrexed disodium Chemical Structure
CAS: 150399-23-8
产品质控
批次：
纯度：
99.97%
99.97
Pemetrexed disodium相关产品
| 相关产品 | Calcium Folinate | 点击展开 |
|---|---|---|
| 相关化合物库 | 代谢化合物库 抗癌代谢化合物库 谷氨酰胺代谢化合物库 糖代谢化合物库 脂代谢化合物库 | 点击展开 |
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 |
|---|---|---|---|---|---|
| A549 | Function Assay | 2.5 μM | 48 h | induces caspase-9, caspase-3 and poly (ADP-ribose) polymerase (PARP) cleavage | 24991768 |
| H1792 | Function Assay | 2.5 μM | 48 h | induces caspase-9, caspase-3 and poly (ADP-ribose) polymerase (PARP) cleavage | 24991768 |
| A549 | Function Assay | 2.5/5/10 μM | 48 h | downregulates Mcl-1 | 24991768 |
| H1792 | Function Assay | 2.5/5/10 μM | 48 h | downregulates Mcl-1 | 24991768 |
| A549 | Apoptosis Assay | 2.5 μM | 48 h | induces apoptosis | 24991768 |
| A549 | Function Assay | 5 μM | 8 h | increases Mcl-1 ubiquitination levels | 24991768 |
| A549 | Function Assay | 1 µM | 4/8/12/24/48 h | increases the level of phosphorylated Akt in a time dependent manner | 24847863 |
| A549 | Function Assay | 0.1/0.3/1 μM | 48 h | increases the level of phosphorylated Akt in a dose dependent manner | 24847863 |
| A549 | Apoptosis Assay | 0.1/0.3/1 μM | 48 h | induces apoptosis in a dose dependent manner | 24847863 |
| A549 | Function Assay | 0.1/0.3/1 μM | 48 h | increases the ratio of S-phase population | 24847863 |
| PC9 | Function Assay | 16 nM | 72 h | induces S-phase arrest | 24840891 |
| PC9/GR | Function Assay | 4.94 μM | 72 h | induces S-phase arrest | 24840891 |
| PC9 | Apoptosis Assay | 16 nM | 72 h | induces 14.54﹪ apoptosis | 24840891 |
| PC9/GR | Apoptosis Assay | 4.94 μM | 72 h | induces 19.54﹪ apoptosis | 24840891 |
| PC9/GR | Function Assay | 4.94 μM | 72 h | increases p-ERK levels | 24840891 |
| PC9/GR | Function Assay | 4.94 μM | 72 h | increases p-AKT levels | 24840891 |
| A549 | Cell Viability Assay | 0.1/0.3/0.5/1 μM | 24/48 h | inhibits cell viability dose and time dependently | 24626722 |
| A549 | Function Assay | 0.1/0.3/0.5/1 μM | 24/48 h | produces the formation of AVOs in a dose-dependent manner | 24626722 |
| H226 | Cell Viability Assay | 1-10 μg/ml | 72 h | IC50>10 μg/ml | 24378576 |
| H290 | Cell Viability Assay | 1-10 μg/ml | 72 h | IC50>10 μg/ml | 24378576 |
| Y-meso14 | Cell Viability Assay | 1-10 μg/ml | 72 h | IC50>10 μg/ml | 24378576 |
| MSTO-211H | Cell Viability Assay | 1-10 μg/ml | 72 h | IC50~0.04 μg/ml | 24378576 |
| HT-29 | Function Assay | 0.05 μM | 72 h | increases the percentage of cells in the S phase | 23959460 |
| LoVo | Function Assay | 0.05 μM | 72 h | increases the percentage of cells in the S phase | 23959460 |
| BXPC-3 | Function Assay | 39.86 μM | 24 h | induces S arrest (P<0.05) and decreases the number of cells in the G2/M phase | 22977607 |
| BXPC-3 | Function Assay | 39.86 μM | 24 h | enhances EGFR phosphorylated levels, and the protein levels | 22977607 |
| PANC-1 | Function Assay | 84 μM | 24 h | enhances EGFR phosphorylated levels, and the protein levels | 22977607 |
| BXPC-3 | Function Assay | 39.86 μM | 24 h | enhances EGFR, HER3 and AKT phosphorylation levels | 22977607 |
| PANC-1 | Function Assay | 84 μM | 24 h | enhances EGFR, HER3 and AKT phosphorylation levels | 22977607 |
| H1792 | Function Assay | 2.5/5/10 μM | 48 h | increases Noxa expression significantly | 24991768 |
| A549 | Function Assay | 2.5/5/10 μM | 48 h | increases Noxa expression significantly | 24991768 |
| A549 | Function Assay | 1 μM | 48 h | leads to mitochondrial dysfunction combined with simvastatin | 25096993 |
| MSTO-211 | Function Assay | 1 μM | 48 h | leads to mitochondrial dysfunction combined with simvastatin | 25096993 |
| A549 | Function Assay | 1 μM | 48 h | enhances intracellular ROS production combined with simvastatin | 25096993 |
| MSTO-211 | Function Assay | 1 μM | 48 h | enhances intracellular ROS production combined with simvastatin | 25096993 |
| A549 | Apoptosis Assay | 1 μM | 48 h | enhances caspase-dependent apoptosis combined with simvastatin | 25096993 |
| MSTO-211 | Apoptosis Assay | 1 μM | 48 h | enhances caspase-dependent apoptosis combined with simvastatin | 25096993 |
| A549 | Cell Viability Assay | 1 μM | 48 h | produces a synergistic inhibitory effect on the cell growth combined with simvastatin | 25096993 |
| MSTO-211 | Cell Viability Assay | 1 μM | 48 h | produces a synergistic inhibitory effect on the cell growth combined with simvastatin | 25096993 |
| H1299 | Cell Viability Assay | 1-1000 nM | 72 h | IC50=178 nM | 25145669 |
| A549 | Cell Viability Assay | 1-1000 nM | 72 h | IC50=137 nM | 25145669 |
| MG-63 | Cell Viability Assay | 0.01-100 μM | 72 h | inhibits cell viability dosedependently | 25152399 |
| U20S | Cell Viability Assay | 0.01-100 μM | 72 h | inhibits cell viability dosedependently | 25152399 |
| HepG3 | Function Assay | 10 μM | 48 h | upregulates phosphorylated (p-) MEK1/2 (Ser217/221) and p-ERK1/2 (Thr202/Tyr204) | 25446102 |
| HepG3 | Function Assay | 0.1–100 μM | 48 h | activates cyto-protective autophagy | 25446102 |
| HepG3 | Function Assay | 0.1–100 μM | 48 h | induces p62 downregulation as well as Beclin-1 and LC3B-II upregulation | 25446102 |
| HepG2 | Apoptosis Assay | 0.1–100 μM | 72 h | induces apoptosis slightly at high concerntration | 25446102 |
| HepG2 | Cell Viability Assay | 0.1–100 μM | 72 h | high concentrations of pemetrexed at (10/100 μM) only slightly inhibits HepG2 cell survival | 25446102 |
| A459 | Apoptosis Assay | 4μM | 48 h | induces apoptosis | 25743822 |
| A459 | Function Assay | 1/2/4 μM | 48 h | decreases the levels of p-Akt | 25743822 |
| A459 | Function Assay | 1/2/4 μM | 24/48 h | induces G1 phase arrest in dose- and time dependent manner | 25743822 |
| T47D | Growth Inhibition Assay | 0.234 mM | 72 h | growth inhibition=30﹪ | 25975637 |
| HeLa | Growth Inhibition Assay | 0.234 mM | 72 h | growth inhibition=20﹪ | 25975637 |
| A549 | Growth Inhibition Assay | 0.234 mM | 72 h | growth inhibition=50﹪ | 25975637 |
| Vero | Growth Inhibition Assay | 0.234 mM | 72 h | growth inhibition=20﹪ | 25975637 |
| T47D | Growth Inhibition Assay | 0.234 mM | 48 h | growth inhibition=20﹪ | 25975637 |
| HeLa | Growth Inhibition Assay | 0.234 mM | 48 h | growth inhibition=10﹪ | 25975637 |
| A549 | Growth Inhibition Assay | 0.234 mM | 48 h | growth inhibition=30﹪ | 25975637 |
| Vero | Growth Inhibition Assay | 0.234 mM | 48 h | growth inhibition=10﹪ | 25975637 |
| T47D | Growth Inhibition Assay | 0.234 mM | 24 h | growth inhibition=10﹪ | 25975637 |
| HeLa | Growth Inhibition Assay | 0.234 mM | 24 h | growth inhibition=5﹪ | 25975637 |
| A549 | Growth Inhibition Assay | 0.234 mM | 24 h | growth inhibition=10﹪ | 25975637 |
| Vero | Growth Inhibition Assay | 0.234 mM | 24 h | growth inhibition=5﹪ | 25975637 |
| A549 | Function Assay | 1 μM | 48 h | increases AMPK phosphorylation and a concomitant decrease in AKT and mTOR phosphorylation cotreated with simvastatin | 26334320 |
| MSTO-211H | Function Assay | 1 μM | 48 h | increases AMPK phosphorylation and a concomitant decrease in AKT and mTOR phosphorylation cotreated with simvastatin | 26334320 |
| A549 | Apoptosis Assay | 1 μM | 24 h | induces apoptosis cotreated with simvastatin | 26334320 |
| MSTO-211H | Apoptosis Assay | 1 μM | 24 h | induces apoptosis cotreated with simvastatin | 26334320 |
| A549 | Function Assay | 1 μM | 24 h | enhances autophagy cotreated with simvastatin | 26334320 |
| MSTO-211H | Function Assay | 1 μM | 24 h | enhances autophagy cotreated with simvastatin | 26334320 |
| A549 | Cell Viability Assay | 1 μM | 48 h | enhances simvastatin inhibited viability | 26334320 |
| MSTO-211H | Cell Viability Assay | 1 μM | 48 h | enhances simvastatin inhibited viability | 26334320 |
| KB | Function assay | 1 uM | 24 hrs | Induction of apoptotic activity in human KB cells at 1 uM after 24 hrs | 18680275 |
| PC43-10 | Function assay | 10 uM | 2 mins | Inhibition of human RFC-mediated [3H]MTX uptake in chinese hamster PC43-10 cells at 10 uM after 2 mins relative to control | 21879757 |
| KB | Function assay | 1 uM | 48 hrs | Inhibition of AICARFTase in human KB cells assessed as phosphorylated AMPK at 1 uM after 48 hrs by Western blot analysis | 24256410 |
| KB | Cell cycle arrest assay | 1 uM | 48 hrs | Cell cycle arrest in human KB cells assessed as accumulation at G1/G0 phase at 1 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control | 24256410 |
| R2/PCFT4 | Function assay | 0.5 uM | 5 mins | Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as intracellular drug level at 0.5 uM at 37 degC at pH 5.5 measured over 5 mins | 26317331 |
| R2 | Function assay | 10 uM | Inhibition of human PCFT-mediated [3H]MTX uptake ectopically expressed in chinese hamster R2 cells at 10 uM at pH 5.5 to 7.2 | 21879757 | |
| PC9 | Growth Inhibition Assay | 72 h | IC50=16.05±1.85 nM | 24840891 | |
| PC9/GR | Growth Inhibition Assay | 72 h | IC50=4.94±0.440 μM | 24840891 | |
| A549 | Growth Inhibition Assay | 96 h | IC50=1.35 μM | 24348854 | |
| A549/PEM-1.6 | Growth Inhibition Assay | 96 h | IC50=5.03 μM | 24348854 | |
| A549/PEM-6.4 | Growth Inhibition Assay | 96 h | IC50=23.39 μM | 24348854 | |
| A549/PEM-16 | Growth Inhibition Assay | 96 h | IC50=51.45 μM | 24348854 | |
| HT-29 | Growth Inhibition Assay | 72 h | IC50=10.07 ± 0.94 μM | 23959460 | |
| LoVo | Growth Inhibition Assay | 72 h | IC50=0.032 ± 0.002 μM | 23959460 | |
| SW620 | Growth Inhibition Assay | 72 h | IC50=1.09 ± 0.01 μM | 23959460 | |
| HCT116 | Growth Inhibition Assay | 72 h | IC50=0.049 ± 0.013 μM | 23959460 | |
| SW1116 | Growth Inhibition Assay | 72 h | IC50=1.70 ± 0.03 μM | 23959460 | |
| WiDr | Growth Inhibition Assay | 72 h | IC50=0.019 ± 0.002 μM | 23959460 | |
| STAV-AB | Growth Inhibition Assay | 48 h | proportion of live cells=64.4±21.8 % | 23840376 | |
| M-14-K | Growth Inhibition Assay | 48 h | proportion of live cells=81.8±12.9 % | 23840376 | |
| STAV-FCS | Growth Inhibition Assay | 48 h | proportion of live cells=88.1±8.9 % | 23840376 | |
| ZL-34 | Growth Inhibition Assay | 48 h | proportion of live cells=95.7±6.5 % | 23840376 | |
| JL-1 | Growth Inhibition Assay | 48 h | proportion of live cells=98.2±2.2 % | 23840376 | |
| DM-3 | Growth Inhibition Assay | 48 h | proportion of live cells=101.3±2.8 % | 23840376 | |
| Jurkat | Growth Inhibition Assay | 48 h | proportion of live cells=76.7±4.3 % | 23840376 | |
| KB | Function assay | 30 mins | IC50 = 0.03 μM | 19371039 | |
| R2 | Antiproliferative assay | 10 to 14 days | IC50 = 0.00494 μM | 21879757 | |
| R2 | Antiproliferative assay | 96 hrs | IC50 = 0.0132 μM | 21879757 | |
| RT16 | Antiproliferative assay | 96 hrs | IC50 = 0.042 μM | 21879757 | |
| D4 | Antiproliferative assay | 96 hrs | IC50 = 0.06 μM | 21879757 | |
| KB | Antiproliferative assay | 96 hrs | IC50 = 0.068 μM | 21879757 | |
| IGROV1 | Antiproliferative assay | 96 hrs | IC50 = 0.102 μM | 21879757 | |
| PC43-10 | Antiproliferative assay | 96 hrs | IC50 = 0.138 μM | 21879757 | |
| IGROV1 | Antiproliferative assay | 96 hrs | IC50 = 0.2 μM | 21879757 | |
| D4 | Antiproliferative assay | 96 hrs | IC50 = 0.254 μM | 21879757 | |
| KB | Antiproliferative assay | 96 hrs | IC50 = 0.327 μM | 21879757 | |
| RT16 | Antiproliferative assay | 96 hrs | IC50 = 0.388 μM | 21879757 | |
| R2 | Antiproliferative assay | 96 hrs | IC50 = 0.894 μM | 21879757 | |
| R2(VC) | Antiproliferative assay | 96 hrs | IC50 = 0.974 μM | 21879757 | |
| R2 | Growth inhibition assay | 96 hrs | IC50 = 0.0132 μM | 24111942 | |
| RT16 | Growth inhibition assay | 96 hrs | IC50 = 0.042 μM | 24111942 | |
| D4 | Growth inhibition assay | 96 hrs | IC50 = 0.06 μM | 24111942 | |
| KB | Growth inhibition assay | 96 hrs | IC50 = 0.068 μM | 24111942 | |
| PC43-10 | Growth inhibition assay | 96 hrs | IC50 = 0.138 μM | 24111942 | |
| D4 | Growth inhibition assay | 96 hrs | IC50 = 0.254 μM | 24111942 | |
| KB | Growth inhibition assay | 96 hrs | IC50 = 0.327 μM | 24111942 | |
| RT16 | Growth inhibition assay | 96 hrs | IC50 = 0.388 μM | 24111942 | |
| MTXRII-OuaR2-4 | Growth inhibition assay | 96 hrs | IC50 = 0.894 μM | 24111942 | |
| R2(VC) | Growth inhibition assay | 96 hrs | IC50 = 0.974 μM | 24111942 | |
| KB | Cytotoxicity assay | 96 hrs | IC50 = 0.00994 μM | 24256410 | |
| KB | Function assay | 30 mins | IC50 = 0.01174 μM | 24256410 | |
| RT16 | Cytotoxicity assay | 96 hrs | IC50 = 0.0182 μM | 24256410 | |
| R2 | Cytotoxicity assay | 96 hrs | IC50 = 0.0223 μM | 24256410 | |
| PC43-10 | Cytotoxicity assay | 96 hrs | IC50 = 0.0306 μM | 24256410 | |
| KB | Cytotoxicity assay | 96 hrs | IC50 = 0.69 μM | 24256410 | |
| R2/PCFT4 | Function assay | 96 hrs | IC50 = 0.0132 μM | 25234128 | |
| RT16 | Function assay | 96 hrs | IC50 = 0.042 μM | 25234128 | |
| D4 | Function assay | 96 hrs | IC50 = 0.06 μM | 25234128 | |
| KB | Cytotoxicity assay | 96 hrs | IC50 = 0.068 μM | 25234128 | |
| PC43-10 | Function assay | 96 hrs | IC50 = 0.138 μM | 25234128 | |
| D4 | Function assay | 96 hrs | IC50 = 0.254 μM | 25234128 | |
| KB | Cytotoxicity assay | 96 hrs | IC50 = 0.327 μM | 25234128 | |
| RT16 | Function assay | 96 hrs | IC50 = 0.388 μM | 25234128 | |
| R2 | Cytotoxicity assay | 96 hrs | IC50 = 0.894 μM | 25234128 | |
| R2 | Cytotoxicity assay | 96 hrs | IC50 = 0.974 μM | 25234128 | |
| KB | Function assay | 1 hr | IC50 = 0.01174 μM | 25602637 | |
| R2/PCFT4 | Function assay | 96 hrs | IC50 = 0.0132 μM | 25602637 | |
| RT16 | Function assay | 96 hrs | IC50 = 0.042 μM | 25602637 | |
| R2 | Cytotoxicity assay | 96 hrs | IC50 = 0.042 μM | 25602637 | |
| KB | Antiproliferative assay | 96 hrs | IC50 = 0.068 μM | 25602637 | |
| PC43-10 | Function assay | 96 hrs | IC50 = 0.138 μM | 25602637 | |
| R2(VC) | Cytotoxicity assay | 96 hrs | IC50 = 0.974 μM | 25602637 | |
| KB | Cytotoxicity assay | 72 hrs | IC50 = 0.07 μM | 25668494 | |
| A549 | Cytotoxicity assay | 72 hrs | IC50 = 0.08 μM | 25668494 | |
| HepG2 | Cytotoxicity assay | 72 hrs | IC50 = 1.26 μM | 25668494 | |
| R2/PCFT4 | Function assay | 2 mins | K = 0.044 μM | 26317331 | |
| R2/PCFT4 | Function assay | 2 mins | K = 0.27 μM | 26317331 | |
| KB | Antiproliferative assay | 72 hrs | IC50 = 0.07 μM | 27017552 | |
| SW620 | Antiproliferative assay | 72 hrs | IC50 = 0.08 μM | 27017552 | |
| A549 | Antiproliferative assay | 72 hrs | IC50 = 1.26 μM | 27017552 | |
| KB | Function assay | 72 hrs | IC50 = 0.07 μM | 28830032 | |
| SW620 | Antiproliferative assay | 72 hrs | IC50 = 0.09 μM | 28830032 | |
| MCF7 | Antiproliferative assay | 72 hrs | IC50 = 0.65 μM | 28830032 | |
| R2/PCFT4 | Function assay | 96 hrs | IC50 = 0.0132 μM | 29425443 | |
| RT16 | Function assay | 96 hrs | IC50 = 0.042 μM | 29425443 | |
| D4 | Function assay | 96 hrs | IC50 = 0.06 μM | 29425443 | |
| KB | Antiproliferative assay | 96 hrs | IC50 = 0.068 μM | 29425443 | |
| PC43-10 | Function assay | 96 hrs | IC50 = 0.138 μM | 29425443 | |
| D4 | Function assay | 96 hrs | IC50 = 0.254 μM | 29425443 | |
| R2/PCFT4 | Function assay | 2 mins | Ki = 0.259 μM | 29425443 | |
| KB | Antiproliferative assay | 96 hrs | IC50 = 0.327 μM | 29425443 | |
| R2 | Cytotoxicity assay | 96 hrs | IC50 = 0.849 μM | 29425443 | |
| RT16 | Function assay | 96 hrs | IC50 = 0.894 μM | 29425443 | |
| R2(VC) | Growth inhibition assay | 96 hrs | IC50 = 0.974 μM | 29425443 | |
| A549 | Antiproliferative assay | 24 hrs | IC50 = 3.31 μM | 29807332 | |
| MDA-MB-231 | Antiproliferative assay | 24 hrs | IC50 = 3.85 μM | 29807332 | |
| OVCAR3 | Antiproliferative assay | 24 hrs | IC50 = 6.9 μM | 29807332 | |
| SGC7901 | Antiproliferative assay | 24 hrs | IC50 = 9.08 μM | 29807332 | |
| KB | Cytotoxicity assay | 96 hrs | Cytotoxicity against human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTitre-Blue fluorescence assay in presence of adenosine/AICA/thymidine | 24256410 | |
| KB | Function assay | 48 hrs | Inhibition of AICARFTase in human KB cells assessed as accumulation of ZMP after 48 hrs by HPLC analysis | 24256410 | |
| H28 | Growth Inhibition Assay | IC50=0.07±0.02 μM | 24714722 | ||
| 211H | Growth Inhibition Assay | IC50=0.07±0.01 μM | 24714722 | ||
| H2052 | Growth Inhibition Assay | IC50=0.57±0.34 μM | 24714722 | ||
| H2452 | Growth Inhibition Assay | IC50＞100 μM | 24714722 | ||
| MES01 | Growth Inhibition Assay | IC50＞100 μM | 24714722 | ||
| MES04 | Growth Inhibition Assay | IC50＞100 μM | 24714722 | ||
| H1993 | Growth Inhibition Assay | IC50=0.17 μM | 24418519 | ||
| H1299 | Growth Inhibition Assay | IC50=1.84 μM | 24418519 | ||
| BXPC-3 | Growth Inhibition Assay | IC50=39.86±1.68 μM | 22977607 | ||
| PANC-1 | Growth Inhibition Assay | IC50=83.76±0.19 μM | 22977607 | ||
| KB | Function assay | IC50 = 0.03 μM | 18680275 | ||
| RT16 | Antiproliferative assay | IC50 = 0.042 μM | 18680275 | ||
| D4 | Antiproliferative assay | IC50 = 0.06 μM | 18680275 | ||
| KB | Antiproliferative assay | IC50 = 0.068 μM | 18680275 | ||
| IGROV1 | Antiproliferative assay | IC50 = 0.102 μM | 18680275 | ||
| PC43-10 | Antiproliferative assay | IC50 = 0.138 μM | 18680275 | ||
| IGROV1 | Antiproliferative assay | IC50 = 0.2 μM | 18680275 | ||
| D4 | Antiproliferative assay | IC50 = 0.254 μM | 18680275 | ||
| KB | Antiproliferative assay | IC50 = 0.327 μM | 18680275 | ||
| RT16 | Antiproliferative assay | IC50 = 0.388 μM | 18680275 | ||
| R2 | Antiproliferative assay | IC50 = 0.894 μM | 18680275 | ||
| R2 | Function assay | Ki = 0.096 μM | 20085328 | ||
| R2 | Function assay | Ki = 1.54 μM | 20085328 | ||
| KB | Function assay | IC50 = 30 μM | 20085328 | ||
| R2 | Function assay | Ki = 0.094 μM | 22243528 | ||
| R2 | Function assay | Ki = 2.54 μM | 22243528 | ||
| R2 | Antiproliferative assay | Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as growth inhibition in the presence of 10 uM thymidine and 320 uM AICA | 21879757 | ||
| R2 | Antiproliferative assay | Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as growth inhibition in the presence of 60 uM adenosine | 21879757 | ||
| R2 | Function assay | Inhibition of GARFTase in chinese hamster R2 cells expressing human PCFT assessed as incorporation of [14C]glycine into [14C]formyl GAR in the presence of 4 uM azaserine | 21879757 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 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: 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 | ||
| 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 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| IGROV1 | Function assay | Effect on TS protein expression in human IGROV1 cells by Western blot analysis | 30035541 | ||
| IGROV1 | Function assay | Effect on DHFR protein expression in human IGROV1 cells by Western blot analysis | 30035541 | ||
| IGROV1 | Function assay | Effect on HSP90 protein expression in human IGROV1 cells by Western blot analysis | 30035541 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Pemetrexed disodium是一种新型抗叶酸和抗代谢药物，作用于TS，DHFR和GARFT，无细胞试验中Ki分别为1.3 nM，7.2 nM 和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | Pemetrexed 是结构新型的抗叶酸抗代谢药物。 | ||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Pemetrexed有效抑制胸苷酸合酶(TS)，Ki为1.3 nM, 也显著抑制其他关键叶酸酶, 包括二氢叶酸还原酶(DHFR)和甘氨酰胺核苷酸转甲酰酶(GARFT) ， Ki分别为7.2 nM和 65 nM。Pemetrexed作用于CCRF-CEM白血病, GC3/C1结肠癌, 和HCT-8 回盲肠癌细胞，具有抗增殖活性,IC50分别为25 nM, 34 nM 和220 nM。而且, 胸甘和次黄嘌呤联用作用于以上三种细胞系，完全可逆转LY231514引起的细胞毒性。[1] 最新研究显示Cisplatin和Pemetrexed联用作用于感染腺病毒表达SOCS-1载体的MPM细胞，通过抑制细胞增殖，侵入, 和 诱导凋亡而具有抗癌效果。[2] | |||
|---|---|---|---|---|
| 激酶实验 | 酶活实验 | |||
| 使用分光光度分析法检测340 nm处由于形成7,8-二氢叶酸产物而导致提高的吸光值，而测定胸苷酸合酶（TS）活性。实验buffer含50 mM N-三（羟甲基）甲基-2-氨基乙烷磺酸, 25 mM MgC12, 6.5 mM 甲醛, 1 mM EDTA, and 75 mM 2-巯基乙醇，pH 7.4。脱氧尿苷一磷酸, 6R-MTHF, 和 hIS 的浓度分别为100 μM, 30μM和 30 nM (1.7 毫单位/mL)。在 6R-MTHF 浓度时,在未受抑制反应中加入6种浓度的抑制剂进行反应。通过回归曲线分析，使用ENZFITTER程序应用用Morrison 等式获得Ki。通过分光光度计法检测在340 nm处底物NADPH 和 7,8-二氢叶酸的消失，而测定DHFR活性。反应在0.5 mL 50 mM磷酸钾buffer 中25oC下进行，磷酸钾buffer含150 mM KC1 和10 nM 2-巯基乙醇,pH 7.5,和14 nM (0.34 毫单位/mL) DHFR。NADPH浓度为 10 μM，7,8-dihydrofolate浓度为5, 10,或 15 μM。 在每种7,8-dihydrofolate浓度时 ，在未受抑制反应中加入7种浓度的抑制剂进行反应。通过回归曲线分析，用ENZFITI'ER微机程序，应用Morrison等式获得Ki值。使用分光光度分析法检测295 nm处由于形成5,8-二氢叶酸产物而导致提高的吸光值，而测定GARFT活性。反应溶剂含 75 mM HEPES,20% 甘油, 和 50 mM α-硫代甘油 , pH 7.5。使用的底物和酶是10 μM α,β-甘氨酰胺核糖核苷酸, 0-10 μM 10-甲基-5,8二氢叶酸, 及10 nM (1.9毫单位/mL) GARFT。使用Beckman DU640 分光光度计的酶应用程序， 通过回归曲线分析，应用Michaelis-Menten等式计算 Ki 值。 | ||||
| 细胞实验 | 细胞系 | CCRF-CEM白血病,GC3/C1 结肠癌,HCT-8回盲肠癌细胞 | ||
| 浓度 | 0到30 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 绘制剂量反应曲线测定IC50。Pemetrexed 溶于DMSO，浓度为4 mg/mL，然后用细胞培养基稀释到所需指定的浓度。培养在完全培养基中的CCRF-CEM白血病细胞加到24孔板上，总体积为2.0 mL。平行孔中加入不同浓度Pemetrexed，DMSO终体积为0.5%。然后在37oC下温育72小时。温育末期，使用ZBI Coulter 计数器测细胞数。在300 μM AICA, 5 μM 胸甘, 100 μM 次黄嘌呤,或5 μM 胸甘和100 μM次黄嘌呤同时存在时，测定每种化合物的 IC50值。为了测粘附的肿瘤细胞,使用修正的初始MTT 比色分析法测定细胞毒性。人类肿瘤细胞接种在96孔平底组织培养板中，每孔含100 μL实验培养基。实验培养基为含10% FCS 的无叶酸RPMI 1640培养基，2 nM 叶酸或2.3 μM叶酸作为唯一叶酸来源。孔1A 作为空白对照。抗叶酸储存液在Dulbecco's PBS中制备，浓度为1 mg/mL, 然后在PBS中连续稀释2倍。在三个重复孔中加入10 μL每种浓度的样品。然后在37oC下温育72小时。MTT溶于PBS，浓度为5 mg/mL,10 μL 储存MTF 溶液加到每孔中,然后在 37oC下再温育2小时。然后每孔中加入100 μL DMSO。然后通过MTT甲增溶,在 Dynatech MR600读数器上进行读数，检测波长为570 nm，参考波长为630 nm。测定IC50值。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-Chk1 / Chk1 / Cyclin D / Cyclin E / p-Histone H3 / Histone H3 / Cyclin B1 / p-Cdc2 / Cdc2 Topo IIα / Topo I / γH2AX / Cleaved PARP / Survivin AKT / p-AKT / GSK3β / p-GSK3β EGFR / p-EGFR |
|
22237209 | |
| Immunofluorescence | p-AKT |
|
24847863 | |
| Growth inhibition assay | Cell viability |
|
28719077 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Pemetrexed 作用于人类H460非小细胞肺癌移植瘤，推迟肿瘤生长。而且, Pemetrexed 和紫杉醇联用，更大程度推迟H460肿瘤生长，且和Vinorelbine及 Carboplatin产生添加反应。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 皮下注射EMT-6乳腺癌,人类HCT116结肠癌,和人类H460非小细胞肺癌的小鼠 |
| Dosages | 100 mg/kg或150 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06378892 | Recruiting | Non Small Cell Lung Cancer Metastatic|ALK Gene Mutation |
Centro di Riferimento Oncologico - Aviano |
March 15 2024 | Phase 2 |
| NCT06010277 | Recruiting | NSCLC|Mesothelioma|Thymoma |
Amphia Hospital|Albert Schweitzer Hospital |
February 6 2023 | Phase 4 |
化学信息&溶解度
| 分子量 | 471.37 | 分子式 | C20H19N5Na2O6 |
| CAS号 | 150399-23-8 | SDF | Download Pemetrexed disodium SDF |
| Smiles | C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)NC(CCC(=O)[O-])C(=O)[O-].[Na+].[Na+] | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
Water : 94 mg/mL (199.41 mM) DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 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。
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