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Pemetrexed Disodium (LY231514) Antifolate
Cat.nr.S1135
Chemische structuur
Molecuulgewicht: 471.37
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Kwaliteitscontrole
Batch:
Zuiverheid:
99.97%
99.97
| Gerelateerde doelwitten | Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras |
|---|---|
| Overig Antifolate Inhibitoren | L-5-Methyltetrahydrofolate calcium Calcium N5-methyltetrahydrofolate |
Celkweek, behandeling & werkzame concentratie
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| PANC-1 | Function Assay | 84 μM | 24 h | enhances EGFR, HER3 and AKT phosphorylation 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 phosphorylated levels, and the protein levels | 22977607 | |
| BXPC-3 | Function Assay | 39.86 μM | 24 h | enhances EGFR phosphorylated levels, and the protein levels | 22977607 | |
| 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 | |
| PANC-1 | Growth Inhibition Assay | IC50=83.76±0.19 μM | 22977607 | |||
| BXPC-3 | Growth Inhibition Assay | IC50=39.86±1.68 μM | 22977607 | |||
| Jurkat | Growth Inhibition Assay | 48 h | proportion of live cells=76.7±4.3 % | 23840376 | ||
| DM-3 | Growth Inhibition Assay | 48 h | proportion of live cells=101.3±2.8 % | 23840376 | ||
| JL-1 | Growth Inhibition Assay | 48 h | proportion of live cells=98.2±2.2 % | 23840376 | ||
| ZL-34 | Growth Inhibition Assay | 48 h | proportion of live cells=95.7±6.5 % | 23840376 | ||
| STAV-FCS | Growth Inhibition Assay | 48 h | proportion of live cells=88.1±8.9 % | 23840376 | ||
| M-14-K | Growth Inhibition Assay | 48 h | proportion of live cells=81.8±12.9 % | 23840376 | ||
| STAV-AB | Growth Inhibition Assay | 48 h | proportion of live cells=64.4±21.8 % | 23840376 | ||
| LoVo | Function Assay | 0.05 μM | 72 h | DMSO | increases the percentage of cells in the S phase | 23959460 |
| HT-29 | Function Assay | 0.05 μM | 72 h | DMSO | increases the percentage of cells in the S phase | 23959460 |
| WiDr | Growth Inhibition Assay | 72 h | DMSO | IC50=0.019 ± 0.002 μM | 23959460 | |
| SW1116 | Growth Inhibition Assay | 72 h | DMSO | IC50=1.70 ± 0.03 μM | 23959460 | |
| HCT116 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.049 ± 0.013 μM | 23959460 | |
| SW620 | Growth Inhibition Assay | 72 h | DMSO | IC50=1.09 ± 0.01 μM | 23959460 | |
| LoVo | Growth Inhibition Assay | 72 h | DMSO | IC50=0.032 ± 0.002 μM | 23959460 | |
| HT-29 | Growth Inhibition Assay | 72 h | DMSO | IC50=10.07 ± 0.94 μM | 23959460 | |
| A549/PEM-16 | Growth Inhibition Assay | 96 h | IC50=51.45 μM | 24348854 | ||
| A549/PEM-6.4 | Growth Inhibition Assay | 96 h | IC50=23.39 μM | 24348854 | ||
| A549/PEM-1.6 | Growth Inhibition Assay | 96 h | IC50=5.03 μM | 24348854 | ||
| A549 | Growth Inhibition Assay | 96 h | IC50=1.35 μM | 24348854 | ||
| MSTO-211H | Cell Viability Assay | 1-10 μg/ml | 72 h | IC50~0.04 μg/ml | 24378576 | |
| Y-meso14 | 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 | |
| H226 | Cell Viability Assay | 1-10 μg/ml | 72 h | IC50>10 μg/ml | 24378576 | |
| H1299 | Growth Inhibition Assay | IC50=1.84 μM | 24418519 | |||
| H1993 | Growth Inhibition Assay | IC50=0.17 μM | 24418519 | |||
| A549 | Function Assay | 0.1/0.3/0.5/1 μM | 24/48 h | DMSO | produces the formation of AVOs in a dose-dependent manner | 24626722 |
| A549 | Cell Viability Assay | 0.1/0.3/0.5/1 μM | 24/48 h | DMSO | inhibits cell viability dose and time dependently | 24626722 |
| MES04 | Growth Inhibition Assay | IC50＞100 μM | 24714722 | |||
| MES01 | Growth Inhibition Assay | IC50＞100 μM | 24714722 | |||
| H2452 | Growth Inhibition Assay | IC50＞100 μM | 24714722 | |||
| H2052 | Growth Inhibition Assay | IC50=0.57±0.34 μM | 24714722 | |||
| 211H | Growth Inhibition Assay | IC50=0.07±0.01 μM | 24714722 | |||
| H28 | Growth Inhibition Assay | IC50=0.07±0.02 μM | 24714722 | |||
| PC9/GR | Function Assay | 4.94 μM | 72 h | increases p-AKT levels | 24840891 | |
| PC9/GR | Function Assay | 4.94 μM | 72 h | increases p-ERK levels | 24840891 | |
| PC9/GR | Apoptosis Assay | 4.94 μM | 72 h | induces 19.54﹪ apoptosis | 24840891 | |
| PC9 | Apoptosis Assay | 16 nM | 72 h | induces 14.54﹪ apoptosis | 24840891 | |
| PC9/GR | Function Assay | 4.94 μM | 72 h | induces S-phase arrest | 24840891 | |
| PC9 | Function Assay | 16 nM | 72 h | induces S-phase arrest | 24840891 | |
| PC9/GR | Growth Inhibition Assay | 72 h | IC50=4.94±0.440 μM | 24840891 | ||
| PC9 | Growth Inhibition Assay | 72 h | IC50=16.05±1.85 nM | 24840891 | ||
| A549 | Function Assay | 0.1/0.3/1 μM | 48 h | increases the ratio of S-phase population | 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 level of phosphorylated Akt in a dose dependent manner | 24847863 | |
| 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 | 5 μM | 8 h | increases Mcl-1 ubiquitination levels | 24991768 | |
| A549 | Apoptosis Assay | 2.5 μM | 48 h | induces apoptosis | 24991768 | |
| H1792 | Function Assay | 2.5/5/10 μM | 48 h | downregulates Mcl-1 | 24991768 | |
| A549 | Function Assay | 2.5/5/10 μM | 48 h | downregulates Mcl-1 | 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 μM | 48 h | induces caspase-9, caspase-3 and poly (ADP-ribose) polymerase (PARP) cleavage | 24991768 | |
| 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 | 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 | |||
| KB | Function assay | 30 mins | IC50 = 0.03 μM | 19371039 | ||
| R2 | Function assay | Ki = 0.096 μM | 20085328 | |||
| R2 | Function assay | Ki = 1.54 μM | 20085328 | |||
| KB | Function assay | IC50 = 30 μM | 20085328 | |||
| 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 | Function assay | Ki = 0.094 μM | 22243528 | |||
| R2 | Function assay | Ki = 2.54 μM | 22243528 | |||
| 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 | Function assay | 1 uM | 24 hrs | Induction of apoptotic activity in human KB cells at 1 uM after 24 hrs | 18680275 | |
| 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 | |||
| 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 | ||
| 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 | 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 | 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 | |
| KB | Function assay | 48 hrs | Inhibition of AICARFTase in human KB cells assessed as accumulation of ZMP after 48 hrs by HPLC analysis | 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 | |
| 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 | |||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
Chemische informatie, opslag en stabiliteit
| Molecuulgewicht | 471.37 | Formule | C20H19N5Na2O6 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 150399-23-8 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | LY-231514 disodium | Smiles | C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)NC(CCC(=O)[O-])C(=O)[O-].[Na+].[Na+] | ||
Oplosbaarheid
|
In vitro |
Water : 94 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
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In vivo |
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In vivo formulatiecalculator (heldere oplossing)
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
mg/kg
g
μL
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
Werkingsmechanisme
| Targets/IC50/Ki |
TS
(Cell-free assay) 1.3 nM(Ki)
DHFR
(Cell-free assay) 7.2 nM(Ki)
GARFT
(Cell-free assay) 65 nM(Ki)
|
|---|---|
| In vitro |
Pemetrexed disodium vertoont antiproliferatieve activiteit in CCRF-CEM leukemie, GC3/C1 darmcarcinoom en HCT-8 ileocecaal carcinoomcellen met een IC50 van respectievelijk 25 nM, 34 nM en 220 nM. Een recente studie toont aan dat cisplatin plus deze verbinding in combinatie met SOCS-1-genoverdracht een antitumor effect vertoont door remming van celproliferatie, invasiviteit en inductie van apoptose in MPM-cellen geïnfecteerd met adenovirus-expressie SOCS-1-vector.
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| Kinase Assay |
Enzymassays en methoden.
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TS-activiteit wordt bepaald met behulp van een spectrofotometrische methode, waarbij de toename van de absorptie bij 340 nm wordt gemeten die het gevolg is van de vorming van het product, 7,8-dihydrofolaat. De assaybuffer bevat 50 mM N-tris[hydroxymethyl]methyl-2-aminoethaansulfonzuur, 25 mM MgC12, 6,5 mM formaldehyde, 1 mM EDTA en 75 mM 2-mercaptoethanol, pH 7,4. De concentraties deoxyuridylaatmonofosfaat, 6R-MTHF en hIS zijn respectievelijk 100 μM, 30 μM en 30 nM (1,7 milli-eenheden/mL). Bij de 6R-MTHF-concentratie worden een ongeremde reactie en zes concentraties remmer getest. Ki app-waarden worden bepaald door de gegevens aan de Morrison-vergelijking aan te passen met behulp van niet-lineaire regressieanalyse met behulp van het programma ENZFITTER. Ki-waarden worden berekend met de vergelijking: Ki app= Ki(1 + [S]/Km), waarbij [S] gelijk is aan 30 μM en Km gelijk is aan 3 μM. DHFR-activiteit wordt spectrofotometrisch bepaald door de verdwijning van de substraten NADPH en 7,8-dihydrofolaat bij 340 nm te meten. De reactie vindt plaats bij 25°C in 0,5 mL 50 mM kaliumfosfaatbuffer, die 150 mM KC1 en 10 nM 2-mercaptoethanol, pH 7,5, en 14 nM (0,34 milli-eenheden/mL) DHFR bevat. De NADPH-concentratie is 10 μM en 7,8-dihydrofolaat wordt gevarieerd op 5, 10 of 15 μM. Bij elke 7,8-dihydrofolaatconcentratie worden een ongeremde reactie en zeven concentraties remmer getest. Het ENZFITI'ER microcomputerprogramma wordt gebruikt om Ki app-waarden te verkrijgen door de gegevens aan de Morrison-vergelijking aan te passen door middel van niet-lineaire regressieanalyse. Ki app= Ki(1 + [S]/Km), waarbij [S] gelijk is aan de gebruikte concentratie van 7,8-dihydrofolaat en Km van 7,8-dihydrofolaat gelijk is aan 0,15 μM. GARFT-activiteit wordt spectrofotometrisch bepaald door de toename van de absorptie te meten die het gevolg is van de vorming van het product 5,8-dideazafolaat bij 295 nm. Het reactieoplosmiddel bevat 75 mM HEPES, 20% glycerol en 50 mM α-thioglycerol, pH 7,5, bij 25°C. De concentraties van substraten en enzym die worden gebruikt zijn 10 μM α,β-glycinamideribonucleotide, 0-10 μM 10-formyl-5,8-dideazafolinezuur en 10 nM (1,9 milli-eenheden/mL) GARFT. Ki-waarden worden berekend met behulp van het Enzyme Mechanism-programma van de Beckman DU640 spectrofotometer, dat niet-lineaire regressieanalyse gebruikt om gegevens aan de Michaelis-Menten-vergelijking voor competitieve remming aan te passen.
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| In vivo |
In het humane H460 niet-kleincellige longcarcinoom xenograft, produceert Pemetrexed disodium een duur-afhankelijke tumor groeisnelheid vertraging (TGD).
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Referenties |
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Toepassingen
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | EGFR / p-EGFR AKT / p-AKT / GSK3β / p-GSK3β Topo IIα / Topo I / γH2AX / Cleaved PARP / Survivin p-Chk1 / Chk1 / Cyclin D / Cyclin E / p-Histone H3 / Histone H3 / Cyclin B1 / p-Cdc2 / Cdc2 |
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30953548 |
| Immunofluorescence | p-AKT |
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24847863 |
| Growth inhibition assay | Cell viability |
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28719077 |
Informatie over klinische proeven
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| 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 |
Technische ondersteuning
Tel: +1-832-582-8158 Ext:3
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