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TSDHFR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

Pemetrexed disodium Chemical Structure

CAS: 150399-23-8

规格 价格 库存 购买数量
10mg 573.3 现货
50mg 1711.71 现货
200mg 4250.61 现货
1g 13677.3 现货
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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
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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TSDHFR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
TS [1]
(Cell-free assay)
DHFR [1]
(Cell-free assay)
GARFT [1]
(Cell-free assay)
1.3 nM(Ki) 7.2 nM(Ki) 65 nM(Ki)
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
批次:

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
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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