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Pemetrexed disodium

別名: LY-231514 disodium 中文名稱：培美曲塞二鈉

Pemetrexed disodium是一種新型抗葉酸和抗代謝藥物，作用于TS，DHFR和GARFT，無細(xì)胞試驗(yàn)中Ki分別為1.3 nM，7.2 nM 和65 nM。Pemetrexed 可誘導(dǎo)自噬和細(xì)胞凋亡。

Pemetrexed disodium Chemical Structure

Pemetrexed disodium Chemical Structure

CAS: 150399-23-8

規(guī)格 價格 庫存 購買數(shù)量
10mg 573.3 現(xiàn)貨
50mg 1711.71 現(xiàn)貨
200mg 4250.61 現(xiàn)貨
1g 13677.3 現(xiàn)貨
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Pemetrexed disodium相關(guān)產(chǎn)品

相關(guān)信號通路圖

DHFR Signaling Pathways

DHFR信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)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

產(chǎn)品描述 Pemetrexed disodium是一種新型抗葉酸和抗代謝藥物，作用于TS，DHFR和GARFT，無細(xì)胞試驗(yàn)中Ki分別為1.3 nM，7.2 nM 和65 nM。Pemetrexed 可誘導(dǎo)自噬和細(xì)胞凋亡。
特性 Pemetrexed 是結(jié)構(gòu)新型的抗葉酸抗代謝藥物。
靶點(diǎn)
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)
體外研究(In Vitro)
體外研究活性 Pemetrexed有效抑制胸苷酸合酶(TS)，Ki為1.3 nM, 也顯著抑制其他關(guān)鍵葉酸酶, 包括二氫葉酸還原酶(DHFR)和甘氨酰胺核苷酸轉(zhuǎn)甲酰酶(GARFT) ， Ki分別為7.2 nM和 65 nM。Pemetrexed作用于CCRF-CEM白血病, GC3/C1結(jié)腸癌, 和HCT-8 回盲腸癌細(xì)胞，具有抗增殖活性,IC50分別為25 nM, 34 nM 和220 nM。而且, 胸甘和次黃嘌呤聯(lián)用作用于以上三種細(xì)胞系，完全可逆轉(zhuǎn)LY231514引起的細(xì)胞毒性。[1] 最新研究顯示Cisplatin和Pemetrexed聯(lián)用作用于感染腺病毒表達(dá)SOCS-1載體的MPM細(xì)胞，通過抑制細(xì)胞增殖，侵入, 和 誘導(dǎo)凋亡而具有抗癌效果。[2]
激酶實(shí)驗(yàn) 酶活實(shí)驗(yàn)
使用分光光度分析法檢測340 nm處由于形成7,8-二氫葉酸產(chǎn)物而導(dǎo)致提高的吸光值，而測定胸苷酸合酶（TS）活性。實(shí)驗(yàn)buffer含50 mM N-三（羥甲基）甲基-2-氨基乙烷磺酸, 25 mM MgC12, 6.5 mM 甲醛, 1 mM EDTA, and 75 mM 2-巰基乙醇，pH 7.4。脫氧尿苷一磷酸, 6R-MTHF, 和 hIS 的濃度分別為100 μM, 30μM和 30 nM (1.7 毫單位/mL)。在 6R-MTHF 濃度時,在未受抑制反應(yīng)中加入6種濃度的抑制劑進(jìn)行反應(yīng)。通過回歸曲線分析，使用ENZFITTER程序應(yīng)用用Morrison 等式獲得Ki。通過分光光度計法檢測在340 nm處底物NADPH 和 7,8-二氫葉酸的消失，而測定DHFR活性。反應(yīng)在0.5 mL 50 mM磷酸鉀buffer 中25oC下進(jìn)行，磷酸鉀buffer含150 mM KC1 和10 nM 2-巰基乙醇,pH 7.5,和14 nM (0.34 毫單位/mL) DHFR。NADPH濃度為 10 μM，7,8-dihydrofolate濃度為5, 10,或 15 μM。 在每種7,8-dihydrofolate濃度時 ，在未受抑制反應(yīng)中加入7種濃度的抑制劑進(jìn)行反應(yīng)。通過回歸曲線分析，用ENZFITI'ER微機(jī)程序，應(yīng)用Morrison等式獲得Ki值。使用分光光度分析法檢測295 nm處由于形成5,8-二氫葉酸產(chǎn)物而導(dǎo)致提高的吸光值，而測定GARFT活性。反應(yīng)溶劑含 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-5,8二氫葉酸, 及10 nM (1.9毫單位/mL) GARFT。使用Beckman DU640 分光光度計的酶應(yīng)用程序， 通過回歸曲線分析，應(yīng)用Michaelis-Menten等式計算 Ki 值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 CCRF-CEM白血病,GC3/C1 結(jié)腸癌,HCT-8回盲腸癌細(xì)胞
濃度 0到30 μM
孵育時間 72小時
方法 繪制劑量反應(yīng)曲線測定IC50。Pemetrexed 溶于DMSO，濃度為4 mg/mL，然后用細(xì)胞培養(yǎng)基稀釋到所需指定的濃度。培養(yǎng)在完全培養(yǎng)基中的CCRF-CEM白血病細(xì)胞加到24孔板上，總體積為2.0 mL。平行孔中加入不同濃度Pemetrexed，DMSO終體積為0.5%。然后在37oC下溫育72小時。溫育末期，使用ZBI Coulter 計數(shù)器測細(xì)胞數(shù)。在300 μM AICA, 5 μM 胸甘, 100 μM 次黃嘌呤,或5 μM 胸甘和100 μM次黃嘌呤同時存在時，測定每種化合物的 IC50值。為了測粘附的腫瘤細(xì)胞,使用修正的初始MTT 比色分析法測定細(xì)胞毒性。人類腫瘤細(xì)胞接種在96孔平底組織培養(yǎng)板中，每孔含100 μL實(shí)驗(yàn)培養(yǎng)基。實(shí)驗(yàn)培養(yǎng)基為含10% FCS 的無葉酸RPMI 1640培養(yǎng)基，2 nM 葉酸或2.3 μM葉酸作為唯一葉酸來源。孔1A 作為空白對照?？谷~酸儲存液在Dulbecco's PBS中制備，濃度為1 mg/mL, 然后在PBS中連續(xù)稀釋2倍。在三個重復(fù)孔中加入10 μL每種濃度的樣品。然后在37oC下溫育72小時。MTT溶于PBS，濃度為5 mg/mL,10 μL 儲存MTF 溶液加到每孔中,然后在 37oC下再溫育2小時。然后每孔中加入100 μL DMSO。然后通過MTT甲增溶,在 Dynatech MR600讀數(shù)器上進(jìn)行讀數(shù)，檢測波長為570 nm，參考波長為630 nm。測定IC50值。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Pemetrexed 作用于人類H460非小細(xì)胞肺癌移植瘤，推遲腫瘤生長。而且, Pemetrexed 和紫杉醇聯(lián)用，更大程度推遲H460腫瘤生長，且和Vinorelbine及 Carboplatin產(chǎn)生添加反應(yīng)。[3]
動物實(shí)驗(yàn) Animal Models 皮下注射EMT-6乳腺癌,人類HCT116結(jié)腸癌,和人類H460非小細(xì)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

化學(xué)信息&溶解度

分子量 471.37 分子式

C20H19N5Na2O6
CAS號 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+]
儲存條件(自收到貨起)

體外溶解度
批次：

Water : 94 mg/mL (199.41 mM)

DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實(shí)驗(yàn)計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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