Pemetrexed disodium

别名: LY-231514 disodium 中文名称：培美曲塞二钠

目录号：S1135 Purity: 99.97%

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K_i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

规格	价格	库存
10mg	RMB 573.3	现货
50mg	RMB 1711.71	现货
200mg	RMB 4250.61	现货
1g	RMB 13677.3	现货
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400-668-6834 info@selleck.cn

客户使用Selleck的Pemetrexed disodium发表文献42篇

产品质控

批次：纯度： 99.97%

99.97

Pemetrexed disodium相关产品

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DHFR抑制剂选择性比较

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K_i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)，K_i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) ， K_i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
激酶实验	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K_i。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25^oC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K_i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 K_i 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37^oC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37^oC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 37^oC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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06010277	Recruiting	NSCLC\|Mesothelioma\|Thymoma	Amphia Hospital\|Albert Schweitzer Hospital	February 6 2023	Phase 4

参考文献
[1] Shih C, et al. Cancer Res. 1997, 57(6), 1116-1123. [2] Iwahori K, et al. Int J Cancer. 2012, doi: 10.1002/ijc.27611. [3] Teicher BA, et al. Clin Cancer Res. 2000, 6(3), 1016-1023.

参考文献

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

Water : 94 mg/mL

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
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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