Referencia número: HY-10820

Pemetrexed

Name: Pemetrexed
Brand: MedChemExpress
SKU: HY-10820
Price: 60.00 USD
Availability: InStock
Rating: 5 (43 reviews)

(Synonyms: LY231514)

43 Cited Publications

Revisión del cliente

Based on 43 publication(s) in Google Scholar

Pemetrexed (LY231514) is an antifolate, the K_i values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

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Pureza : 99.91%
No. CAS: 137281-23-3
Fòrmula: C₂₀H₂₁N₅O₆
Peso molecular:427.41

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pemetrexed Chemical Structure

No. CAS: 137281-23-3

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (43)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
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Actividad biológica

Descripciòn

IC₅₀ & Target

Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	39.4 nM Compound: PMX	Antiproliferative activity against human A2780 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human A2780 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
A549	IC₅₀	0.08 μM Compound: PMX	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25668494]
A549	IC₅₀	1.26 μM Compound: PMX	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay in presence of leucovorin Antiproliferative activity against human A549 cells after 72 hrs by MTT assay in presence of leucovorin	[PMID: 27017552]
A549	IC₅₀	3.31 μM Compound: PTX	Antiproliferative activity against human A549 cells after 24 hrs by MTT assay Antiproliferative activity against human A549 cells after 24 hrs by MTT assay	[PMID: 29807332]
A549	IC₅₀	1260 nM Compound: PMX	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
A549	IC₅₀	2.07 μM Compound: PTX	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37437348]
BEAS-2B	CC₅₀	151.16 μM Compound: PTX	Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 37437348]
Calu-1	IC₅₀	5.12 μM Compound: PTX	Antiproliferative activity against human Calu-1 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human Calu-1 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37437348]
CCRF-CEM	IC₅₀	1.6 x 10^-8 M Compound: 15	Compound was evaluated for the half-maximal inhibition against human CCRF-CEM lymphoblastic leukemic cell growth Compound was evaluated for the half-maximal inhibition against human CCRF-CEM lymphoblastic leukemic cell growth	[PMID: 1447744]
CHO	IC₅₀	13.2 nM Compound: PMX	Antitumor activity against CHO cells expressing PCFT (R2/PCFT4) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay Antitumor activity against CHO cells expressing PCFT (R2/PCFT4) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay	[PMID: 37582241]
CHO	IC₅₀	138 nM Compound: PMX	Antitumor activity against CHO cells expressing human RFC (PC43-10) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay Antitumor activity against CHO cells expressing human RFC (PC43-10) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay	[PMID: 37582241]
CHO	IC₅₀	42 nM Compound: PMX	Antitumor activity against CHO cells expressing human FR-alpha (RT16) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay Antitumor activity against CHO cells expressing human FR-alpha (RT16) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay	[PMID: 37582241]
CHO	IC₅₀	60 nM Compound: PMX	Antitumor activity against CHO cells expressing human FR-beta (D4) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay Antitumor activity against CHO cells expressing human FR-beta (D4) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay	[PMID: 37582241]
CHO	IC₅₀	894 nM Compound: PMX	Cytotoxicity against transporter-null (R2) CHO cells assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay Cytotoxicity against transporter-null (R2) CHO cells assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay	[PMID: 37582241]
HepG2	IC₅₀	1.26 μM Compound: PMX	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25668494]
HUVEC	IC₅₀	1.73 μM Compound: PMX	Cytotoxicity against HUVEC assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against HUVEC assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
IGROV-1	IC₅₀	102 nM Compound: pemetrexed	Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells	[PMID: 18680275]
IGROV-1	IC₅₀	200 nM Compound: pemetrexed	Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells in presence of folic acid Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells in presence of folic acid	[PMID: 18680275]
IGROV-1	IC₅₀	102 nM Compound: PMX, LY-231514	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
IGROV-1	IC₅₀	200 nM Compound: PMX, LY-231514	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
IGROV-1	IC₅₀	>20 μM Compound: PMX	Anticlonogenic activity against human IGROV1 cells incubated for 24 hrs followed by compound wash out and measured after 10 days by methylene blue staining-based assay Anticlonogenic activity against human IGROV1 cells incubated for 24 hrs followed by compound wash out and measured after 10 days by methylene blue staining-based assay	[PMID: 29701475]
IGROV-1	IC₅₀	104 nM Compound: PMX	Antiproliferative activity against wild type human IGROV1 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against wild type human IGROV1 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	22.2 nM Compound: PMX	Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	46.6 nM Compound: PMX	Antiproliferative activity against FRalpha knockout human IGROV1 KD4 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against FRalpha knockout human IGROV1 KD4 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	71 nM Compound: PMX	Antiproliferative activity against human IGROV1 cells harboring non targeted control shRNA sequence after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human IGROV1 cells harboring non targeted control shRNA sequence after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	71 nM Compound: 1; PMX	Antiproliferative activity against human IGROV-1 cells assessed as inhibition of cell growth incubated for 96 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human IGROV-1 cells assessed as inhibition of cell growth incubated for 96 hrs by CellTiter-Blue cell viability assay	[PMID: 38116433]
KB	IC₅₀	30 nM Compound: pemetrexed	Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine	[PMID: 18680275]
KB	IC₅₀	327 nM Compound: pemetrexed	Antiproliferative activity against human RFC and FRalpha expressing human KB cells in presence of folic acid Antiproliferative activity against human RFC and FRalpha expressing human KB cells in presence of folic acid	[PMID: 18680275]
KB	IC₅₀	68 nM Compound: pemetrexed	Antiproliferative activity against human RFC and FRalpha expressing human KB cells Antiproliferative activity against human RFC and FRalpha expressing human KB cells	[PMID: 18680275]
KB	IC₅₀	30 nM Compound: PMX	Inhibition of GARFTase in human KB cells assessed as inhibition of incorporation of [14C]glycine into [14C]formyl GAR after 30 mins in presence of azaserine Inhibition of GARFTase in human KB cells assessed as inhibition of incorporation of [14C]glycine into [14C]formyl GAR after 30 mins in presence of azaserine	[PMID: 19371039]
KB	IC₅₀	30 μM Compound: PMX	Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay	[PMID: 20085328]
KB	IC₅₀	327 nM Compound: PMX, LY-231514	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
KB	IC₅₀	68 nM Compound: PMX, LY-231514	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
KB	IC₅₀	327 nM Compound: PMX, pemetrexed	Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid	[PMID: 24111942]
KB	IC₅₀	68 nM Compound: PMX, pemetrexed	Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
KB	IC₅₀	11.74 nM Compound: 6, Pemetrexed, PMX, Alimta	Inhibition of GARFTase in human KB cells assessed as incorporation of [14C]-glycine into [14C]-formyl GAR incubated 30 mins prior to [14C]-glycine addition measured after 16 hrs by radiometric assay in presence of azaserin Inhibition of GARFTase in human KB cells assessed as incorporation of [14C]-glycine into [14C]-formyl GAR incubated 30 mins prior to [14C]-glycine addition measured after 16 hrs by radiometric assay in presence of azaserin	[PMID: 24256410]
KB	IC₅₀	690 nM Compound: 6, Pemetrexed, PMX, Alimta	Cytotoxicity against human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTitre-Blue fluorescence assay in presence of folic acid Cytotoxicity against human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTitre-Blue fluorescence assay in presence of folic acid	[PMID: 24256410]
KB	IC₅₀	9.94 nM Compound: 6, Pemetrexed, PMX, Alimta	Cytotoxicity against human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTitre-Blue fluorescence assay Cytotoxicity against human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTitre-Blue fluorescence assay	[PMID: 24256410]
KB	IC₅₀	327 nM Compound: PMX	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	68 nM Compound: PMX	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	11.74 nM Compound: PMX, LY231514	Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as incorporation of [U-14C]-glycine into [14C]-formyl glycinamide ribonucleotide incubated for 1 hr followed by [U-14C]-glycine addition measured after 16 hrs Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as incorporation of [U-14C]-glycine into [14C]-formyl glycinamide ribonucleotide incubated for 1 hr followed by [U-14C]-glycine addition measured after 16 hrs	[PMID: 25602637]
KB	IC₅₀	68 nM Compound: PMX, LY231514	Antiproliferative activity against human KB cells expressing RFC/FRalpha/PCFT after 96 hrs by CellTiter-Blue assay Antiproliferative activity against human KB cells expressing RFC/FRalpha/PCFT after 96 hrs by CellTiter-Blue assay	[PMID: 25602637]
KB	IC₅₀	0.07 μM Compound: PMX	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25668494]
KB	IC₅₀	0.07 μM Compound: PMX	Antiproliferative activity against human KB cells after 72 hrs by MTT assay in presence of leucovorin Antiproliferative activity against human KB cells after 72 hrs by MTT assay in presence of leucovorin	[PMID: 27017552]
KB	IC₅₀	327 nM Compound: PMX	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	68 nM Compound: PMX	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	70.2 nM Compound: PMX	Antiproliferative activity against human KB cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human KB cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]
KB	IC₅₀	327 nM Compound: PMX	Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 32503687]
KB	IC₅₀	68 nM Compound: PMX	Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of DHFR in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
KB	IC₅₀	68 nM Compound: PMX	Antitumor activity against human KB cells expressing RFC transporter coexpressing FR-alpha and PCFT transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay Antitumor activity against human KB cells expressing RFC transporter coexpressing FR-alpha and PCFT transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay	[PMID: 37582241]
KB	IC₅₀	9.95 nM Compound: 1; PMX	Antiproliferative activity against human KB cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KB cells assessed as cell growth inhibition incubated for 96 hrs by CellTiter-Blue cell viability assay	[PMID: 38116433]
L1210	IC₅₀	2.2 x 10^-8 M Compound: 15	Compound was evaluated for the half-maximal inhibition against mouse L1210 leukemic cell growth Compound was evaluated for the half-maximal inhibition against mouse L1210 leukemic cell growth	[PMID: 1447744]
MCF7	IC₅₀	0.65 μM Compound: PMX	Antiproliferative activity against human MCF7 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay Antiproliferative activity against human MCF7 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay	[PMID: 28830032]
MDA-MB-231	IC₅₀	3.85 μM Compound: PTX	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 29807332]
NCI-H1975	IC₅₀	2.13 μM Compound: PTX	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37437348]
OVCAR-3	IC₅₀	6.9 μM Compound: PTX	Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay	[PMID: 29807332]
R2	IC₅₀	894 nM Compound: pemetrexed	Antiproliferative activity against human RFC expressing Chinese hamster R2 cells Antiproliferative activity against human RFC expressing Chinese hamster R2 cells	[PMID: 18680275]
R2	IC₅₀	13.2 nM Compound: PMX, LY-231514	Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	4.94 nM Compound: PMX, LY-231514	Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days	[PMID: 21879757]
R2	IC₅₀	894 nM Compound: PMX, LY-231514	Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	13.2 nM Compound: PMX, pemetrexed	Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
R2	IC₅₀	22.3 nM Compound: 6, Pemetrexed, PMX, Alimta	Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay	[PMID: 24256410]
R2	IC₅₀	>1000 nM Compound: 6, Pemetrexed, PMX, Alimta	Cytotoxicity against chinese hamster R2 cells after 96 hrs by CellTitre-Blue fluorescence assay Cytotoxicity against chinese hamster R2 cells after 96 hrs by CellTitre-Blue fluorescence assay	[PMID: 24256410]
R2	IC₅₀	894 nM Compound: PMX	Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	974 nM Compound: PMX	Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	42 nM Compound: PMX, LY231514	Cytotoxicity against RFC-deficient Chinese hamster R2 cells assessed as growth inhibition after 96 hrs by CellTiter-Blue assay Cytotoxicity against RFC-deficient Chinese hamster R2 cells assessed as growth inhibition after 96 hrs by CellTiter-Blue assay	[PMID: 25602637]
R2	IC₅₀	42 nM Compound: PMX	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis	[PMID: 27458733]
R2	IC₅₀	849 nM Compound: PMX	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
R2	IC₅₀	138 nM Compound: PMX	Antiproliferative activity in Chinese hamster R2 cells deficient in RFC, PCFT, and FRalpha assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Antiproliferative activity in Chinese hamster R2 cells deficient in RFC, PCFT, and FRalpha assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
R2	IC₅₀	13.2 nM Compound: PMX	Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
R2	IC₅₀	894 nM Compound: PMX	Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4/FRalpha-null R2 cells assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4/FRalpha-null R2 cells assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
SGC-7901	IC₅₀	9.08 μM Compound: PTX	Antiproliferative activity against human SGC7901 cells after 24 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 24 hrs by MTT assay	[PMID: 29807332]
SW-620	IC₅₀	0.08 μM Compound: PMX	Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay in presence of leucovorin Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay in presence of leucovorin	[PMID: 27017552]
SW-620	IC₅₀	0.09 μM Compound: PMX	Antiproliferative activity against human SW620 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay Antiproliferative activity against human SW620 cells in folate free medium after 72 hrs in presence of leucovorin by MTT assay	[PMID: 28830032]
SW-620	IC₅₀	80.2 nM Compound: PMX	Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31200235]

In Vitro

Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (K_m=1.6 μM and V_max/K_m=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (K_i=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (K_i=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 137281-23-3
Appearance Solid
Peso molecular 427.41
Fòrmula C₂₀H₂₁N₅O₆
Color White to off-white
SMILES

O=C1NC(N)=NC2=C1C(CCC3=CC=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)C=C3)=CN2
Synonyms

LY231514
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (43)

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Mol Cancer

Organoids derived from patients provide a new opportunity for research and individualized treatment of malignant peritoneal mesothelioma. [Abstract]

2024 Jan 10;23(1):12. PMID: 38200517
Nat Commun

2026 Oct 1.
Mol Cell

Metabolic Diversity in Human Non-Small Cell Lung Cancer Cells. [Abstract]

2019 Dec 5;76(5):838-851.e5. PMID: 31564558

Pemetrexed purchased from MedChemExpress. Usage Cited in: Mol Cell. 2019 Dec 5;76(5):838-851.e5. [Abstract]

The relationship between SerG6m3 and Pemetrexed disodium (0.01-1.0 μM; 3 d) IC₅₀.
Theranostics

The deubiquitinating enzyme UCHL1 promotes resistance to pemetrexed in non-small cell lung cancer by upregulating thymidylate synthase. [Abstract]

2020 May 15;10(13):6048-6060. PMID: 32483437

Pemetrexed purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060. [Abstract]

Western blot analysis of UCHL1 levels in PEM-R cells and their parental cells. The mRNA and protein levels of UCHL1 in the PEM-R cells are significantly increased, relative to in the parental cells.

Pemetrexed purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 15;10(13):6048-6060. [Abstract]

Immunofluorescence assay showing the expression and intracellular location of UCHL1 in NSCLC cells. Increased UCHL1 levels are observed in both the cytoplasm and the nucleus of the PEM-R cells.
J Exp Clin Cancer Res

FL496, an FL118-derived small molecule, induces growth inhibition, senescence, and apoptosis of malignant pleural mesothelioma (MPM) cells, and exhibits anti-MPM tumor efficacy strikingly superior to the pemetrexed-cisplatin combination. [Abstract]

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Deep Learning-Powered Scalable Cancer Organ Chip for Cancer Precision Medicine. [Abstract]

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J Control Release

Effective combination of liposome-targeted chemotherapy and PD-L1 blockade of murine colon cancer. [Abstract]

2023 Jan:353:490-506. PMID: 36460179

Pemetrexed purchased from MedChemExpress. Usage Cited in: J Control Release. 2023 Jan:353:490-506. [Abstract]

Cell viability of MC38 and CT26 cells after incubation with DTX, PMX, DTX+PMX, DTX-LPs,PMX-LPs, and DTX/PMX-LPs for 48 and 72 hours (n = 4, equivalent PMX (Pemetrexed) concentration is 0.048, 0.16, 1.2, 6, 30 µg/ml).

Pemetrexed purchased from MedChemExpress. Usage Cited in: J Control Release. 2023 Jan:353:490-506. [Abstract]

The apoptotic rate after treatment with different Pemetrexed (1.37 μg/mL; 24 h) of drugs and formulations
Pharmacol Res

Time-dependent proteomics and drug response in expanding cancer cells. [Abstract]

2024 Jun:204:107208. PMID: 38729587
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Increasing the tumour targeting of antitumour drugs through anlotinib-mediated modulation of the extracellular matrix and the RhoA/ROCK signalling pathway. [Abstract]

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Cell Death Discov

Targeting mitochondrial one-carbon enzyme MTHFD2 together with pemetrexed confers therapeutic advantages in lung adenocarcinoma. [Abstract]

2022 Jul 5;8(1):307. PMID: 35790743

Pemetrexed purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Jul 5;8(1):307. [Abstract]

The IC50 value of pemetrexed ( 0.039 to 50 μM, 5 days) in A549 cells.

Pemetrexed purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Jul 5;8(1):307. [Abstract]

A549 and H1299 cells were treated with pemetrexed (5 μM), DS18561882 (10 μM), or combination for 5 days. Cell proliferative abilities were detected by MTT assay.
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

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Bio-inspired self-assembly of omega-3 fatty acids and peptides for responsive drug delivery. [Abstract]

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SETDB1 tumour suppressor roles in near-haploid mesothelioma involve TP53. [Abstract]

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RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

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Virol Sin

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Pemetrexed purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Cell proliferation and viability of ACC-2 cell lines treated with Pemetrexed disodium (0.01-2 μg/mL; 48 h) were measured by the Cell Counting Kit-8 (CCK-8).

Pemetrexed purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Pemetrexed disodium (0.5 μg/mL; 48 h) caused significant cytotoxicity effects on ACC-2 cells.

Pemetrexed purchased from MedChemExpress. Usage Cited in: Odontology. 2020 Apr;108(2):300-311. [Abstract]

Pemetrexed disodium (0.5 μg/mL; 12 h) increased early stage apoptotic and total apoptotic cells in ACC-2 cells.

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Pemetrexed disodium (0.5 μg/mL; 24 h) decreased RNAP II levels in ACC-2 cells.
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Research Square Print

September 27th, 2022.
University of Texas

2015.

Solvente y solubilidad

In Vitro:

DMSO : 250 mg/mL (584.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3397 mL

11.6984 mL

23.3967 mL

5 mM

0.4679 mL

2.3397 mL

4.6793 mL

10 mM

0.2340 mL

1.1698 mL

2.3397 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 20 mg/mL (46.79 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 20% SBE-β-CD in Saline

Solubility: 5 mg/mL (11.70 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (560 KB)
- English - EN (560 KB)
- Français - FR (560 KB)
- Deutsch - DE (560 KB)
- Norwegian - NO (560 KB)
- Español - ES (560 KB)
- Swedish - SV (560 KB)
- Italian - IT (560 KB)
- Korean - KR (560 KB)
- Portuguese - PT (560 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23. [Content Brief]

[2]. Anraku M, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignantmesothelioma. J Immunol. 2010 Jul 15;185(2):956-66. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3397 mL	11.6984 mL	23.3967 mL	58.4918 mL
	5 mM	0.4679 mL	2.3397 mL	4.6793 mL	11.6984 mL
	10 mM	0.2340 mL	1.1698 mL	2.3397 mL	5.8492 mL
	15 mM	0.1560 mL	0.7799 mL	1.5598 mL	3.8995 mL
	20 mM	0.1170 mL	0.5849 mL	1.1698 mL	2.9246 mL
	25 mM	0.0936 mL	0.4679 mL	0.9359 mL	2.3397 mL
	30 mM	0.0780 mL	0.3899 mL	0.7799 mL	1.9497 mL
	40 mM	0.0585 mL	0.2925 mL	0.5849 mL	1.4623 mL
	50 mM	0.0468 mL	0.2340 mL	0.4679 mL	1.1698 mL
	60 mM	0.0390 mL	0.1950 mL	0.3899 mL	0.9749 mL
	80 mM	0.0292 mL	0.1462 mL	0.2925 mL	0.7311 mL
	100 mM	0.0234 mL	0.1170 mL	0.2340 mL	0.5849 mL

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Pemetrexed

43 Cited Publications

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