Pemetrexed

Catalog No.S1135 Synonyms: LY-231514

Pemetrexed  Chemical Structure

Molecular Weight(MW): 471.37

Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively.

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Cited by 8 Publications

3 Customer Reviews

  • Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.

    Cancer Res 2014 74(21), 5948-54. Pemetrexed purchased from Selleck.

    Cell viability of U2OS cells after indicated pemetrexed in different concentrations or plus C6 ceramide (C6, 5 ug/ml) treatment was tested by MTT assay.

    Biochem Biophys Res Commun 2014 452(1), 72-8. Pemetrexed purchased from Selleck.

  • A549 cells were treated with pemetrexed and/or MK1775 for 72 hours and counted by flow cytometry and the number of live cells relative to untreated is depicted.

    Mol Cancer Ther 2013 12, 2675-84. Pemetrexed purchased from Selleck.

Purity & Quality Control

Choose Selective DHFR Inhibitors

Biological Activity

Description Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively.
Targets
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)
In vitro

Pemetrexed disodium shows the antiproliferative activity in CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells with IC50 of 25 nM, 34 nM and 220 nM, respectively. [1] A recent study shows that cisplatin plus Pemetrexed combined with SOCS-1 gene delivery shows the antitumor effect by inhibition of cell proliferation, invasiveness, and induction of apoptosis in MPM cells infected with adenovirus-expressing SOCS-1 vector. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MSTO-211H NELud4JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVWxJO69VQ>? NWTtU3AzPDhiaB?= M3LRbIVvcGGwY3XzJJNqdX[jc4TheIlvKGmwaHnibZRm\CC4aXHibYxqfHl? NVHIXHBiOjZ|M{SzNlA>
A549 MlXJR4VtdCCYaXHibYxqfHliQYPzZZk> NULoSHFUOSEQvF2= Ml;0OFghcA>? Mn3H[Y5p[W6lZYOgd4lufmG|dHH0bY4hcW6qaXLpeIVlKH[rYXLpcIl1gQ>? MYKyOlM{PDN{MB?=
MSTO-211H M{TRW2Z2dmO2aX;uJGF{e2G7 MWGxJO69VQ>? MljNNlQhcA>? MoTI[Y5p[W6lZYOgZZV1d3CqYXf5JINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NY\6V25YOjZ|M{SzNlA>
A549 M{Dm[mZ2dmO2aX;uJGF{e2G7 M3:welEh|ryP MVuyOEBp NG\weWNmdmijbnPld{BifXSxcHjh[5kh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> MlnxNlY{OzR|MkC=
MSTO-211H NHXQNnRCeG:ydH;zbZMhSXO|YYm= Mn7wNUDPxE1? MkDrNlQhcA>? NVfsUWh1cW6mdXPld{BieG:ydH;zbZMh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> Mn\xNlY{OzR|MkC=
A549 MnLSRZBweHSxc3nzJGF{e2G7 MoLnNUDPxE1? M4HTNlI1KGh? MmHYbY5lfWOnczDhdI9xfG:|aYOgZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= MVqyOlM{PDN{MB?=
MSTO-211H NGHvVZJHfW6ldHnvckBCe3OjeR?= NYTXTWlPOSEQvF2= NIrRfFk1QCCq MkX6bY5kemWjc3XzJGFOWEticHjvd5Bpd3K7bHH0bY9vKGGwZDDhJINwdmOxbXn0ZY51KGSnY4LlZZNmKGmwIFHLWEBidmRibWTPVkBxcG:|cHjvdplt[XSrb36gZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= NV;0SI9HOjZ|M{SzNlA>
A549 MoPYSpVv[3Srb36gRZN{[Xl? MmO0NUDPxE1? NYXSZ4FTPDhiaB?= NEfDOINqdmO{ZXHz[ZMhSU2SSzDwbI9{eGixconsZZRqd25iYX7kJIEh[2:wY3;tbZRidnRiZHXjdoVie2ViaX6gRWtVKGGwZDDtWG9TKHCqb4PwbI9zgWyjdHnvckBkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> M1HOZ|I3OzN2M{Kw
Vero M{S3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMlI{PMLibV2= M2niTFI1KGh? MYTndo94fGhiaX7obYJqfGmxbk2189mr MnTSNlU6PzV4M{e=
A549 M2PNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnnVGtZOC5{M{VCpI1O MVqyOEBp NE\ZOJNoem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= NX;TSGlvOjV7N{W2N|c>
HeLa MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjtRpcxNjJ|NNMgcW0> NE\kZ5QzPCCq MWTndo94fGhiaX7obYJqfGmxbk2189mr NXqxbZo6OjV7N{W2N|c>
T47D MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHpNE4zOzUEoH3N Ml63NlQhcA>? M2XBUYdzd3e2aDDpcohq[mm2aX;uQVEx97ns NGjSdHgzPTl5NU[zOy=>
Vero M4ftSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIKxZokxNjJ|NNMgcW0> NIT6UXg1QCCq MknE[5Jwf3SqIHnubIljcXSrb369NVDwwap? M1jmTVI2QTd3NkO3
A549 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuwMlI{PMLibV2= NYf6[ohOPDhiaB?= Ml3B[5Jwf3SqIHnubIljcXSrb369N|Dwwap? M4DzTVI2QTd3NkO3
HeLa NV3US29xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGwMlI{PMLibV2= Ml\GOFghcA>? NF;FU5loem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= MX2yOVk4PTZ|Nx?=
T47D MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLqZYwxNjJ|NNMgcW0> M1TBRVQ5KGh? MWXndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? Ml\GNlU6PzV4M{e=
Vero NGfyeZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjzcZcxNjJ|NNMgcW0> MVm3NkBp MWLndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? MV[yOVk4PTZ|Nx?=
A549 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLhWZRGOC5{M{VCpI1O MlK4O|IhcA>? MlzM[5Jwf3SqIHnubIljcXSrb369OVDwwap? M17LPVI2QTd3NkO3
HeLa MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlI{PMLibV2= NGXETmU4OiCq NUPUTIVP\3Kxd4ToJIlvcGmkaYTpc44:OjExubq= NECzR40zPTl5NU[zOy=>
T47D NYDZWoVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDYNE4zOzUEoH3N MV23NkBp MW\ndo94fGhiaX7obYJqfGmxbk2zNQ+6sg>? MXeyOVk4PTZ|Nx?=
A459 NYLkZ|ExTnWwY4Tpc44hSXO|YYm= NVzyRoV6OS9{L{Sg{txO M2rk[lI1NzR6IHi= MkDLbY5lfWOnczDHNUBxcGG|ZTDhdpJme3RiaX6g[I9{\S1iYX7kJJRqdWViZHXw[Y5l\W62IH3hco5meg>? MWqyOVc1Ozh{Mh?=
A459 MUjGeY5kfGmxbjDBd5NigQ>? M{XUWFEwOi92IN88US=> MXe0PEBp NVnpSnV1\GWlcnXhd4V{KHSqZTDs[ZZmdHNib3[gdE1Cc3R? MUSyOVc1Ozh{Mh?=
A459 NX7hS2NtSXCxcITvd4l{KEG|c3H5 M3;iN|TPxE1? M3XmWFQ5KGh? NWHuSIpKcW6mdXPld{BieG:ydH;zbZM> MX:yOVc1Ozh{Mh?=
HepG2 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn;INE4y6oDVMUCwxsDPxE1? MofXO|IhcA>? MUDobYdpKGOxbnPlcpRz[XSrb37zJI9nKHCnbXX0doV5\WRiYYSgLFExNzFyMNMg{txOMSCxbnz5JJNtcWeqdHz5JIlvcGmkaYTzJGhmeEd{IHPlcIwhe3W{dnn2ZYw> M4fyW|I2PDR4MUCy
HepG2 MUTBdI9xfG:|aYOgRZN{[Xl? NI[wd2cxNjIkgKOxNFDDqM7:TR?= M4LmblczKGh? NYfqR45UcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJkh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= NGjtXVczPTR2NkGwNi=>
HepG3 NUnIVm5HTnWwY4Tpc44hSXO|YYm= NIi4T44xNjIkgKOxNFDDqM7:TR?= MmjLOFghcA>? NYfqWo5HcW6mdXPld{BxPjJiZH;3cpJm\3WuYYTpc44h[XNid3XscEBieyCEZXPsbY4uOSCjbnSgUGM{Si2LSTD1dJJm\3WuYYTpc44> MXuyOVQ1PjFyMh?=
HepG3 M4HaO2Z2dmO2aX;uJGF{e2G7 M{fHWVAvOeLCk{GwNOKh|ryP NFeyUFY1QCCq NHrX[GRi[3SrdnH0[ZMh[3m2bz3wdo91\WO2aY\lJIF2fG:yaHHnfeKh MVmyOVQ1PjFyMh?=
HepG3 NF7SZXZHfW6ldHnvckBCe3OjeR?= NWq0bo1QOTEEoN88US=> NVjHUY5kPDhiaB?= NVfTeHRJfXC{ZXf1cIF1\XNicHjvd5Bpd3K7bHH0[YQhMHBvKTDNSWsyNzJiKGPldlIyPy9{MkGpJIFv\CCyLVXST|EwOiBqVHjyNlAzN1S7ckKwOEk> Mn\ONlU1PDZzMEK=
U20S MoqyR4VtdCCYaXHibYxqfHliQYPzZZk> MmfGNE4xOS1zMECg{txO NWDrN25PPzJiaB?= NEjJNlNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5Nm\GWyZX7k[Y51dHl? M17xWlI2OTV{M{m5
MG-63 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Moq0NE4xOS1zMECg{txO MlSwO|IhcA>? MoPSbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[YRmeGWwZHXueIx6 M17mfVI2OTV{M{m5
A549 MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIPCXlQyNTFyMECgcm0> NYH1eVBZPzJiaB?= NFmyN2pKSzVyPUGzO{BvVQ>? NGPuOVYzPTF2NU[2PS=>
H1299 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mm\nNU0yODByIH7N NGr6ZYk4OiCq M17NOWlEPTB;MUe4JI5O M2Ttc|I2OTR3Nk[5
MSTO-211 NGrJflJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NI\FU5oyKM7:TR?= M3ezcVQ5KGh? MV\wdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv M1T1S|I2ODl4OUmz
A549 MnrQR4VtdCCYaXHibYxqfHliQYPzZZk> MYOxJO69VQ>? M33i[|Q5KGh? NUfJUZJMeHKxZIXj[ZMh[SC|eX7ldodqe3SrYzDpcohq[mm2b4L5JIVn\mWldDDvckB1cGViY3XscEBoem:5dHigZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= NWfPOIdoOjVyOU[5PVM>
MSTO-211 MYnBdI9xfG:|aYOgRZN{[Xl? NFHpb2IyKM7:TR?= NGXITIo1QCCq NF3KSmhmdmijbnPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> NETEOGMzPTB7Nkm5Ny=>
A549 MoHmRZBweHSxc3nzJGF{e2G7 M33YU|Eh|ryP NFPwbpQ1QCCq NFzEO2xmdmijbnPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> NYDqfphJOjVyOU[5PVM>
MSTO-211 NIGwRXBHfW6ldHnvckBCe3OjeR?= NVHEOWx[OSEQvF2= Ml3OOFghcA>? NXrwPJlT\W6qYX7j[ZMhcW62cnHj[YxtfWyjcjDSU3MheHKxZIXjeIlwdiClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv NXrVPZlsOjVyOU[5PVM>
A549 MmXRSpVv[3Srb36gRZN{[Xl? NUHpOGVYOSEQvF2= M3nyc|Q5KGh? NIj2NWVmdmijbnPld{BqdnS{YXPlcIx2dGG{IGLPV{Bxem:mdXP0bY9vKGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MkTkNlUxQTZ7OUO=
MSTO-211 NVjtSoRVTnWwY4Tpc44hSXO|YYm= MnrzNUDPxE1? M3HFeVQ5KGh? MYXs[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? NHjRNnkzPTB7Nkm5Ny=>
A549 MYLGeY5kfGmxbjDBd5NigQ>? Mn7SNUDPxE1? M2DHSFQ5KGh? NHPEV5lt\WGmczD0c{BucXSxY3jvcoRzcWGuIHT5d4Z2dmO2aX;uJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= MYSyOVA6Pjl7Mx?=
A549  NVzlR4tRTnWwY4Tpc44hSXO|YYm= M1nlO|IvPS93L{GwJO69VQ>? MlTnOFghcA>? MmTXbY5kemWjc3XzJG5wgGFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NXruRpppOjR7OUG3Olg>
H1792 M{LyW2Z2dmO2aX;uJGF{e2G7 MnjYNk42NzVxMUCg{txO M{jDSlQ5KGh? M2r4N4lv[3KnYYPld{BPd3ijIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? M3fBW|I1QTlzN{[4
A549  NXfTT45CTnWwY4Tpc44hSXO|YYm= NVj2[FhzOi53IN88US=> MlqzOFghcA>? M2fQeolv\HWlZYOgZ4F{eGG|ZT25MEBk[XOyYYPlMVMh[W6mIIDvcJkhMEGGUD3ybYJwe2VrIIDvcJlu\XKjc3WgLHBCWlBrIHPs[YF3[Wen M2juflI1QTlzN{[4
H1792 MVnGeY5kfGmxbjDBd5NigQ>? MXSyMlUh|ryP Mn;FOFghcA>? MVHpcoR2[2W|IHPhd5Bie2VvOTygZ4F{eGG|ZT2zJIFv\CCyb3z5JEhCTFBvcnnic5NmMSCyb3z5cYVz[XOnIDjQRXJRMSClbHXheoFo\Q>? NF7ObZQzPDl7MUe2PC=>
A549  NECyS|ZHfW6ldHnvckBCe3OjeR?= MWWyMlUwPS9zMDFOwG0> M3iy[FQ5KGh? MX3kc5dvemWpdXzheIV{KE2lbD2xxsA> NUfUT3J{OjR7OUG3Olg>
H1792 NYPKdIdSTnWwY4Tpc44hSXO|YYm= Mn;VNk42NzVxMUCg{txO MYC0PEBp M1n6VYRwf26{ZXf1cIF1\XNiTXPsMVHDqA>? NEL1ZpgzPDl7MUe2PC=>
A549 MojIRZBweHSxc3nzJGF{e2G7 Mn\lNk42KM7:TR?= M{HrOVQ5KGh? MlzybY5lfWOnczDhdI9xfG:|aYO= NFWwenIzPDl7MUe2PC=>
A549 NWKwPHFGTnWwY4Tpc44hSXO|YYm= NEnQbog2KM7:TR?= NW\GN2MyQCCq M122bIlv[3KnYYPld{BO[2xvMTD1ZolyfWm2aX7heIlwdiCuZY\lcJM> M{TwTVI1QTlzN{[4
A549 MVTGeY5kfGmxbjDBd5NigQ>? MU[xJOK2VQ>? MonvOE85NzF{L{K0M|Q5KGh? MlvsbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyaH;zdIhwenmuYYTl[EBCc3RiaX6gZUB1cW2nIHTldIVv\GWwdDDtZY5v\XJ? NFjmcXMzPDh2N{i2Ny=>
A549 MknzSpVv[3Srb36gRZN{[Xl? MXywMlEwOC5|L{Gg{txO MljNOFghcA>? NE\MN49qdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIDoc5NxcG:{eXzheIVlKEGtdDDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M3rHZVI1QDR5OE[z
A549 Mk[5RZBweHSxc3nzJGF{e2G7 NWOzO3F{OC5zL{CuN{8yKM7:TR?= M1PzXFQ5KGh? MV3pcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M3;We|I1QDR5OE[z
A549 M1Ph[mZ2dmO2aX;uJGF{e2G7 MnTJNE4yNzBwMz:xJO69VQ>? MYC0PEBp MmfmbY5kemWjc3XzJJRp\SC{YYTpc{Bw\iCVLYDoZZNmKHCxcIXsZZRqd25? MW[yOFg1Pzh4Mx?=
PC9 Mn\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1roNlczKGh? M3;vTmlEPTB;MU[uNFXDuTFwOEWgcm0> M{nibVI1QDRyOEmx
PC9/GR NHH2ZWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP3e2xGPzJiaB?= M3P6SGlEPTB;ND65OOKyOC52NECg{txO MYWyOFg1ODh7MR?=
PC9 NXexTId6TnWwY4Tpc44hSXO|YYm= MoX3NVYhdk1? M4jRWFczKGh? NWSwXGxLcW6mdXPld{BUNXCqYYPlJIFzemW|dB?= NYmydHZnOjR6NEC4PVE>
PC9/GR NIjS[nlHfW6ldHnvckBCe3OjeR?= MWS0Mlk1KM7:TR?= M4nSVlczKGh? MYPpcoR2[2W|IGOtdIhie2ViYYLy[ZN1 NVX5bWx7OjR6NEC4PVE>
PC9 NXLodol4SXCxcITvd4l{KEG|c3H5 MVmxOkBvVQ>? NF;yVoo4OiCq NVLJNotRcW6mdXPld{AyPC53NP-5rkBieG:ydH;zbZM> MmX5NlQ5PDB6OUG=
PC9/GR NHPWWWFCeG:ydH;zbZMhSXO|YYm= NXXpNohYPC57NDFOwG0> NWnIS3JZPzJiaB?= M1XKU4lv\HWlZYOgNVkvPTUxubqgZZBweHSxc3nz NGTicoszPDh2MEi5NS=>
PC9/GR MmTXSpVv[3Srb36gRZN{[Xl? MmeyOE46PCEQvF2= MoTrO|IhcA>? MlHTbY5kemWjc3XzJJAuTVKNIHzleoVtew>? M1vTZVI1QDRyOEmx
PC9/GR NH60NohHfW6ldHnvckBCe3OjeR?= M2nEPFQvQTRizszN NXjS[IxlPzJiaB?= NWXqVVVmcW6lcnXhd4V{KHBvQVvUJIxmfmWucx?= MWOyOFg1ODh7MR?=
H28 M3[5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\TdmRYUUN3ME2wMlA4yrFyLkCyJO69VQ>? NUTuNlFkOjR5MUS3NlI>
211H M3:5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4OwbGlEPTB;MD6wO:KyOC5yMTFOwG0> M17rd|I1PzF2N{Ky
H2052 NFnudZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LVc2lEPTB;MD61O:KyOC5|NDFOwG0> M3\jU|I1PzF2N{Ky
H2452 NI\ycnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPBTWM2OO,:nkGwNEDPxE1? NV7ZT2xTOjR5MUS3NlI>
MES01 NWPzR4Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H1RmlEPTExvK6xNFAh|ryP MkfDNlQ4OTR5MkK=
MES04 NVLGSpNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|Ux97zgMUCwJO69VQ>? NXHWOVE{OjR5MUS3NlI>
A549 NH7W[pZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3HIblAvOS9yLkOvNE42NzFizszN NHXleGIzPC92ODDo NVfnSXVTTE2VTx?= MofqbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NEXrPGczPDZ{NkeyNi=>
A549 M335ZWZ2dmO2aX;uJGF{e2G7 MkLxNE4yNzBwMz:wMlUwOSEQvF2= M4rYSVI1NzR6IHi= NGXueplFVVOR NGrMWIpxem:mdXPld{B1cGViZn;ycYF1cW:wIH;mJGFXV3NiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYKyOFYzPjd{Mh?=
H1993 NGf4ZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vybmlEPTB;MD6xO{DPxE1? MoPZNlQ1OTh3MUm=
H1299 MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXNbZN{UUN3ME2xMlg1KM7:TR?= NUDaNGJbOjR2MUi1NVk>
H226 NYLzZ2dIS2WubDDWbYFjcWyrdImgRZN{[Xl? M4\OTVEuOTBizsznM41t MU[3NkBp NGjKOldKSzVyPkGwJO69\y:vbB?= Mn\ENlQ{Pzh3N{[=
H290 MlXrR4VtdCCYaXHibYxqfHliQYPzZZk> M{eyc|EuOTBizsznM41t Mm\IO|IhcA>? M3LkeGlEPTB-MUCg{txoN22u NHq1PZUzPDN5OEW3Oi=>
Y-meso14 M3\vSWNmdGxiVnnhZoltcXS7IFHzd4F6 NYrRXWt5OS1zMDFOwIcwdWx? M1G5XVczKGh? NHjBfm9KSzVyPkGwJO69\y:vbB?= NVXOSFg{OjR|N{i1O|Y>
MSTO-211H NXPPOpY5S2WubDDWbYFjcWyrdImgRZN{[Xl? NEfSbJAyNTFyIN88[{9udA>? NUGxUGxJPzJiaB?= MU\JR|UxhjBwMESg{txoN22u MWOyOFM4QDV5Nh?=
A549 NWPFXWRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO5OkBp NV3URmZbUUN3ME2xMlM2KM7:TR?= NFywfmEzPDN2OEi1OC=>
A549/PEM-1.6 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX65OkBp NYrSOXRHUUN3ME21MlA{KM7:TR?= MmnDNlQ{PDh6NUS=
A549/PEM-6.4 M1j6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\pPVYhcA>? M1nPR2lEPTB;MkOuN|kh|ryP NWHQZ5VZOjR|NEi4OVQ>
A549/PEM-16 M4PCRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHvVJI6PiCq NFnwbnhKSzVyPUWxMlQ2KM7:TR?= M1ztNVI1OzR6OEW0
HT-29 NH[4eldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSwXGFlPzMEoHlCpC=> MV;EUXNQyqB? NYXrbpRqUUN3ME2xNE4xPyEEsTCwMlk1KM7:TR?= NFi4bGUzOzl3OUS2NC=>
LoVo NEi0fXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XuOFczyqCqwrC= NWrUd|RWTE2VT9Mg MXPJR|UxRTBwMEOyJOKyKDBwMECyJO69VQ>? NUXCWoZ6OjN7NUm0OlA>
SW620 MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVq3NuKhcMLi NEm3W|RFVVORwrC= M{jCR2lEPTB;MT6wPUDDuSByLkCxJO69VQ>? NFroSVMzOzl3OUS2NC=>
HCT116 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkKyO|LDqGkEoB?= NXW2enhMTE2VT9Mg MU\JR|UxRTBwMES5JOKyKDBwMEGzJO69VQ>? M3;XSlI{QTV7NE[w
SW1116 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\udlI4OsLiaNMg NYDNVHRxTE2VT9Mg NYO2doFXUUN3ME2xMlcxKMLzIECuNFMh|ryP MWWyN|k2QTR4MB?=
WiDr MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXe3NuKhcMLi MmfaSG1UV8Li NGqyfHlKSzVyPUCuNFE6KMLzIECuNFAzKM7:TR?= MlztNlM6PTl2NkC=
HT-29 MoThSpVv[3Srb36gRZN{[Xl? NFi1fHgxNjB3wrFOwG0> NF7wflU4OsLiaB?= M2jTRmROW00EoB?= M1LjTolv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckB1cGViUzDwbIF{\cLi M{WxVVI{QTV7NE[w
LoVo MW\GeY5kfGmxbjDBd5NigQ>? MXKwMlA2yqEQvF2= NHnjfoY4OsLiaB?= Ml35SG1UV8Li M{[2fIlv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckB1cGViUzDwbIF{\cLi NHT6[WMzOzl3OUS2NC=>
STAV-AB NHLZdFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXPOFghcA>? Mo\0dJJweG:{dHnvckBw\iCuaY\lJINmdGy|PU[0MlTDuTJzLkigKS=> NYfRXYl{OjN6NECzO|Y>
M-14-K M4m0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvJNoRvPDhiaB?= NUD1UGxueHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVgyNjkEsUGyMlkhLQ>? NIPQT4szOzh2MEO3Oi=>
STAV-FCS M2DrW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXe0PEBp NYXjXJc{eHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVg5NjIEsUiuPUAm MWWyN|g1ODN5Nh?=
ZL-34 NXzZZppFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXm0PEBp MlyydJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm1MlfDuTZwNTCl MXuyN|g1ODN5Nh?=
JL-1 NF\tZXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jtcFQ5KGh? Ml\4dJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm4MlLDuTJwMjCl M1PNZlI{QDRyM{e2
DM-3 NIrkb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYG1XYwxPDhiaB?= NFv2Vodxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9NVAyNjQEsUKuPEAm NGn5WVAzOzh2MEO3Oi=>
Jurkat M2\ST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPlOFghcA>? MmPQdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUe2MlfDuTRwMzCl NUTne2o3OjN6NECzO|Y>
BXPC-3 NWT5fnJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN7Lki2xtEyNjZ6IN88US=> NE\EXo0zOjl5N{[wOy=>
PANC-1 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTh|Lke2xtExNjF7IN88US=> NXrBT3NXOjJ7N{e2NFc>
BXPC-3 MoG3SpVv[3Srb36gRZN{[Xl? NFqwdnM{QS56NjCg{txO NX;jWGx6OjRiaB?= MYTpcoR2[2W|IGOgZZJz\XO2IDjQQFAvODVrIHHu[EBl\WO{ZXHz[ZMhfGinIH71cYJmeiCxZjDj[YxteyCrbjD0bIUhTzJxTTDwbIF{\cLi NF7pSHIzOjl5N{[wOy=>
BXPC-3 M176dWZ2dmO2aX;uJGF{e2G7 MWKzPU45PiBizszN MnjBNlQhcA>? NUH5fmVF\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> NIP3bHIzOjl5N{[wOy=>
PANC-1 M3LIbWZ2dmO2aX;uJGF{e2G7 MVi4OEDPxE1? M1;DN|I1KGh? NXu2b3h1\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> NHPBboozOjl5N{[wOy=>
BXPC-3 NWLZOIhjTnWwY4Tpc44hSXO|YYm= NYrYVWNZOzlwOE[gJO69VQ>? MoTXNlQhcA>? NUfKcYhs\W6qYX7j[ZMhTUeIUjygTGVTOyCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= MXmyNlk4PzZyNx?=
PANC-1 NU\WWZptTnWwY4Tpc44hSXO|YYm= M1LoOVg1KM7:TR?= MnfiNlQhcA>? M{XuZoVvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NGPEUGUzOjl5N{[wOy=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Chk1 / Chk1 / Cyclin D / Cyclin E / p-Histone H3 / Histone H3 / Cyclin B1 / p-Cdc2 / Cdc2 ; 

PubMed: 22237209     


Protein alterations in the response to DNA damage, cell cycle progression, and cell death were detected in (c) UDG−/− cells and (d) UDG+/+ cells treated with pemetrexed. Cells were collected at 6 and 24 h after pemetrexed treatment. Results are representative of two independent experiments.

Topo IIα / Topo I / γH2AX / Cleaved PARP / Survivin; 

PubMed: 22237209     


Protein alterations involved in regulation of apoptotic cell death were detected in (c) UDG−/− cells and (d) UDG+/+ cells treated with pemetrexed. Cells were collected at 6 and 24 h after pemetrexed treatment. Results are representative of two independent experiments.

AKT / p-AKT / GSK3β / p-GSK3β ; 

PubMed: 24847863     


Akt activation in a time course dependent manner. Human lung adenocarcinoma A549 cells were treated without or with 1 µM pemetrexed for 0, 4, 8, 12, 24, and 48 h, and then cell lysates were isolated. After treatment, the levels of total Akt, phosphorylated Akt, total GSK3β, and phosphorylated GSK3β were examined by Western blot analysis. β-Actin was used as an internal loading control. 

EGFR / p-EGFR ; 

PubMed: 30953548     


After treatment with incremental exposure time of pemetrexed. The total and phosphorylated EGFR, AKT, and MAPK proteins in PC-9 cells were detected by Western blot. GAPDH served as the loading control. 

22237209 24847863 30953548
Immunofluorescence
p-AKT; 

PubMed: 24847863     


A549 cells were treated with 0, 0.1, 0.3, and 1 µM pemetrexed for 48 h. After treatment, the subcellular distribution of p-AktS473 was detected by confocal microscopy after immunostaining with anti-phospho-AktS473 and Rhodamine-conjugated secondary antibody. Hoechst 33342 was used to counter stain nuclei, and the images were overlaid to determine the Akt localization within the cell.

24847863
Growth inhibition assay
Cell viability; 

PubMed: 28719077     


Effects of metformin and (or) pemetrexed on the proliferation of human NSCLC cell lines. (A) Antiproliferative effects of metformin on NSCLC cells. (B) Effects of pemetrexed on the proliferation of the three tested cell lines. (C) Metformin in combination with pemetrexed inhibits the proliferation of the tested cells. (D–F) Effects of metformin and (or) pemetrexed on the proliferation of A549(D), HCC827(E), and H1975(F) cell lines. (G–I) Strengthening antiproliferative effects of metformin in combination with pemetrexed on A549(G), HCC827(H), H1975(I) cell lines,*P < 0.05. Metf represents metformin; Pem represents pemetrexed.

28719077
In vivo In the human H460 non-small cell lung carcinoma xenograft, Pemetrexed disodium produces a duration-dependent tumor growth delay (TGD). [3]

Protocol

Kinase Assay:[1]
+ Expand

Enzyme Assays and Methods. :

TS activity is assayed using a spectrophotometric method, which involved monitoring the increase in absorbance at 340 nm resulting from formation of the product, 7,8-dihydrofolate. The assay buffer contains 50 mM N-tris[hydroxymethyljmethyl-2-aminoethanesulfonic acid, 25 mM MgC12, 6.5 mM formaldehyde, 1 mM EDTA, and 75 mM 2-mercaptoethanol, pH 7.4. The concentrations of deoxyuridylate monophosphate, 6R-MTHF, and hIS are 100 μM, 30μM and 30 nM (1.7 milliunits/mL), respectively. At the 6R-MTHF concentration, an uninhibited reaction and six concentrations of inhibitor are assayed. Ki app values are determined by fitting the data to the Morrison equation using nonlinear regression analysis with the aid of the program ENZFITTER. Ki values are calculated using the equation: Ki app= Ki(1 + [S]/Km), where [S] is equal to 30 μM and Km is equal to 3 μM. DHFR activity is assayed spectrophotometrically by monitoring the dis appearance of the substrates NADPH and 7,8-dihydrofolate at 340 nm. The reaction takes place at 25°C in 0.5 mL of 50 mM potassium phosphate buffer, which contains 150 mM KC1 and 10 nM 2-mercaptoethanol, pH 7.5, and 14 nM (0.34 milliunitlmL) DHFR. The NADPH concentration is 10 μM and 7,8-dihydrofolate is varied at 5, 10, or 15 μM. At each 7,8-dihydrofolate concentration, an uninhibited reaction and seven concentrations of inhibitor are assayed. The ENZFITI'ER microcomputer program is used to obtain Ki app values by fitting the data to the Morrison equation by nonlinear regression analysis. Ki app= Ki(1 + [S]/Km), where [S] is equal to the concentration of 7,8-dihydrofolate used and Km of 7,8-dihydrofolate is equal to 0.15 μM. GARFT activity is assayed spectrophotometrically by monitoring the increase of absorbance resulting from formation of the product 5,8-dideazafolate at 295 nm. The reaction solvent contains 75 mM HEPES, 20% glycerol, and 50 mM a-thioglygerol, pH 7.5, at 25°C. The concentrations of substrates and enzyme used are 10 μM α,β-glycinamide ribonucleotide, 0-10 μM 10-formyl-5,8-dideazafolic acid, and 10 nM (1.9 milliunits/mL) GARFT. Ki values are calculated using the Enzyme Mechanism program of the Beckman DU640 spectrophotometer, which uses nonlinear regression analysis to fit data to the Michaelis-Menten equation for competitive inhibition.
Cell Research:[1]
+ Expand
  • Cell lines: CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells.
  • Concentrations: 0-30 μM
  • Incubation Time: 72 hours
  • Method: Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC50). Pemetrexed disodium is dissolved initially in DMSO at a concentration of 4 mg/mL and further diluted with cell culture medium to the desired concentration. CCRF-CEM leukemia cells in complete medium are added to 24-well Cluster plates in a total volume of 2.0 mL. Pemetrexed disodium at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 hour at 37 °C in an atmosphere of 5% CO2 in air. At the end of the incubation, cell numbers are determined on a ZBI Coulter counter. For several studies, IC50s are determined for each compound in the presence of either 300 μM AICA, 5 μM thymidine, 100 μM hypoxanthine, or combination of 5 μM hymidine plus 100 μM hypoxanthine. For adherent tumor cells, a modification of the original MTT colorimetric assay is used to measure cell cytotoxicity. The human tumor cells are seeded in 100 μL assay medium/well in 96-well flat-bottomed tissue culture plates. The assay medium contains folic acid-free RPMI 1640 supplemented with 10% FCS and either 2 nM folinic acid or 2.3 μM folic acid as the sole folate source. Well 1A is left blank. Stock solutions of antifolates are prepared in Dulbecco's PBS at 1 mg/mL, and a series of 2-fold dilutions are subsequently made in PBS. Ten-μL aliquots of each concentration are added to triplicate wells. Plates are incubated for 72 hours at 37 °C in a humidified atmosphere of 5% CO2-in-air. MTT is dissolved in PBS at 5 mg/mL, 10 μL of stock MTF solution are added to each well of an assay, and the plates are incubated at 37 °C for 2 additional hours. Following incubation, 100 μL of DMSO are added to each well. After thorough formazan solubilization, the plates are read on a Dynatech MR600 reader, using a test wavelength of 570 nm and a reference wavelength of 630 nm. The IC50 is determined as the concentration of drug required to inhibit cell growth by 50% compared to an untreated controls.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: EMT-6 mammary carcinoma, the human HCT 116 colon carcinoma, and the human H460 non-small cell lung carcinoma are injected s.c. into the nude mice.
  • Formulation: Pemetrexed disodium is dissolved in DMSO and then diluted in water.
  • Dosages: 100 mg/kg or 150 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 94 mg/mL (199.41 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 471.37
Formula

C20H19N5Na2O6

CAS No. 150399-23-8
Storage powder
in solvent
Synonyms LY-231514

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03875144 Not yet recruiting Peritoneal Mesothelioma|Peritoneal Carcinomatosis Institut du Cancer de Montpellier - Val d''Aurelle November 2019 Phase 2
NCT03875144 Not yet recruiting Peritoneal Mesothelioma|Peritoneal Carcinomatosis Institut du Cancer de Montpellier - Val d''Aurelle November 2019 Phase 2
NCT03863483 Not yet recruiting Nonsquamous Non-Small Cell Lung Cancer Xin-Hua Xu|China Three Gorges University Yichang China July 1 2019 Phase 2
NCT03863483 Not yet recruiting Nonsquamous Non-Small Cell Lung Cancer Xin-Hua Xu|China Three Gorges University Yichang China July 1 2019 Phase 2
NCT03830411 Not yet recruiting Nonsquamous Non-Small Cell Lung Cancer Xin-Hua Xu|China Three Gorges University Yichang China June 1 2019 Phase 2
NCT03830411 Not yet recruiting Nonsquamous Non-Small Cell Lung Cancer Xin-Hua Xu|China Three Gorges University Yichang China June 1 2019 Phase 2

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID