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 11 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 M1y3fmNmdGxiVnnhZoltcXS7IFHzd4F6 M{T3WFEh|ryP NITiU4I1QCCq MnXU[Y5p[W6lZYOgd4lufmG|dHH0bY4hcW6qaXLpeIVlKH[rYXLpcIl1gQ>? M1Ox[|I3OzN2M{Kw
A549 NGDCZ2FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NELNOWoyKM7:TR?= MX:0PEBp MYjlcohidmOnczDzbY13[XO2YYTpckBqdmirYnn0[YQhfmmjYnnsbZR6 MYGyOlM{PDN{MB?=
MSTO-211H M1PhO2Z2dmO2aX;uJGF{e2G7 MV[xJO69VQ>? MlXPNlQhcA>? M2fHNYVvcGGwY3XzJIF2fG:yaHHnfUBkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> M3T1UVI3OzN2M{Kw
A549 M{Xpd2Z2dmO2aX;uJGF{e2G7 M4Xq[lEh|ryP NXvDToY2OjRiaB?= MlLX[Y5p[W6lZYOgZZV1d3CqYXf5JINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu MWeyOlM{PDN{MB?=
MSTO-211H NFzQSpNCeG:ydH;zbZMhSXO|YYm= NUO4VmNFOSEQvF2= MkXuNlQhcA>? NXS5flhbcW6mdXPld{BieG:ydH;zbZMh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> MWWyOlM{PDN{MB?=
A549 MnfpRZBweHSxc3nzJGF{e2G7 NIjoOlMyKM7:TR?= M4HUfFI1KGh? NWHocnRZcW6mdXPld{BieG:ydH;zbZMh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NGfDdVAzPjN|NEOyNC=>
MSTO-211H NVLkclRNTnWwY4Tpc44hSXO|YYm= NHzFNWYyKM7:TR?= MlfnOFghcA>? NHnLW2FqdmO{ZXHz[ZMhSU2SSzDwbI9{eGixconsZZRqd25iYX7kJIEh[2:wY3;tbZRidnRiZHXjdoVie2ViaX6gRWtVKGGwZDDtWG9TKHCqb4PwbI9zgWyjdHnvckBkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> M2PGT|I3OzN2M{Kw
A549 MVjGeY5kfGmxbjDBd5NigQ>? MW[xJO69VQ>? NYC5Zm9RPDhiaB?= M1XjUIlv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NXuxd2syOjZ|M{SzNlA>
Vero NXjHdlg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqyNE4zOzUEoH3N MoDXNlQhcA>? NEe1W|doem:5dHigbY5pcWKrdHnvcl0297ns NVLYUFlVOjV7N{W2N|c>
A549 NFL5NlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\PUFAvOjN2wrDtUS=> M{jVU|I1KGh? NGGxVWloem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= NHjvV24zPTl5NU[zOy=>
HeLa NXG2cXk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jZOVAvOjN2wrDtUS=> NWjFPFgyOjRiaB?= MoT3[5Jwf3SqIHnubIljcXSrb369Og+6sg>? Mlf3NlU6PzV4M{e=
T47D NHf5NYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\EUXExNjJ|NNMgcW0> Mn;hNlQhcA>? NXqw[nVP\3Kxd4ToJIlvcGmkaYTpc44:OTExubq= NHPyTJAzPTl5NU[zOy=>
Vero MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqwMlI{PMLibV2= MVy0PEBp NGTHfoJoem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= M{XKb|I2QTd3NkO3
A549 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWiwMlI{PMLibV2= MVi0PEBp NEnHNpNoem:5dHigbY5pcWKrdHnvcl0{OO,7qh?= NH6wbHMzPTl5NU[zOy=>
HeLa NFnGWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknwNE4zOzUEoH3N NF;2emc1QCCq M4Xvdodzd3e2aDDpcohq[mm2aX;uQVEx97ns MkH0NlU6PzV4M{e=
T47D MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMlI{PMLibV2= MWi0PEBp M33QOodzd3e2aDDpcohq[mm2aX;uQVIx97ns Mke3NlU6PzV4M{e=
Vero MoToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HPR|AvOjN2wrDtUS=> NUGxZXBJPzJiaB?= MULndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? NYDnO4xkOjV7N{W2N|c>
A549 NEW0O29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTsT3RWOC5{M{VCpI1O MU[3NkBp M17JO4dzd3e2aDDpcohq[mm2aX;uQVUx97ns MnTRNlU6PzV4M{e=
HeLa NXLQT|ZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTZNXlGOC5{M{VCpI1O Mn;pO|IhcA>? M2n3eYdzd3e2aDDpcohq[mm2aX;uQVIx97ns Moe3NlU6PzV4M{e=
T47D MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnpUJhYOC5{M{VCpI1O M2HGVFczKGh? MnLp[5Jwf3SqIHnubIljcXSrb369N|Dwwap? M2G4RlI2QTd3NkO3
A459 MlLWSpVv[3Srb36gRZN{[Xl? NWLmSZdkOS9{L{Sg{txO NGTOTVAzPC92ODDo NV\IfFJ5cW6mdXPld{BIOSCyaHHz[UBienKnc4SgbY4h\G:|ZT2gZY5lKHSrbXWg[IVx\W6mZX70JI1idm6nch?= NI\pPVYzPTd2M{iyNi=>
A459 M1PqXGZ2dmO2aX;uJGF{e2G7 M1j1b|EwOi92IN88US=> MoP1OFghcA>? NIryN5Rl\WO{ZXHz[ZMhfGinIHzleoVteyCxZjDwMWFsfA>? M3S3N|I2PzR|OEKy
A459 NH3EN5FCeG:ydH;zbZMhSXO|YYm= MoLHOO69VQ>? MkXZOFghcA>? M3\1XIlv\HWlZYOgZZBweHSxc3nz M2\jfFI2PzR|OEKy
HepG2 NVz1OIt7S2WubDDWbYFjcWyrdImgRZN{[Xl? NHvjb4IxNjIkgKOxNFDDqM7:TR?= NYLsV4ZWPzJiaB?= MXHobYdpKGOxbnPlcpRz[XSrb37zJI9nKHCnbXX0doV5\WRiYYSgLFExNzFyMNMg{txOMSCxbnz5JJNtcWeqdHz5JIlvcGmkaYTzJGhmeEd{IHPlcIwhe3W{dnn2ZYw> MXeyOVQ1PjFyMh?=
HepG2 NF7EXo1CeG:ydH;zbZMhSXO|YYm= M1jNWFAvOeLCk{GwNOKh|ryP NIXqcHU4OiCq MX7pcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueTDheEBpcWeqIHPvcoNmem62cnH0bY9v MonXNlU1PDZzMEK=
HepG3 MkXrSpVv[3Srb36gRZN{[Xl? M1nEb|AvOeLCk{GwNOKh|ryP NG\Bb2M1QCCq MkPzbY5lfWOnczDwOlIh\G:5boLl[5Vt[XSrb36gZZMhf2WubDDhd{BD\WOuaX6tNUBidmRiTFOzRk1KUSC3cILl[5Vt[XSrb36= NULoeIRyOjV2NE[xNFI>
HepG3 MULGeY5kfGmxbjDBd5NigQ>? NGLYblYxNjIkgKOxNFDDqM7:TR?= MWC0PEBp NFXZcJJi[3SrdnH0[ZMh[3m2bz3wdo91\WO2aY\lJIF2fG:yaHHnfeKh M{TXbVI2PDR4MUCy
HepG3 M1vweGZ2dmO2aX;uJGF{e2G7 NGDlS|kyOMLizszN MUi0PEBp MYX1dJJm\3WuYYTld{BxcG:|cHjvdplt[XSnZDCodE0qKE2HS{GvNkApW2W{MkG3M|IzOSliYX7kJJAuTVKNMT:yJEhVcHJ{MEKvWJlzOjB2KR?= MXGyOVQ1PjFyMh?=
U20S NVT1RVdWS2WubDDWbYFjcWyrdImgRZN{[Xl? M2CydlAvODFvMUCwJO69VQ>? NF23VI44OiCq NXXkTmNLcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\WSncHXu[IVvfGy7 NHvuN5czPTF3MkO5PS=>
MG-63 MmjkR4VtdCCYaXHibYxqfHliQYPzZZk> M2nP[FAvODFvMUCwJO69VQ>? NF;ERZU4OiCq NHf3[XhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5Nm\GWyZX7k[Y51dHl? M1n5SFI2OTV{M{m5
A549 M4DFUmNmdGxiVnnhZoltcXS7IFHzd4F6 M3u3NFEuOTByMDDuUS=> MUC3NkBp NHXHOYhKSzVyPUGzO{BvVQ>? Mo\WNlUyPDV4Nkm=
H1299 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXOxMVExODBibl2= NWT2eVVyPzJiaB?= M2jaZWlEPTB;MUe4JI5O MVWyOVE1PTZ4OR?=
MSTO-211 M1zoemNmdGxiVnnhZoltcXS7IFHzd4F6 M1PzUFEh|ryP NH2xWnI1QCCq M1vvNpBzd2S3Y3XzJIEhe3mwZYLnbZN1cWNiaX7obYJqfG:{eTDl[oZm[3Rib36geIhmKGOnbHyg[5Jwf3SqIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? MoPnNlUxQTZ7OUO=
A549 M2PjbGNmdGxiVnnhZoltcXS7IFHzd4F6 MlTrNUDPxE1? M1LCTVQ5KGh? MX\wdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv MVeyOVA6Pjl7Mx?=
MSTO-211 NX\KVndqSXCxcITvd4l{KEG|c3H5 MUGxJO69VQ>? MXe0PEBp M2nOVYVvcGGwY3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu MXqyOVA6Pjl7Mx?=
A549 NWj6Nm1CSXCxcITvd4l{KEG|c3H5 NXHzRYtuOSEQvF2= NF\FS5Y1QCCq M1fUXIVvcGGwY3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu NWnBPXh7OjVyOU[5PVM>
MSTO-211 MUnGeY5kfGmxbjDBd5NigQ>? MUKxJO69VQ>? MU[0PEBp NF7BO4NmdmijbnPld{BqdnS{YXPlcIx2dGG{IGLPV{Bxem:mdXP0bY9vKGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> NXvNZWF4OjVyOU[5PVM>
A549 MofXSpVv[3Srb36gRZN{[Xl? NXHSWmRUOSEQvF2= MoXaOFghcA>? M4\CWoVvcGGwY3XzJIlvfHKjY3XscJVt[XJiUl;TJJBzd2S3Y4Tpc44h[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> NHTucWgzPTB7Nkm5Ny=>
MSTO-211 MnfqSpVv[3Srb36gRZN{[Xl? NVHzZ2VNOSEQvF2= MoTLOFghcA>? NVPMXoZXdGWjZIOgeI8hdWm2b3Poc45lemmjbDDkfZNnfW6ldHnvckBkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu M17ucFI2ODl4OUmz
A549 MX\GeY5kfGmxbjDBd5NigQ>? M4i2XVEh|ryP MVO0PEBp MmPwcIVi\HNidH:gcYl1d2Oqb37kdolidCCmeYPmeY5kfGmxbjDjc41jcW6nZDD3bZRpKHOrbY\hd5RifGmw MX[yOVA6Pjl7Mx?=
A549  NVK5c5FSTnWwY4Tpc44hSXO|YYm= MmTjNk42NzVxMUCg{txO MVq0PEBp MoPIbY5kemWjc3XzJG5wgGFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MkXtNlQ6QTF5Nki=
H1792 NGfLfJJHfW6ldHnvckBCe3OjeR?= NHfKOo8zNjVxNT:xNEDPxE1? NXTzUWJMPDhiaB?= MnK3bY5kemWjc3XzJG5wgGFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NWXhR|RHOjR7OUG3Olg>
A549  NFPmbY1HfW6ldHnvckBCe3OjeR?= NWXORlk1Oi53IN88US=> MYW0PEBp NVPkOJpzcW6mdXPld{Bk[XOyYYPlMVktKGOjc4Dhd4UuOyCjbnSgdI9tgSBqQVTQMZJq[m:|ZTmgdI9tgW2ncnHz[UApWEGUUDmgZ4xm[X[jZ3W= M3\vUlI1QTlzN{[4
H1792 M164WmZ2dmO2aX;uJGF{e2G7 M1PxbVIvPSEQvF2= MYi0PEBp MlHXbY5lfWOnczDjZZNx[XOnLUmsJINie3Cjc3WtN{BidmRicH;sfUApSUSSLYLpZo9{\SlicH;sfY1memG|ZTCoVGFTWCliY3zlZZZi\2V? NGf4UpkzPDl7MUe2PC=>
A549  NWSxdmFETnWwY4Tpc44hSXO|YYm= NV33bXJiOi53L{WvNVAh|ryP M{\XNVQ5KGh? NH7nPZZld3ewcnXneYxifGW|IF3jcE0yyqB? NWrHSmlxOjR7OUG3Olg>
H1792 MXLGeY5kfGmxbjDBd5NigQ>? MViyMlUwPS9zMDFOwG0> Ml6yOFghcA>? MXHkc5dvemWpdXzheIV{KE2lbD2xxsA> NGXmVlIzPDl7MUe2PC=>
A549 M2HJcGFxd3C2b4Ppd{BCe3OjeR?= NF[2XZMzNjVizszN MofmOFghcA>? NW\KXWw5cW6mdXPld{BieG:ydH;zbZM> NWTKfmp4OjR7OUG3Olg>
A549 MV7GeY5kfGmxbjDBd5NigQ>? NUP3Wo11PSEQvF2= MX24JIg> MX;pcoNz\WG|ZYOgUYNtNTFidXLpdZVqfGmwYYTpc44hdGW4ZXzz NEjCfIszPDl7MUe2PC=>
A549 MVLGeY5kfGmxbjDBd5NigQ>? MWOxJOK2VQ>? MYW0M|gwOTJxMkSvOFghcA>? MYDpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHCqb4PwbI9zgWyjdHXkJGFsfCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? MXOyOFg1Pzh4Mx?=
A549 NVT3UGs2TnWwY4Tpc44hSXO|YYm= MYqwMlEwOC5|L{Gg{txO M1\HO|Q5KGh? NUjSfIRbcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwbI9{eGixconsZZRm\CCDa4SgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MYKyOFg1Pzh4Mx?=
A549 NG\EbnVCeG:ydH;zbZMhSXO|YYm= MUOwMlEwOC5|L{Gg{txO NWDYV2pmPDhiaB?= M1\Qb4lv\HWlZYOgZZBweHSxc3nzJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MYqyOFg1Pzh4Mx?=
A549 NHXMXZJHfW6ldHnvckBCe3OjeR?= MWiwMlEwOC5|L{Gg{txO NVTZcWEyPDhiaB?= M4jWd4lv[3KnYYPld{B1cGVicnH0bY8hd2ZiUz3wbIF{\SCyb4D1cIF1cW:w NGPyR3MzPDh2N{i2Ny=>
PC9 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXG3NkBp NUPYeol7UUN3ME2xOk4xPcLzMT64OUBvVQ>? M2naT|I1QDRyOEmx
PC9/GR M1fiXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M376SlczKGh? MYDJR|UxRTRwOUVCtVAvPDRyIN88US=> Mkj5NlQ5PDB6OUG=
PC9 MX3GeY5kfGmxbjDBd5NigQ>? NYf5OVk1OTZibl2= M37vNVczKGh? MYHpcoR2[2W|IGOtdIhie2ViYYLy[ZN1 MnLWNlQ5PDB6OUG=
PC9/GR MULGeY5kfGmxbjDBd5NigQ>? MkjOOE46PCEQvF2= NHv1[lI4OiCq MlHobY5lfWOnczDTMZBp[XOnIHHydoV{fA>? Mn\QNlQ5PDB6OUG=
PC9 NUnQWJNoSXCxcITvd4l{KEG|c3H5 MlTONVYhdk1? MVK3NkBp NHuydY5qdmS3Y3XzJFE1NjV278oqJIFxd3C2b4Ppdy=> NWXPO2hVOjR6NEC4PVE>
PC9/GR M2fWT2Fxd3C2b4Ppd{BCe3OjeR?= Mm[zOE46PCEQvF2= NEjSSXk4OiCq MXTpcoR2[2W|IEG5MlU197nsIHHwc5B1d3Orcx?= NG\McY8zPDh2MEi5NS=>
PC9/GR MnXOSpVv[3Srb36gRZN{[Xl? MnPiOE46PCEQvF2= MXK3NkBp Mm\5bY5kemWjc3XzJJAuTVKNIHzleoVtew>? MXGyOFg1ODh7MR?=
PC9/GR NF\vWXdHfW6ldHnvckBCe3OjeR?= MUW0Mlk1KM7:TR?= M4nPNVczKGh? NIjjV2ZqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy| NGrOT2ozPDh2MEi5NS=>
H28 M3Xhbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHSUpltUUN3ME2wMlA4yrFyLkCyJO69VQ>? NGmyWGozPDdzNEeyNi=>
211H MkXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYO2bZF2UUN3ME2wMlA4yrFyLkCxJO69VQ>? NETReFgzPDdzNEeyNi=>
H2052 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTnTWM2OD1yLkW3xtExNjN2IN88US=> NWftS3pxOjR5MUS3NlI>
H2452 NFjiV5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XLXWlEPTExvK6xNFAh|ryP M1\YOFI1PzF2N{Ky
MES01 M1zkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjSTmJKSzVy78{eNVAxKM7:TR?= NVSz[FhGOjR5MUS3NlI>
MES04 NYm2PYhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm1cmN{UUN3MP-8olExOCEQvF2= MUWyOFcyPDd{Mh?=
A549 NYrBeGtCS2WubDDWbYFjcWyrdImgRZN{[Xl? NGXXUHAxNjFxMD6zM|AvPS9zIN88US=> Ml3DNlQwPDhiaB?= NHrifnJFVVOR MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NV3lNHk1OjR4Mk[3NlI>
A549 NXjL[|RSTnWwY4Tpc44hSXO|YYm= NYfU[WRQOC5zL{CuN{8xNjVxMTFOwG0> NIG2dYEzPC92ODDo Mnj2SG1UVw>? MlPLdJJw\HWlZYOgeIhmKG[xcn3heIlwdiCxZjDBWm9{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXLmPYt[OjR4Mk[3NlI>
H1993 M4\vUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVyzSVREUUN3ME2wMlE4KM7:TR?= MUKyOFQyQDVzOR?=
H1299 NXHMV2hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7ye2lKSzVyPUGuPFQh|ryP M17ac|I1PDF6NUG5
H226 NXvFfJZ{S2WubDDWbYFjcWyrdImgRZN{[Xl? MYWxMVExKM7:Zz;tcC=> NXj4[HJjPzJiaB?= NXH1bno6UUN3ME6xNEDPxGdxbXy= NY[5PIU1OjR|N{i1O|Y>
H290 M3TnWGNmdGxiVnnhZoltcXS7IFHzd4F6 NH;B[5oyNTFyIN88[{9udA>? MXG3NkBp NED4cJdKSzVyPkGwJO69\y:vbB?= NEnycYgzPDN5OEW3Oi=>
Y-meso14 M{TXVWNmdGxiVnnhZoltcXS7IFHzd4F6 MXuxMVExKM7:Zz;tcC=> NYrIWnNwPzJiaB?= NVfs[IpnUUN3ME6xNEDPxGdxbXy= MlzPNlQ{Pzh3N{[=
MSTO-211H MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYGxMVExKM7:Zz;tcC=> NH7iXY44OiCq NH7ZSIlKSzVyfkCuNFQh|rypL33s M3zIRlI1Ozd6NUe2
A549 NF\GNXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm3WnpKQTZiaB?= NYO4WHNoUUN3ME2xMlM2KM7:TR?= M1vaNlI1OzR6OEW0
A549/PEM-1.6 NX7rT2xST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\3RZA6PiCq NUjUZ3MyUUN3ME21MlA{KM7:TR?= NUXYfIs{OjR|NEi4OVQ>
A549/PEM-6.4 M3PYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYq4cXRwQTZiaB?= M4PDN2lEPTB;MkOuN|kh|ryP NGnaSlgzPDN2OEi1OC=>
A549/PEM-16 M1i2c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PRPFk3KGh? NGnvN3BKSzVyPUWxMlQ2KM7:TR?= M2PWR|I1OzR6OEW0
HT-29 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nVSlczyqCqwrC= NHrhN2NFVVORwrC= MnvRTWM2OD1zMD6wO{DDuSByLkm0JO69VQ>? NV76dGprOjN7NUm0OlA>
LoVo MkLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[3NuKhcMLi MXzEUXNQyqB? NXzRfJRDUUN3ME2wMlA{OiEEsTCwMlAxOiEQvF2= NYHucWtVOjN7NUm0OlA>
SW620 MlzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHTO|LDqGkEoB?= NXTFWo9WTE2VT9Mg NH3admpKSzVyPUGuNFkhyrFiMD6wNUDPxE1? MlHWNlM6PTl2NkC=
HCT116 M13KeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TkNFczyqCqwrC= M360dmROW00EoB?= NGTvcFdKSzVyPUCuNFQ6KMLzIECuNFE{KM7:TR?= MoDHNlM6PTl2NkC=
SW1116 NEWwdotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHJdGE4OsLiaNMg M4ezbWROW00EoB?= NWnSbGpEUUN3ME2xMlcxKMLzIECuNFMh|ryP NEWxfVQzOzl3OUS2NC=>
WiDr NHm1SY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnzZ2c4OsLiaNMg NH3HXVJFVVORwrC= MoHzTWM2OD1yLkCxPUDDuSByLkCwNkDPxE1? MkH0NlM6PTl2NkC=
HT-29 MUHGeY5kfGmxbjDBd5NigQ>? NGTVfWgxNjB3wrFOwG0> MkTrO|LDqGh? MlrSSG1UV8Li Ml3kbY5kemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJJRp\SCVIIDoZZNmyqB? M2PQU|I{QTV7NE[w
LoVo Ml;pSpVv[3Srb36gRZN{[Xl? NWDlVYs1OC5yNdMg{txO M3Hi[FczyqCq MkXwSG1UV8Li MU\pcoNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6geIhmKFNicHjhd4XDqA>? MknBNlM6PTl2NkC=
STAV-AB NH7QfmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX4OFghcA>? NH\VVWNxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9OlQvPMLzMkGuPEAm MYmyN|g1ODN5Nh?=
M-14-K NILIZYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPHbVA1QCCq MYTwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OEGuPOKyOTJwOTCl M2PsOVI{QDRyM{e2
STAV-FCS MlzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYC0PEBp NFPMSG5xem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PFgvOcLzOD65JEU> NHf0dmUzOzh2MEO3Oi=>
ZL-34 NYm2c|VCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X3O|Q5KGh? MlH1dJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm1MlfDuTZwNTCl M4LVeVI{QDRyM{e2
JL-1 NYfXR2hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX34cVhtPDhiaB?= MlHKdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm4MlLDuTJwMjCl NHmyWZIzOzh2MEO3Oi=>
DM-3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M336SVQ5KGh? NFjO[3dxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9NVAyNjQEsUKuPEAm NIDUZ2wzOzh2MEO3Oi=>
Jurkat MkTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYi0PEBp MUXwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;N{[uO:KyPC5|IDW= NHTFemgzOzh2MEO3Oi=>
BXPC-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfMWHdKSzVyPUO5Mlg3yrFzLk[4JO69VQ>? NXXvenY4OjJ7N{e2NFc>
PANC-1 MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljjTWM2OD16Mz63OuKyOC5zOTFOwG0> MUeyNlk4PzZyNx?=
BXPC-3 MULGeY5kfGmxbjDBd5NigQ>? NV7k[JNKOzlwOE[gJO69VQ>? M4rsclI1KGh? NWfXSmdvcW6mdXPld{BUKGG{cnXzeEApWDxyLkC1LUBidmRiZHXjdoVie2W|IITo[UBvfW2kZYKgc4Yh[2WubIOgbY4hfGinIFeyM20heGijc3ZCpC=> M1TlVlIzQTd5NkC3
BXPC-3 M4PDdmZ2dmO2aX;uJGF{e2G7 MU[zPU45PiBizszN MXOyOEBp NXrHOlFM\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> MnPuNlI6Pzd4MEe=
PANC-1 M4qxXWZ2dmO2aX;uJGF{e2G7 NXT0do9CQDRizszN MV6yOEBp M1q0V4VvcGGwY3XzJGVITlJicHjvd5Bpd3K7bHH0[YQhdGW4ZXzzMEBidmRidHjlJJBzd3SnaX6gcIV3\Wy|wrC= MV:yNlk4PzZyNx?=
BXPC-3 MnHPSpVv[3Srb36gRZN{[Xl? M3v2cFM6Njh4IDFOwG0> M{PX[|I1KGh? M4m4d4VvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NX7ST2VkOjJ7N{e2NFc>
PANC-1 MkLhSpVv[3Srb36gRZN{[Xl? NEPCcI85PCEQvF2= MkDFNlQhcA>? MlH0[Y5p[W6lZYOgSWdHWixiSFXSN{BidmRiQVvUJJBpd3OyaH;yfYxifGmxbjDs[ZZmdHN? MUWyNlk4PzZyNx?=

... 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03298763 Recruiting Genetic: MSCTRAIL|Drug: Placebo Adenocarcinoma of Lung University College London March 5 2019 Phase 1|Phase 2
NCT03656549 Recruiting Drug: Pemetrexed Non Small Cell Lung Cancer|Mesothelioma Radboud University|ZonMw: The Netherlands Organisation for Health Research and Development February 1 2019 Phase 2
NCT03655821 Recruiting Drug: Pemetrexed Non Small Cell Lung Cancer|Mesothelioma Radboud University|ZonMw: The Netherlands Organisation for Health Research and Development February 1 2019 Phase 4
NCT03526900 Recruiting Drug: Atezolizumab Non-small Cell Lung Cancer Stage IV Spanish Lung Cancer Group July 7 2018 Phase 2

Tech Support

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID