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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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.

    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.

  • 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.

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 M1H2bWNmdGxiVnnhZoltcXS7IFHzd4F6 Moq0NUDPxE1? MnPzOFghcA>? M3:0e4VvcGGwY3XzJJNqdX[jc4TheIlvKGmwaHnibZRm\CC4aXHibYxqfHl? MmD6NlY{OzR|MkC=
A549 M2r2[2NmdGxiVnnhZoltcXS7IFHzd4F6 NInyOpUyKM7:TR?= M2O1TVQ5KGh? M{XNO4VvcGGwY3XzJJNqdX[jc4TheIlvKGmwaHnibZRm\CC4aXHibYxqfHl? NXrDdYhDOjZ|M{SzNlA>
MSTO-211H M3HMTmZ2dmO2aX;uJGF{e2G7 M{fnNFEh|ryP MmHnNlQhcA>? M3i2XIVvcGGwY3XzJIF2fG:yaHHnfUBkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> M2H6dlI3OzN2M{Kw
A549 NGr6N5FHfW6ldHnvckBCe3OjeR?= M4rHcVEh|ryP MXqyOEBp MVTlcohidmOnczDheZRweGijZ4mgZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= Mlf1NlY{OzR|MkC=
MSTO-211H MXLBdI9xfG:|aYOgRZN{[Xl? NF7WNZEyKM7:TR?= M3rBdFI1KGh? NIHLR2lqdmS3Y3XzJIFxd3C2b4Ppd{Bkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> NVnweIZ{OjZ|M{SzNlA>
A549 MXfBdI9xfG:|aYOgRZN{[Xl? NVn4[pg6OSEQvF2= NIPVZpgzPCCq MofDbY5lfWOnczDhdI9xfG:|aYOgZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= NHPsOGczPjN|NEOyNC=>
MSTO-211H MYPGeY5kfGmxbjDBd5NigQ>? NWDSW|U6OSEQvF2= M1vyXVQ5KGh? NUf5e2s2cW6lcnXhd4V{KEGPUFugdIhwe3Cqb4L5cIF1cW:wIHHu[EBiKGOxbnPvcYl1[W62IHTlZ5Jm[XOnIHnuJGFMXCCjbnSgcXRQWiCyaH;zdIhwenmuYYTpc44h[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NVPwXI81OjZ|M{SzNlA>
A549 M3LOVGZ2dmO2aX;uJGF{e2G7 M{HDSlEh|ryP NU\qfGNmPDhiaB?= M1f0c4lv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NFu5PXMzPjN|NEOyNC=>
Vero M3;QeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzlSoJNOC5{M{VCpI1O MnP2NlQhcA>? Ml2z[5Jwf3SqIHnubIljcXSrb369Og+6sg>? NYHEZmlrOjV7N{W2N|c>
A549 NGH1Xo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDNUYcxNjJ|NNMgcW0> MWqyOEBp NVHMb2dV\3Kxd4ToJIlvcGmkaYTpc44:OTExubq= NVXTfGYzOjV7N{W2N|c>
HeLa NH3ie29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfPfIllOC5{M{VCpI1O NHnkXW0zPCCq NVntZ|Ns\3Kxd4ToJIlvcGmkaYTpc44:Pe,7qh?= M3jsTVI2QTd3NkO3
T47D NHfQW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrJWpkxNjJ|NNMgcW0> MU[yOEBp M2j2OYdzd3e2aDDpcohq[mm2aX;uQVEx97ns NX7mRoRGOjV7N{W2N|c>
Vero NGjWdHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH1NE4zOzUEoH3N MUO0PEBp NITCdG9oem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= M4GwelI2QTd3NkO3
A549 MnO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUKwMlI{PMLibV2= NIK1c5A1QCCq NV3lZXFU\3Kxd4ToJIlvcGmkaYTpc44:OzExubq= MkT5NlU6PzV4M{e=
HeLa NEnIcYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfqPXM3OC5{M{VCpI1O M4TzdVQ5KGh? M1Gxfodzd3e2aDDpcohq[mm2aX;uQVEx97ns MX:yOVk4PTZ|Nx?=
T47D NGiwSllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTkNE4zOzUEoH3N NVzsOVI2PDhiaB?= Mm\J[5Jwf3SqIHnubIljcXSrb369NlDwwap? NX;iNYFSOjV7N{W2N|c>
Vero MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHJNE4zOzUEoH3N NVy2TpV2PzJiaB?= NUHDeWRy\3Kxd4ToJIlvcGmkaYTpc44:OjExubq= M{GyblI2QTd3NkO3
A549 NWHTUGdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO2dHF3OC5{M{VCpI1O MW[3NkBp Mm\P[5Jwf3SqIHnubIljcXSrb369OVDwwap? MXmyOVk4PTZ|Nx?=
HeLa M4\2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\nNE4zOzUEoH3N M{nlflczKGh? MVnndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? NYn0SIVGOjV7N{W2N|c>
T47D MlzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXXOnFZOC5{M{VCpI1O NYW3S3ZzPzJiaB?= NYDGXldS\3Kxd4ToJIlvcGmkaYTpc44:OzExubq= MknMNlU6PzV4M{e=
A459 M3HBTGZ2dmO2aX;uJGF{e2G7 NUP5R5pwOS9{L{Sg{txO MUGyOE81QCCq NIT2NmZqdmS3Y3XzJGcyKHCqYYPlJIFzemW|dDDpckBld3OnLTDhcoQhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ MWSyOVc1Ozh{Mh?=
A459 NHPmO49HfW6ldHnvckBCe3OjeR?= MkXRNU8zNzRizszN M4TtR|Q5KGh? M{HlfYRm[3KnYYPld{B1cGVibHX2[Yx{KG:oIICtRYt1 NF;0dWczPTd2M{iyNi=>
A459 MUnBdI9xfG:|aYOgRZN{[Xl? MWK0{txO M{XucFQ5KGh? Mn32bY5lfWOnczDhdI9xfG:|aYO= NULyTnZ{OjV5NEO4NlI>
HepG2 MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1TIfFAvOeLCk{GwNOKh|ryP MoP1O|IhcA>? MUTobYdpKGOxbnPlcpRz[XSrb37zJI9nKHCnbXX0doV5\WRiYYSgLFExNzFyMNMg{txOMSCxbnz5JJNtcWeqdHz5JIlvcGmkaYTzJGhmeEd{IHPlcIwhe3W{dnn2ZYw> NFy4NVYzPTR2NkGwNi=>
HepG2 NFPaeo1CeG:ydH;zbZMhSXO|YYm= NGPSVW0xNjIkgKOxNFDDqM7:TR?= MUe3NkBp NGnOfm9qdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfUBifCCqaXfoJINwdmOncn70doF1cW:w NH\NU|YzPTR2NkGwNi=>
HepG3 NXHrenpsTnWwY4Tpc44hSXO|YYm= NYHwc254OC5z4pETNVAxyqEQvF2= NH7Pe5A1QCCq M4DYcolv\HWlZYOgdFYzKGSxd37y[Yd2dGG2aX;uJIF{KHenbHygZZMhSmWlbHnuMVEh[W6mIFzDN2IuUUlidYDy[Yd2dGG2aX;u NVq3SWhFOjV2NE[xNFI>
HepG3 MnL0SpVv[3Srb36gRZN{[Xl? M1zmOVAvOeLCk{GwNOKh|ryP M4j2d|Q5KGh? MXThZ5RqfmG2ZYOgZ5l1dy2ycn;0[YN1cX[nIHH1eI9xcGGpedMg MmHNNlU1PDZzMEK=
HepG3 MnrjSpVv[3Srb36gRZN{[Xl? M3zQcVExyqEQvF2= NYD4OpVZPDhiaB?= MYL1dJJm\3WuYYTld{BxcG:|cHjvdplt[XSnZDCodE0qKE2HS{GvNkApW2W{MkG3M|IzOSliYX7kJJAuTVKNMT:yJEhVcHJ{MEKvWJlzOjB2KR?= NIDQVlczPTR2NkGwNi=>
U20S NIfYU2RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mnn0NE4xOS1zMECg{txO NVzae25XPzJiaB?= MnrDbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[YRmeGWwZHXueIx6 NIHoWHgzPTF3MkO5PS=>
MG-63 MlW5R4VtdCCYaXHibYxqfHliQYPzZZk> NFPQT3ExNjBzLUGwNEDPxE1? NXvzPXN2PzJiaB?= MW\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4Pl[IVx\W6mZX70cJk> MYKyOVE2OjN7OR?=
A549 MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGjXfZQyNTFyMECgcm0> MYm3NkBp NVjoU4FVUUN3ME2xN|chdk1? NIjQXZIzPTF2NU[2PS=>
H1299 M{LYNGNmdGxiVnnhZoltcXS7IFHzd4F6 NX\mZ4VoOS1zMECwJI5O M13aNFczKGh? M{XMWWlEPTB;MUe4JI5O NHPDdmszPTF2NU[2PS=>
MSTO-211 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3XreVEh|ryP NF6ycok1QCCq MV3wdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv NXTzVoh3OjVyOU[5PVM>
A549 MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWjqdXRiOSEQvF2= NHTmXYo1QCCq NH\MVmRxem:mdXPld{BiKHO7bnXy[4l{fGmlIHnubIljcXSxcomg[YZn\WO2IH;uJJRp\SClZXzsJIdzd3e2aDDjc41jcW6nZDD3bZRpKHOrbY\hd5RifGmw NInROG0zPTB7Nkm5Ny=>
MSTO-211 M{PwN2Fxd3C2b4Ppd{BCe3OjeR?= M3vsXFEh|ryP MWq0PEBp NILnSIFmdmijbnPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> NE[3RYozPTB7Nkm5Ny=>
A549 MV\BdI9xfG:|aYOgRZN{[Xl? NUXV[ldDOSEQvF2= M174eVQ5KGh? MlPu[Y5p[W6lZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= NV3heZpHOjVyOU[5PVM>
MSTO-211 M1fv[GZ2dmO2aX;uJGF{e2G7 MofsNUDPxE1? M3HQfFQ5KGh? MVTlcohidmOnczDpcpRz[WOnbHz1cIFzKFKRUzDwdo9lfWO2aX;uJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= NFK1NWYzPTB7Nkm5Ny=>
A549 M1vpeGZ2dmO2aX;uJGF{e2G7 NVi2PWFsOSEQvF2= MlLJOFghcA>? M3XOcIVvcGGwY3XzJIlvfHKjY3XscJVt[XJiUl;TJJBzd2S3Y4Tpc44h[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> MoXFNlUxQTZ7OUO=
MSTO-211 MnvRSpVv[3Srb36gRZN{[Xl? MVixJO69VQ>? NYmwUW8zPDhiaB?= MUjs[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? MXGyOVA6Pjl7Mx?=
A549 MX;GeY5kfGmxbjDBd5NigQ>? MkLGNUDPxE1? MXS0PEBp NFLifYtt\WGmczD0c{BucXSxY3jvcoRzcWGuIHT5d4Z2dmO2aX;uJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= MXyyOVA6Pjl7Mx?=
A549  M3vsTmZ2dmO2aX;uJGF{e2G7 M1TtOlIvPS93L{GwJO69VQ>? NWXDZ2oxPDhiaB?= MU\pcoNz\WG|ZYOgUo95[SCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> NXjUb4FtOjR7OUG3Olg>
H1792 NH:yPG9HfW6ldHnvckBCe3OjeR?= MYqyMlUwPS9zMDFOwG0> M4rXPVQ5KGh? NFfXbY1qdmO{ZXHz[ZMhVm:6YTDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? NVXjToNqOjR7OUG3Olg>
A549  MknESpVv[3Srb36gRZN{[Xl? NEm1SmMzNjVizszN M{nP[|Q5KGh? MnTlbY5lfWOnczDjZZNx[XOnLUmsJINie3Cjc3WtN{BidmRicH;sfUApSUSSLYLpZo9{\SlicH;sfY1memG|ZTCoVGFTWCliY3zlZZZi\2V? MVmyOFk6OTd4OB?=
H1792 MlPHSpVv[3Srb36gRZN{[Xl? M{Oz[|IvPSEQvF2= MXm0PEBp M1vzWolv\HWlZYOgZ4F{eGG|ZT25MEBk[XOyYYPlMVMh[W6mIIDvcJkhMEGGUD3ybYJwe2VrIIDvcJlu\XKjc3WgLHBCWlBrIHPs[YF3[Wen MWGyOFk6OTd4OB?=
A549  M1Pj[2Z2dmO2aX;uJGF{e2G7 MnvFNk42NzVxMUCg{txO MnXyOFghcA>? M4q0UIRwf26{ZXf1cIF1\XNiTXPsMVHDqA>? MXiyOFk6OTd4OB?=
H1792 M2T0R2Z2dmO2aX;uJGF{e2G7 MUmyMlUwPS9zMDFOwG0> NETzUIQ1QCCq NHnGbFhld3ewcnXneYxifGW|IF3jcE0yyqB? M131UFI1QTlzN{[4
A549 M373UGFxd3C2b4Ppd{BCe3OjeR?= MnHQNk42KM7:TR?= NELxSZA1QCCq MXvpcoR2[2W|IHHwc5B1d3Orcx?= MYqyOFk6OTd4OB?=
A549 MlvLSpVv[3Srb36gRZN{[Xl? NWnmXm84PSEQvF2= NYPV[nd3QCCq NFHsfI9qdmO{ZXHz[ZMhVWOuLUGgeYJqeXWrdHnuZZRqd25ibHX2[Yx{ Mmi5NlQ6QTF5Nki=
A549 NV[5fIpJTnWwY4Tpc44hSXO|YYm= NUS4OHZSOSEEtV2= NIKwR3o1NzhxMUKvNlQwPDhiaB?= MXzpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHCqb4PwbI9zgWyjdHXkJGFsfCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? NETOU2EzPDh2N{i2Ny=>
A549 M4G4XmZ2dmO2aX;uJGF{e2G7 NV7Bb|lsOC5zL{CuN{8yKM7:TR?= MVy0PEBp MWnpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHCqb4PwbI9zgWyjdHXkJGFsfCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHf5c4szPDh2N{i2Ny=>
A549 MXXBdI9xfG:|aYOgRZN{[Xl? MoD2NE4yNzBwMz:xJO69VQ>? NUXn[GJ[PDhiaB?= MXnpcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NUnJS5JEOjR6NEe4OlM>
A549 NHjRRphHfW6ldHnvckBCe3OjeR?= NF7hNoUxNjFxMD6zM|Eh|ryP NF7i[nI1QCCq NV7BTZRRcW6lcnXhd4V{KHSqZTDyZZRqdyCxZjDTMZBp[XOnIIDvdJVt[XSrb36= MVOyOFg1Pzh4Mx?=
PC9 NX:xbZZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHhO|IhcA>? MU\JR|UxRTF4LkC1xtEyNjh3IH7N M{e4eVI1QDRyOEmx
PC9/GR NH73OWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm3NkBp NIjJ[WZKSzVyPUSuPVTDuTBwNESwJO69VQ>? M1HSV|I1QDRyOEmx
PC9 MVTGeY5kfGmxbjDBd5NigQ>? M{DuXlE3KG6P MVW3NkBp MmDGbY5lfWOnczDTMZBp[XOnIHHydoV{fA>? MWSyOFg1ODh7MR?=
PC9/GR NVK2UlF4TnWwY4Tpc44hSXO|YYm= M4XiS|QvQTRizszN MX[3NkBp Ml7vbY5lfWOnczDTMZBp[XOnIHHydoV{fA>? NGG4NogzPDh2MEi5NS=>
PC9 Mn3yRZBweHSxc3nzJGF{e2G7 MUexOkBvVQ>? NXrZNJExPzJiaB?= NFXkNXVqdmS3Y3XzJFE1NjV278oqJIFxd3C2b4Ppdy=> NIj1ZZAzPDh2MEi5NS=>
PC9/GR M3zGXmFxd3C2b4Ppd{BCe3OjeR?= M{PVOlQvQTRizszN M2LxTFczKGh? Mlm4bY5lfWOnczCxPU42PO,7qjDhdI9xfG:|aYO= NX\RPXN7OjR6NEC4PVE>
PC9/GR NFzuOIRHfW6ldHnvckBCe3OjeR?= NXflZ2w4PC57NDFOwG0> MoTtO|IhcA>? MnvZbY5kemWjc3XzJJAuTVKNIHzleoVtew>? M3rmW|I1QDRyOEmx
PC9/GR MWnGeY5kfGmxbjDBd5NigQ>? NHvNRmw1Njl2IN88US=> NHv3Ung4OiCq M3WzW4lv[3KnYYPld{BxNUGNVDDs[ZZmdHN? NWjiUJZmOjR6NEC4PVE>
H28 NHjSeJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3KbXV3UUN3ME2wMlA4yrFyLkCyJO69VQ>? M3ztfVI1PzF2N{Ky
211H MnviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMEhCtVAvODFizszN MU[yOFcyPDd{Mh?=
H2052 NYPCc3pjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTBwNUhCtVAvOzRizszN M3;kd|I1PzF2N{Ky
H2452 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LPfmlEPTExvK6xNFAh|ryP MmnaNlQ4OTR5MkK=
MES01 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTmWXR3UUN3MP-8olExOCEQvF2= NYPEflF[OjR5MUS3NlI>
MES04 M2LQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|Ux97zgMUCwJO69VQ>? NX;uZmpsOjR5MUS3NlI>
A549 NH[1TY1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWCwMlEwOC5|L{CuOU8yKM7:TR?= NWHqbWxDOjRxNEigbC=> NX[1ZYZzTE2VTx?= NWC5OpZjcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MVyyOFYzPjd{Mh?=
A549 MU\GeY5kfGmxbjDBd5NigQ>? NIrOdmgxNjFxMD6zM|AvPS9zIN88US=> M{\2XFI1NzR6IHi= M33hVmROW09? M4rEOZBzd2S3Y3XzJJRp\SCob4LtZZRqd25ib3[gRXZQeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVfPU5FrOjR4Mk[3NlI>
H1993 NH;WZpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;S[4IzUUN3ME2wMlE4KM7:TR?= M1HMV|I1PDF6NUG5
H1299 MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrw[29KSzVyPUGuPFQh|ryP NGCzRWMzPDRzOEWxPS=>
H226 M2HVemNmdGxiVnnhZoltcXS7IFHzd4F6 NYrvR2lmOS1zMDFOwIcwdWx? NFHaco44OiCq MWDJR|UxRjFyIN88[{9udA>? NYjReoVwOjR|N{i1O|Y>
H290 MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUTOOI5GOS1zMDFOwIcwdWx? MV63NkBp NV\teFRlUUN3ME6xNEDPxGdxbXy= NXjlcol7OjR|N{i1O|Y>
Y-meso14 MnrrR4VtdCCYaXHibYxqfHliQYPzZZk> M1jYdFEuOTBizsznM41t M37sRlczKGh? M1TX[WlEPTB-MUCg{txoN22u Ml\ENlQ{Pzh3N{[=
MSTO-211H NUPzNWx6S2WubDDWbYFjcWyrdImgRZN{[Xl? NI\WdXYyNTFyIN88[{9udA>? MmfkO|IhcA>? MYrJR|UxhjBwMESg{txoN22u M3vVSVI1Ozd6NUe2
A549 M4DVemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDsdok6PiCq M1nDTWlEPTB;MT6zOUDPxE1? MV:yOFM1QDh3NB?=
A549/PEM-1.6 Mkm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvX[ms6PiCq NGC1VlBKSzVyPUWuNFMh|ryP MmnzNlQ{PDh6NUS=
A549/PEM-6.4 NVnPRYhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S4eFk3KGh? MUnJR|UxRTJ|LkO5JO69VQ>? MV[yOFM1QDh3NB?=
A549/PEM-16 M4\YeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYm5OkBp MU\JR|UxRTVzLkS1JO69VQ>? NHv4eFAzPDN2OEi1OC=>
HT-29 MnvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTwO|LDqGkEoB?= M2i3UGROW00EoB?= MYfJR|UxRTFyLkC3JOKyKDBwOUSg{txO M2\0bFI{QTV7NE[w
LoVo NXrIPGFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYG3NuKhcMLi Ml7ySG1UV8Li MXLJR|UxRTBwMEOyJOKyKDBwMECyJO69VQ>? M3n3bVI{QTV7NE[w
SW620 MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\3cFE4OsLiaNMg M2L4fmROW00EoB?= NV61S2NDUUN3ME2xMlA6KMLzIECuNFEh|ryP MViyN|k2QTR4MB?=
HCT116 NVH4bI94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX63NuKhcMLi M4CxUGROW00EoB?= Mlv4TWM2OD1yLkC0PUDDuSByLkCxN{DPxE1? M4jIXFI{QTV7NE[w
SW1116 NHLQeIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXG3NuKhcMLi NVSyT5RFTE2VT9Mg NUi2dpZmUUN3ME2xMlcxKMLzIECuNFMh|ryP NVPaemc5OjN7NUm0OlA>
WiDr MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[wdplxPzMEoHlCpC=> MmLBSG1UV8Li MlXBTWM2OD1yLkCxPUDDuSByLkCwNkDPxE1? NIHne5kzOzl3OUS2NC=>
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LoVo M{LsXWZ2dmO2aX;uJGF{e2G7 Ml\yNE4xPcLizszN MVu3NuKhcA>? MlzGSG1UV8Li M1TtT4lv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckB1cGViUzDwbIF{\cLi Mmj0NlM6PTl2NkC=
STAV-AB M{e5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DiSVQ5KGh? NWrJZ5dweHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVY1NjUEsUKxMlghLQ>? NWLWUVduOjN6NECzO|Y>
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STAV-FCS MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV20PEBp NIHaXHJxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PFgvOcLzOD65JEU> MmnlNlM5PDB|N{[=
ZL-34 MofLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPCNXA1QCCq NHvQVnBxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PVUvP8LzNj61JEU> M1fiWVI{QDRyM{e2
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BXPC-3 M1z0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnzWmJ7UUN3ME2zPU45PsLzMT62PEDPxE1? M4TlfVIzQTd5NkC3
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PANC-1 Mn;wSpVv[3Srb36gRZN{[Xl? NWHwWYJJQDRizszN M2S0OlI1KGh? MWHlcohidmOnczDFS2ZTNCCKRWKzJIFv\CCDS2SgdIhwe3Cqb4L5cIF1cW:wIHzleoVtew>? MXqyNlk4PzZyNx?=

... Click to View More Cell Line Experimental Data

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]
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  • 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:
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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02357147 Active, not recruiting Mesothelioma, Malignant Morphotek November 4, 2015 Phase 2
NCT02185690 Not yet recruiting Lungcancer University Health Network, Toronto|Novartis Pharmaceuticals March 2017 Phase 1
NCT02964689 Not yet recruiting Advanced Non-small Cell Lung Cancer|KRAS Gene Mutation|Lung Cancer Swiss Group for Clinical Cancer Research March 2017 Phase 1
NCT02998528 Recruiting Non Small Cell Lung Cancer Bristol-Myers Squibb January 2017 Phase 3
NCT03023319 Recruiting Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Nagla Karim|University of Cincinnati January 2017 Phase 1
NCT03003962 Not yet recruiting Non Small Cell Lung Carcinoma (NSCLC) AstraZeneca January 2017 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID