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 MmnHR4VtdCCYaXHibYxqfHliQYPzZZk> M1j5SlEh|ryP Moj0OFghcA>? MWPlcohidmOnczDzbY13[XO2YYTpckBqdmirYnn0[YQhfmmjYnnsbZR6 NHPBfYwzPjN|NEOyNC=>
A549 NYTMXZhvS2WubDDWbYFjcWyrdImgRZN{[Xl? NEjUXFcyKM7:TR?= Mme5OFghcA>? MV;lcohidmOnczDzbY13[XO2YYTpckBqdmirYnn0[YQhfmmjYnnsbZR6 M4\4bFI3OzN2M{Kw
MSTO-211H NYjFfFVnTnWwY4Tpc44hSXO|YYm= MVyxJO69VQ>? MYCyOEBp NUnWW3VO\W6qYX7j[ZMh[XW2b4DoZYd6KGOxdILlZZRm\CC5aYToJJNqdX[jc4TheIlv MYGyOlM{PDN{MB?=
A549 NUfkUXExTnWwY4Tpc44hSXO|YYm= NEDjZoYyKM7:TR?= MWiyOEBp NYGxeG9p\W6qYX7j[ZMh[XW2b4DoZYd6KGOxdILlZZRm\CC5aYToJJNqdX[jc4TheIlv MmqxNlY{OzR|MkC=
MSTO-211H M4T3eWFxd3C2b4Ppd{BCe3OjeR?= M{j1R|Eh|ryP M{ftbVI1KGh? M{jBfolv\HWlZYOgZZBweHSxc3nzJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu MXyyOlM{PDN{MB?=
A549 MX3BdI9xfG:|aYOgRZN{[Xl? MmiwNUDPxE1? NHHvUZkzPCCq MWjpcoR2[2W|IHHwc5B1d3OrczDjc5Rz\WG2ZXSge4l1cCC|aX32ZZN1[XSrbh?= M4T4cFI3OzN2M{Kw
MSTO-211H M3TrUmZ2dmO2aX;uJGF{e2G7 NV;xdWRkOSEQvF2= NFO2RZo1QCCq M133XIlv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NFzzXJozPjN|NEOyNC=>
A549 MWPGeY5kfGmxbjDBd5NigQ>? MWmxJO69VQ>? NIXUSnY1QCCq MonIbY5kemWjc3XzJGFOWEticHjvd5Bpd3K7bHH0bY9vKGGwZDDhJINwdmOxbXn0ZY51KGSnY4LlZZNmKGmwIFHLWEBidmRibWTPVkBxcG:|cHjvdplt[XSrb36gZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= M1ftfVI3OzN2M{Kw
Vero Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[yNE4zOzUEoH3N MUmyOEBp NGHjSFVoem:5dHigbY5pcWKrdHnvcl0297ns Mke5NlU6PzV4M{e=
A549 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DaR|AvOjN2wrDtUS=> MlT1NlQhcA>? NWjKUZpz\3Kxd4ToJIlvcGmkaYTpc44:OTExubq= MmjJNlU6PzV4M{e=
HeLa Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPuNE4zOzUEoH3N M1uzblI1KGh? NV3QbFJP\3Kxd4ToJIlvcGmkaYTpc44:Pe,7qh?= NHX2cVYzPTl5NU[zOy=>
T47D M4CyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmwMlI{PMLibV2= NV60VXk3OjRiaB?= M4f6SIdzd3e2aDDpcohq[mm2aX;uQVEx97ns M2\aTFI2QTd3NkO3
Vero M1jtSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjReZYxNjJ|NNMgcW0> NFvXWpk1QCCq M2OycIdzd3e2aDDpcohq[mm2aX;uQVEx97ns MYeyOVk4PTZ|Nx?=
A549 NV;QeW8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSxUI0xNjJ|NNMgcW0> MYK0PEBp NHHuPVloem:5dHigbY5pcWKrdHnvcl0{OO,7qh?= NUTaRlN{OjV7N{W2N|c>
HeLa NXz4TIpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\zWphIOC5{M{VCpI1O MWG0PEBp M13iNIdzd3e2aDDpcohq[mm2aX;uQVEx97ns MWGyOVk4PTZ|Nx?=
T47D NEPlXJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX1NE4zOzUEoH3N NIrZcJo1QCCq NFfpfoRoem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= MW[yOVk4PTZ|Nx?=
Vero M2\3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnwNE4zOzUEoH3N MWC3NkBp NFfXXZdoem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= MorMNlU6PzV4M{e=
A549 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHX[2o5OC5{M{VCpI1O MX63NkBp NV3vTGt1\3Kxd4ToJIlvcGmkaYTpc44:PTExubq= NX;4fZU2OjV7N{W2N|c>
HeLa MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17LW|AvOjN2wrDtUS=> NETP[|E4OiCq NVzyVpBj\3Kxd4ToJIlvcGmkaYTpc44:OjExubq= NXjqeZRFOjV7N{W2N|c>
T47D NYLufJJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jOVlAvOjN2wrDtUS=> MV63NkBp NUHVV2oz\3Kxd4ToJIlvcGmkaYTpc44:OzExubq= MWmyOVk4PTZ|Nx?=
A459 NGn6dpFHfW6ldHnvckBCe3OjeR?= MV[xM|IwPCEQvF2= NH\rTWszPC92ODDo MX;pcoR2[2W|IFexJJBp[XOnIHHydoV{fCCrbjDkc5NmNSCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz NULBNmJUOjV5NEO4NlI>
A459 NGrwWFJHfW6ldHnvckBCe3OjeR?= NXvrSHVJOS9{L{Sg{txO M2jCZ|Q5KGh? NFjue4pl\WO{ZXHz[ZMhfGinIHzleoVteyCxZjDwMWFsfA>? MY[yOVc1Ozh{Mh?=
A459 MWDBdI9xfG:|aYOgRZN{[Xl? NXnvSnV{PM7:TR?= MnrWOFghcA>? NHzlUXJqdmS3Y3XzJIFxd3C2b4Ppdy=> NGPC[GszPTd2M{iyNi=>
HepG2 Mm\LR4VtdCCYaXHibYxqfHliQYPzZZk> M{n4eVAvOeLCk{GwNOKh|ryP MUS3NkBp MXLobYdpKGOxbnPlcpRz[XSrb37zJI9nKHCnbXX0doV5\WRiYYSgLFExNzFyMNMg{txOMSCxbnz5JJNtcWeqdHz5JIlvcGmkaYTzJGhmeEd{IHPlcIwhe3W{dnn2ZYw> MVeyOVQ1PjFyMh?=
HepG2 MoHMRZBweHSxc3nzJGF{e2G7 MVuwMlHjiJNzMEFCpO69VQ>? MnexO|IhcA>? M3PNUolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5JIF1KGirZ3igZ49v[2W{boTyZZRqd25? NHTBToUzPTR2NkGwNi=>
HepG3 MkTsSpVv[3Srb36gRZN{[Xl? MlvCNE4y6oDVMUCwxsDPxE1? MmLsOFghcA>? M4fDWYlv\HWlZYOgdFYzKGSxd37y[Yd2dGG2aX;uJIF{KHenbHygZZMhSmWlbHnuMVEh[W6mIFzDN2IuUUlidYDy[Yd2dGG2aX;u NWC4ZldpOjV2NE[xNFI>
HepG3 NGjtO5dHfW6ldHnvckBCe3OjeR?= NFvQd4ExNjIkgKOxNFDDqM7:TR?= NYXETVQ3PDhiaB?= M2r5T4FkfGm4YYTld{BkgXSxLYDyc5Rm[3SrdnWgZZV1d3CqYXf5xsA> MmHqNlU1PDZzMEK=
HepG3 NYTVR441TnWwY4Tpc44hSXO|YYm= NVLpOoJuOTEEoN88US=> MVi0PEBp MXX1dJJm\3WuYYTld{BxcG:|cHjvdplt[XSnZDCodE0qKE2HS{GvNkApW2W{MkG3M|IzOSliYX7kJJAuTVKNMT:yJEhVcHJ{MEKvWJlzOjB2KR?= M3HOdVI2PDR4MUCy
U20S MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoXNNE4xOS1zMECg{txO MUm3NkBp MYrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4Pl[IVx\W6mZX70cJk> M1m5SVI2OTV{M{m5
MG-63 M2\XfmNmdGxiVnnhZoltcXS7IFHzd4F6 NYnpdpBiOC5yMT2xNFAh|ryP MV63NkBp M1HBRYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Vl\XCnbnTlcpRtgQ>? MX6yOVE2OjN7OR?=
A549 M4TG[mNmdGxiVnnhZoltcXS7IFHzd4F6 MXuxMVExODBibl2= MV63NkBp MV3JR|UxRTF|NzDuUS=> M{P5ZVI2OTR3Nk[5
H1299 M17QW2NmdGxiVnnhZoltcXS7IFHzd4F6 MX6xMVExODBibl2= MVW3NkBp M3HFT2lEPTB;MUe4JI5O M2Cx[FI2OTR3Nk[5
MSTO-211 M3PjZmNmdGxiVnnhZoltcXS7IFHzd4F6 NX7sfI5wOSEQvF2= NIfkSpk1QCCq MYHwdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv M3WwSFI2ODl4OUmz
A549 M{DEfGNmdGxiVnnhZoltcXS7IFHzd4F6 MV[xJO69VQ>? MWq0PEBp NXj4cWNjeHKxZIXj[ZMh[SC|eX7ldodqe3SrYzDpcohq[mm2b4L5JIVn\mWldDDvckB1cGViY3XscEBoem:5dHigZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= MYqyOVA6Pjl7Mx?=
MSTO-211 MkXRRZBweHSxc3nzJGF{e2G7 NVnZXFl5OSEQvF2= NYLrd4VZPDhiaB?= NF3pO5FmdmijbnPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> MX[yOVA6Pjl7Mx?=
A549 NWXFPWhLSXCxcITvd4l{KEG|c3H5 MVuxJO69VQ>? NWXKPFMzPDhiaB?= MXXlcohidmOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= NWG5U5VwOjVyOU[5PVM>
MSTO-211 NWXSSWRzTnWwY4Tpc44hSXO|YYm= M{LyT|Eh|ryP NVPEXmkyPDhiaB?= NY\HRnk2\W6qYX7j[ZMhcW62cnHj[YxtfWyjcjDSU3MheHKxZIXjeIlwdiClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv M1PQXVI2ODl4OUmz
A549 MoH0SpVv[3Srb36gRZN{[Xl? Ml7FNUDPxE1? NXrIbIFbPDhiaB?= MVvlcohidmOnczDpcpRz[WOnbHz1cIFzKFKRUzDwdo9lfWO2aX;uJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= M3:3O|I2ODl4OUmz
MSTO-211 MUnGeY5kfGmxbjDBd5NigQ>? NYDpWm15OSEQvF2= NYfnbZhJPDhiaB?= MY\s[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? MW[yOVA6Pjl7Mx?=
A549 MXzGeY5kfGmxbjDBd5NigQ>? NYjGdItWOSEQvF2= M37ZTlQ5KGh? MX;s[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? M363WVI2ODl4OUmz
A549  NF;ucFJHfW6ldHnvckBCe3OjeR?= M2XFOlIvPS93L{GwJO69VQ>? M4P4RlQ5KGh? MmfYbY5kemWjc3XzJG5wgGFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 M{KzS|I1QTlzN{[4
H1792 NIrsU5BHfW6ldHnvckBCe3OjeR?= MnHkNk42NzVxMUCg{txO Ml7hOFghcA>? NHHRWnVqdmO{ZXHz[ZMhVm:6YTDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? NGDSPIwzPDl7MUe2PC=>
A549  M2rvb2Z2dmO2aX;uJGF{e2G7 MnT4Nk42KM7:TR?= NYTSVFdyPDhiaB?= MkDUbY5lfWOnczDjZZNx[XOnLUmsJINie3Cjc3WtN{BidmRicH;sfUApSUSSLYLpZo9{\SlicH;sfY1memG|ZTCoVGFTWCliY3zlZZZi\2V? NV7uSFlzOjR7OUG3Olg>
H1792 NHixUZZHfW6ldHnvckBCe3OjeR?= NF7t[I4zNjVizszN MmrqOFghcA>? NVHYR|hscW6mdXPld{Bk[XOyYYPlMVktKGOjc4Dhd4UuOyCjbnSgdI9tgSBqQVTQMZJq[m:|ZTmgdI9tgW2ncnHz[UApWEGUUDmgZ4xm[X[jZ3W= M4TxO|I1QTlzN{[4
A549  NIr4VFNHfW6ldHnvckBCe3OjeR?= MVGyMlUwPS9zMDFOwG0> NXjuRmtIPDhiaB?= MmG4[I94dnKnZ4XsZZRmeyCPY3ytNeKh MYKyOFk6OTd4OB?=
H1792 NXvkTodjTnWwY4Tpc44hSXO|YYm= MXWyMlUwPS9zMDFOwG0> MUC0PEBp MlPo[I94dnKnZ4XsZZRmeyCPY3ytNeKh NXXiT3VbOjR7OUG3Olg>
A549 MWnBdI9xfG:|aYOgRZN{[Xl? NF3HUXEzNjVizszN M1[1dFQ5KGh? NXHhRpZ[cW6mdXPld{BieG:ydH;zbZM> MUiyOFk6OTd4OB?=
A549 NXvi[|h3TnWwY4Tpc44hSXO|YYm= M4fiSVUh|ryP M176fFghcA>? MmHqbY5kemWjc3XzJG1kdC1zIIXibZF2cXSrbnH0bY9vKGyndnXsdy=> MYOyOFk6OTd4OB?=
A549 MULGeY5kfGmxbjDBd5NigQ>? M3HtRVEhyrWP M4PXO|QwQC9zMj:yOE81QCCq MnHTbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyaH;zdIhwenmuYYTl[EBCc3RiaX6gZUB1cW2nIHTldIVv\GWwdDDtZY5v\XJ? M{\tUVI1QDR5OE[z
A549 MWXGeY5kfGmxbjDBd5NigQ>? Mn;YNE4yNzBwMz:xJO69VQ>? M2fQbFQ5KGh? M4DSVIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicHjvd5Bpd3K7bHH0[YQhSWu2IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MnW4NlQ5PDd6NkO=
A549 NYHkc|FmSXCxcITvd4l{KEG|c3H5 NGP3PYgxNjFxMD6zM|Eh|ryP M4nhWFQ5KGh? NVXFXVh6cW6mdXPld{BieG:ydH;zbZMhcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MlzWNlQ5PDd6NkO=
A549 NV72bHpJTnWwY4Tpc44hSXO|YYm= Mlv5NE4yNzBwMz:xJO69VQ>? M{PLcVQ5KGh? MmjVbY5kemWjc3XzJJRp\SC{YYTpc{Bw\iCVLYDoZZNmKHCxcIXsZZRqd25? MYOyOFg1Pzh4Mx?=
PC9 NHz0c3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn2OYk4OiCq M4jGd2lEPTB;MU[uNFXDuTFwOEWgcm0> NF7JRYEzPDh2MEi5NS=>
PC9/GR NXTzZlRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWe3NkBp NEjzNlZKSzVyPUSuPVTDuTBwNESwJO69VQ>? NIGxWnYzPDh2MEi5NS=>
PC9 NGLGWlNHfW6ldHnvckBCe3OjeR?= NH;BeFIyPiCwTR?= M2jvN|czKGh? M{nPfIlv\HWlZYOgV{1xcGG|ZTDhdpJme3R? MVqyOFg1ODh7MR?=
PC9/GR NYPFRVQ{TnWwY4Tpc44hSXO|YYm= MXu0Mlk1KM7:TR?= Ml\0O|IhcA>? NVHUWIFtcW6mdXPld{BUNXCqYYPlJIFzemW|dB?= Ml;SNlQ5PDB6OUG=
PC9 NWTQNnFGSXCxcITvd4l{KEG|c3H5 M1rCfFE3KG6P MnG2O|IhcA>? MlH5bY5lfWOnczCxOE42PO,7qjDhdI9xfG:|aYO= Moi1NlQ5PDB6OUG=
PC9/GR Ml;NRZBweHSxc3nzJGF{e2G7 MoLwOE46PCEQvF2= MlLSO|IhcA>? NWnJXmZqcW6mdXPld{AyQS53NP-5rkBieG:ydH;zbZM> MVeyOFg1ODh7MR?=
PC9/GR NXe2V|NlTnWwY4Tpc44hSXO|YYm= NXnVb2xFPC57NDFOwG0> MmCzO|IhcA>? MVfpcoNz\WG|ZYOgdE1GWktibHX2[Yx{ M3\tTlI1QDRyOEmx
PC9/GR NYXKWHBWTnWwY4Tpc44hSXO|YYm= NXO2VFhHPC57NDFOwG0> NYS4dYw2PzJiaB?= NVzjO3F4cW6lcnXhd4V{KHBvQVvUJIxmfmWucx?= MoDWNlQ5PDB6OUG=
H28 Mmj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwMEhCtVAvODJizszN NH;lVoMzPDdzNEeyNi=>
211H Mm\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvITWM2OD1yLkC3xtExNjBzIN88US=> Mn7LNlQ4OTR5MkK=
H2052 NEftTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrNTWM2OD1yLkW3xtExNjN2IN88US=> M4S1SlI1PzF2N{Ky
H2452 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|Ux97zgMUCwJO69VQ>? Mm\yNlQ4OTR5MkK=
MES01 M3TkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXGb5REUUN3MP-8olExOCEQvF2= MWCyOFcyPDd{Mh?=
MES04 NWL0fo44T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|Ux97zgMUCwJO69VQ>? M{nZdFI1PzF2N{Ky
A549 NIPjdnpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUSwMlEwOC5|L{CuOU8yKM7:TR?= MmLMNlQwPDhiaB?= NX\pOXJbTE2VTx?= Ml7KbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NVfTOXc5OjR4Mk[3NlI>
A549 MXPGeY5kfGmxbjDBd5NigQ>? MkDTNE4yNzBwMz:wMlUwOSEQvF2= M{\3Z|I1NzR6IHi= MlL6SG1UVw>? M1vJRZBzd2S3Y3XzJJRp\SCob4LtZZRqd25ib3[gRXZQeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlH4NlQ3OjZ5MkK=
H1993 M4LxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzO[ZRqUUN3ME2wMlE4KM7:TR?= MX[yOFQyQDVzOR?=
H1299 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q2dGlEPTB;MT64OEDPxE1? MkDRNlQ1OTh3MUm=
H226 NXn2bZBuS2WubDDWbYFjcWyrdImgRZN{[Xl? M{HS[FEuOTBizsznM41t NEfsUI04OiCq NYDQOFY1UUN3ME6xNEDPxGdxbXy= NHrDcnMzPDN5OEW3Oi=>
H290 M2ftPWNmdGxiVnnhZoltcXS7IFHzd4F6 NILa[mIyNTFyIN88[{9udA>? NHXSVpY4OiCq MV3JR|UxRjFyIN88[{9udA>? NUT5VVB5OjR|N{i1O|Y>
Y-meso14 Mo\RR4VtdCCYaXHibYxqfHliQYPzZZk> MYWxMVExKM7:Zz;tcC=> NX31NlBWPzJiaB?= NWPQdHBuUUN3ME6xNEDPxGdxbXy= NFvjb2kzPDN5OEW3Oi=>
MSTO-211H M2jpbGNmdGxiVnnhZoltcXS7IFHzd4F6 NXvtd45WOS1zMDFOwIcwdWx? M4TZeFczKGh? NX7ZPIQyUUN3MI6wMlA1KM7:Zz;tcC=> Moe5NlQ{Pzh3N{[=
A549 NH;4bWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C4Tlk3KGh? M3fsd2lEPTB;MT6zOUDPxE1? NWrLblNkOjR|NEi4OVQ>
A549/PEM-1.6 NW[2eGQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HoUFk3KGh? NWDkPFBNUUN3ME21MlA{KM7:TR?= MknsNlQ{PDh6NUS=
A549/PEM-6.4 NF[4W2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3izXlk3KGh? NG[0PYxKSzVyPUKzMlM6KM7:TR?= M3TxVlI1OzR6OEW0
A549/PEM-16 NFfKOlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX25OkBp MlfUTWM2OD13MT60OUDPxE1? NGnuRWwzPDN2OEi1OC=>
HT-29 M3S5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnBWlA4OsLiaNMg M3OwW2ROW00EoB?= NV21b25ZUUN3ME2xNE4xPyEEsTCwMlk1KM7:TR?= NY\Re|YyOjN7NUm0OlA>
LoVo Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHNPXY4OsLiaNMg M1XHS2ROW00EoB?= MmTQTWM2OD1yLkCzNkDDuSByLkCwNkDPxE1? NVGwcGg{OjN7NUm0OlA>
SW620 NYezTmxVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXuVGlTPzMEoHlCpC=> NEf2WmdFVVORwrC= M3j5OWlEPTB;MT6wPUDDuSByLkCxJO69VQ>? NYLre2dIOjN7NUm0OlA>
HCT116 NGLKcGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fTbFczyqCqwrC= NWrRRXZCTE2VT9Mg NWT0fIR[UUN3ME2wMlA1QSEEsTCwMlAyOyEQvF2= MYCyN|k2QTR4MB?=
SW1116 NIDGXmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPCO|LDqGkEoB?= MWPEUXNQyqB? NFL4flhKSzVyPUGuO|AhyrFiMD6wN{DPxE1? M4Psc|I{QTV7NE[w
WiDr NYLZeHJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jRTFczyqCqwrC= NVHE[GRTTE2VT9Mg MXPJR|UxRTBwMEG5JOKyKDBwMECyJO69VQ>? NYP5UJNTOjN7NUm0OlA>
HT-29 MUjGeY5kfGmxbjDBd5NigQ>? NHP2cVcxNjB3wrFOwG0> MYO3NuKhcA>? M1HDXGROW00EoB?= MVfpcoNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6geIhmKFNicHjhd4XDqA>? NVuyWpZGOjN7NUm0OlA>
LoVo MlmxSpVv[3Srb36gRZN{[Xl? MV:wMlA2yqEQvF2= NF\Rbpk4OsLiaB?= M1PIVmROW00EoB?= NW\oUoo5cW6lcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKHSqZTDTJJBp[XOnwrC= M1fUbFI{QTV7NE[w
STAV-AB MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFKySlk1QCCq MlTsdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PU[0MlTDuTJzLkigKS=> M1npdlI{QDRyM{e2
M-14-K NGTFcppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPMVmZ2PDhiaB?= NVnBfpBqeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVgyNjkEsUGyMlkhLQ>? MkjkNlM5PDB|N{[=
STAV-FCS NHXUOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm0PEBp MkDNdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUi4MlHDuThwOTCl NXy5UWhkOjN6NECzO|Y>
ZL-34 M3;4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXq[2Q5PDhiaB?= MXzwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OUWuO:KyPi53IDW= M3nIZlI{QDRyM{e2
JL-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnyyOFghcA>? MV7wdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OUiuNuKyOi5{IDW= NXzvbG03OjN6NECzO|Y>
DM-3 NEHuSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXG0PEBp NFPU[Y1xem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9NVAyNjQEsUKuPEAm NFS1N3czOzh2MEO3Oi=>
Jurkat NULMS|h3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\1W3Y6PDhiaB?= M1nteJBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{23Ok44yrF2LkOgKS=> NE[0V|gzOzh2MEO3Oi=>
BXPC-3 M1fBPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTN7Lki2xtEyNjZ6IN88US=> NX\EbWJLOjJ7N{e2NFc>
PANC-1 NVrYWJRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHeyZ45KSzVyPUizMlc3yrFyLkG5JO69VQ>? MVqyNlk4PzZyNx?=
BXPC-3 M1rLdGZ2dmO2aX;uJGF{e2G7 NG[yO4E{QS56NjCg{txO M4TRdlI1KGh? NH;VTXdqdmS3Y3XzJHMh[XK{ZYP0JEhRRDBwMEWpJIFv\CCmZXPy[YF{\XNidHjlJI52dWKncjDv[kBk\WyuczDpckB1cGViR{KvUUBxcGG|ZdMg M3nufVIzQTd5NkC3
BXPC-3 NVLEb3J2TnWwY4Tpc44hSXO|YYm= MWqzPU45PiBizszN MUeyOEBp NX;YNWN7\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> Mn;pNlI6Pzd4MEe=
PANC-1 NIHiRYlHfW6ldHnvckBCe3OjeR?= M3W5eVg1KM7:TR?= NI\POpkzPCCq Ml;R[Y5p[W6lZYOgSWdHWiCyaH;zdIhwenmuYYTl[EBt\X[nbIOsJIFv\CC2aHWgdJJwfGWrbjDs[ZZmdHQEoB?= NHfKUVAzOjl5N{[wOy=>
BXPC-3 MYnGeY5kfGmxbjDBd5NigQ>? NES3TIU{QS56NjCg{txO M13tR|I1KGh? MmTj[Y5p[W6lZYOgSWdHWixiSFXSN{BidmRiQVvUJJBpd3OyaH;yfYxifGmxbjDs[ZZmdHN? MUWyNlk4PzZyNx?=
PANC-1 MUXGeY5kfGmxbjDBd5NigQ>? NULGbXczQDRizszN Mln5NlQhcA>? MV\lcohidmOnczDFS2ZTNCCKRWKzJIFv\CCDS2SgdIhwe3Cqb4L5cIF1cW:wIHzleoVtew>? NV73Zop7OjJ7N{e2NFc>

... 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
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