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 17 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 MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2Lo[FEh|ryP NUHPc3JHPDhiaB?= NWTh[mg{\W6qYX7j[ZMhe2mvdnHzeIF1cW5iaX7obYJqfGWmII\pZYJqdGm2eR?= NVvmVGxQOjZ|M{SzNlA>
A549 NF32WlhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEDkcXkyKM7:TR?= NILCbHU1QCCq NUPFTpV[\W6qYX7j[ZMhe2mvdnHzeIF1cW5iaX7obYJqfGWmII\pZYJqdGm2eR?= NFvNSIQzPjN|NEOyNC=>
MSTO-211H NYDuXXRtTnWwY4Tpc44hSXO|YYm= MX:xJO69VQ>? M4SxNlI1KGh? M2Tl[IVvcGGwY3XzJIF2fG:yaHHnfUBkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> NHXMPVYzPjN|NEOyNC=>
A549 NWHFdnA2TnWwY4Tpc44hSXO|YYm= MnLPNUDPxE1? NETpeFMzPCCq MmHY[Y5p[W6lZYOgZZV1d3CqYXf5JINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu MmTDNlY{OzR|MkC=
MSTO-211H M3G0RWFxd3C2b4Ppd{BCe3OjeR?= NEexcmgyKM7:TR?= NFzuXHczPCCq NFjae4FqdmS3Y3XzJIFxd3C2b4Ppd{Bkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> M33kPVI3OzN2M{Kw
A549 M1nYfmFxd3C2b4Ppd{BCe3OjeR?= NYHrfGQ5OSEQvF2= MoHlNlQhcA>? NVmxbZd[cW6mdXPld{BieG:ydH;zbZMh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NH3vbXkzPjN|NEOyNC=>
MSTO-211H MWTGeY5kfGmxbjDBd5NigQ>? M{nQZlEh|ryP MYi0PEBp MkDKbY5kemWjc3XzJGFOWEticHjvd5Bpd3K7bHH0bY9vKGGwZDDhJINwdmOxbXn0ZY51KGSnY4LlZZNmKGmwIFHLWEBidmRibWTPVkBxcG:|cHjvdplt[XSrb36gZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= MYWyOlM{PDN{MB?=
A549 NGLXZoZHfW6ldHnvckBCe3OjeR?= NV7FW5BQOSEQvF2= MYe0PEBp M4\yVYlv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu MlS0NlY{OzR|MkC=
Vero MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nzPFAvOjN2wrDtUS=> NX\FR2hYOjRiaB?= M2GwOYdzd3e2aDDpcohq[mm2aX;uQVXwwap? M3nJZlI2QTd3NkO3
A549 M3HBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPONE4zOzUEoH3N NWfvN3JtOjRiaB?= MkDN[5Jwf3SqIHnubIljcXSrb369NVDwwap? MXOyOVk4PTZ|Nx?=
HeLa NFrnbFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjqVFgxNjJ|NNMgcW0> Mn3sNlQhcA>? NH3YUHloem:5dHigbY5pcWKrdHnvcl0297ns NFPlXlczPTl5NU[zOy=>
T47D NEflNIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHMcVR7OC5{M{VCpI1O MXKyOEBp NETDPJJoem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= M3;0R|I2QTd3NkO3
Vero M4f3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTINE4zOzUEoH3N MYW0PEBp M1z4Uodzd3e2aDDpcohq[mm2aX;uQVEx97ns MmTRNlU6PzV4M{e=
A549 NWq4O4pzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rvXFAvOjN2wrDtUS=> NXftXmx[PDhiaB?= NIXxPWZoem:5dHigbY5pcWKrdHnvcl0{OO,7qh?= MWiyOVk4PTZ|Nx?=
HeLa MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHvNE4zOzUEoH3N NYX1NYhuPDhiaB?= MVLndo94fGhiaX7obYJqfGmxbk2xNQ+6sg>? Mo\lNlU6PzV4M{e=
T47D M2LQUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H1SFAvOjN2wrDtUS=> NV;mSWp{PDhiaB?= MVnndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? M3rz[|I2QTd3NkO3
Vero NFvpTpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMlI{PMLibV2= MUi3NkBp NF3uUFNoem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= MnHJNlU6PzV4M{e=
A549 M{DVVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf4NE4zOzUEoH3N NXHxRpBbPzJiaB?= NELa[2Noem:5dHigbY5pcWKrdHnvcl02OO,7qh?= NEXaV2EzPTl5NU[zOy=>
HeLa Ml;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3RNWIxNjJ|NNMgcW0> NH7KWYg4OiCq NFnBcWNoem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= MY[yOVk4PTZ|Nx?=
T47D M1yzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:1NE4zOzUEoH3N NVHweGNlPzJiaB?= MXvndo94fGhiaX7obYJqfGmxbk2zNQ+6sg>? NEPHSYwzPTl5NU[zOy=>
A459 NUm2VlJQTnWwY4Tpc44hSXO|YYm= NX7tUHRuOS9{L{Sg{txO NXjOb|RbOjRxNEigbC=> MnjybY5lfWOnczDHNUBxcGG|ZTDhdpJme3RiaX6g[I9{\S1iYX7kJJRqdWViZHXw[Y5l\W62IH3hco5meg>? NVSyWmpWOjV5NEO4NlI>
A459 M{PQSWZ2dmO2aX;uJGF{e2G7 MnXaNU8zNzRizszN NFXWfpc1QCCq NUPIe215\GWlcnXhd4V{KHSqZTDs[ZZmdHNib3[gdE1Cc3R? MljyNlU4PDN6MkK=
A459 NUnO[IVnSXCxcITvd4l{KEG|c3H5 M33UWlTPxE1? M4n0PFQ5KGh? M3L6Rolv\HWlZYOgZZBweHSxc3nz MoG2NlU4PDN6MkK=
HepG2 M{jxVmNmdGxiVnnhZoltcXS7IFHzd4F6 M1u4fFAvOeLCk{GwNOKh|ryP M3LtOFczKGh? NYOzdYdkcGmpaDDjc45k\W62cnH0bY9veyCxZjDw[Y1mfHKneHXkJIF1KChzMD:xNFDDqM7:TTmgc45tgSC|bHnnbJRtgSCrbnjpZol1eyCKZYDHNkBk\WyuIIP1dpZqfmGu Mn3qNlU1PDZzMEK=
HepG2 M17xO2Fxd3C2b4Ppd{BCe3OjeR?= MlfTNE4y6oDVMUCwxsDPxE1? NGjBW5g4OiCq NFS2SoNqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfUBifCCqaXfoJINwdmOncn70doF1cW:w Ml71NlU1PDZzMEK=
HepG3 NFHl[5dHfW6ldHnvckBCe3OjeR?= M123SFAvOeLCk{GwNOKh|ryP MV20PEBp NH;GdmFqdmS3Y3XzJJA3OiCmb4fudoVofWyjdHnvckBieyC5ZXzsJIF{KEKnY3zpck0yKGGwZDDMR|NDNUmLIIXwdoVofWyjdHnvci=> M4PaVFI2PDR4MUCy
HepG3 NILabpZHfW6ldHnvckBCe3OjeR?= MWGwMlHjiJNzMEFCpO69VQ>? NIjMXmo1QCCq MX3hZ5RqfmG2ZYOgZ5l1dy2ycn;0[YN1cX[nIHH1eI9xcGGpedMg MoC0NlU1PDZzMEK=
HepG3 NU\ZPFhYTnWwY4Tpc44hSXO|YYm= NG\GXmMyOMLizszN MVW0PEBp MljxeZBz\We3bHH0[ZMheGixc4Doc5J6dGG2ZXSgLJAuMSCPRVuxM|IhMFOnckKxO{8zOjFrIHHu[EBxNUWUS{GvNkApXGi{MkCyM3R6ejJyNDm= NF[yPHUzPTR2NkGwNi=>
U20S MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYGwMlAyNTFyMDFOwG0> M3LP[FczKGh? MUXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4Pl[IVx\W6mZX70cJk> MVyyOVE2OjN7OR?=
MG-63 NV65[ZY1S2WubDDWbYFjcWyrdImgRZN{[Xl? NXz0SmQxOC5yMT2xNFAh|ryP NXnOSWhiPzJiaB?= MVjpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4Pl[IVx\W6mZX70cJk> MknPNlUyPTJ|OUm=
A549 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEi1TWgyNTFyMECgcm0> MnvlO|IhcA>? M4DnZmlEPTB;MUO3JI5O NVToTIJCOjVzNEW2Olk>
H1299 MlLiR4VtdCCYaXHibYxqfHliQYPzZZk> M{DJ[lEuOTByMDDuUS=> MWe3NkBp MnTXTWM2OD1zN{igcm0> MV2yOVE1PTZ4OR?=
MSTO-211 NX25eXl6S2WubDDWbYFjcWyrdImgRZN{[Xl? M{m4cFEh|ryP NVmwR2hbPDhiaB?= MUjwdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv MorZNlUxQTZ7OUO=
A549 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXv2Wm5POSEQvF2= MmHQOFghcA>? NXHqUIJIeHKxZIXj[ZMh[SC|eX7ldodqe3SrYzDpcohq[mm2b4L5JIVn\mWldDDvckB1cGViY3XscEBoem:5dHigZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= MXOyOVA6Pjl7Mx?=
MSTO-211 MWfBdI9xfG:|aYOgRZN{[Xl? MmGzNUDPxE1? NWfnRpZrPDhiaB?= MmOz[Y5p[W6lZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= M3\QfFI2ODl4OUmz
A549 MnnWRZBweHSxc3nzJGF{e2G7 NYLRb5lkOSEQvF2= MkLQOFghcA>? M3HXSIVvcGGwY3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu M3\zdVI2ODl4OUmz
MSTO-211 M{TI[GZ2dmO2aX;uJGF{e2G7 M4jKR|Eh|ryP Ml6xOFghcA>? NYH5[3pN\W6qYX7j[ZMhcW62cnHj[YxtfWyjcjDSU3MheHKxZIXjeIlwdiClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv NF;nXVAzPTB7Nkm5Ny=>
A549 MWLGeY5kfGmxbjDBd5NigQ>? NEfW[JMyKM7:TR?= MY[0PEBp NHL2[YVmdmijbnPld{BqdnS{YXPlcIx2dGG{IGLPV{Bxem:mdXP0bY9vKGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MUKyOVA6Pjl7Mx?=
MSTO-211 MWnGeY5kfGmxbjDBd5NigQ>? MYKxJO69VQ>? M1fRZ|Q5KGh? MWns[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? NED3SZAzPTB7Nkm5Ny=>
A549 Ml\lSpVv[3Srb36gRZN{[Xl? NHP0eYoyKM7:TR?= MVi0PEBp MVPs[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? NHXMS|gzPTB7Nkm5Ny=>
A549  Ml\TSpVv[3Srb36gRZN{[Xl? NUPxRZpGOi53L{WvNVAh|ryP MWO0PEBp M2\h[Ylv[3KnYYPld{BPd3ijIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? Mn75NlQ6QTF5Nki=
H1792 M17ERmZ2dmO2aX;uJGF{e2G7 MlHPNk42NzVxMUCg{txO MnPNOFghcA>? M1jPOolv[3KnYYPld{BPd3ijIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? M2XmOlI1QTlzN{[4
A549  NEXYSHZHfW6ldHnvckBCe3OjeR?= M4\OTFIvPSEQvF2= NEDHTmc1QCCq NF;wZY5qdmS3Y3XzJINie3Cjc3WtPUwh[2G|cHHz[U0{KGGwZDDwc4x6KCiDRGCtdoljd3OnKTDwc4x6dWW{YYPlJEhRSVKSKTDjcIVifmGpZR?= M3;QdlI1QTlzN{[4
H1792 NYLmN4wyTnWwY4Tpc44hSXO|YYm= MYqyMlUh|ryP NUTHepp5PDhiaB?= NXTQSoRGcW6mdXPld{Bk[XOyYYPlMVktKGOjc4Dhd4UuOyCjbnSgdI9tgSBqQVTQMZJq[m:|ZTmgdI9tgW2ncnHz[UApWEGUUDmgZ4xm[X[jZ3W= MmHNNlQ6QTF5Nki=
A549  MYTGeY5kfGmxbjDBd5NigQ>? MlzLNk42NzVxMUCg{txO MWK0PEBp NGr4T|Zld3ewcnXneYxifGW|IF3jcE0yyqB? M3HLb|I1QTlzN{[4
H1792 NIjXToZHfW6ldHnvckBCe3OjeR?= NU\MPFB3Oi53L{WvNVAh|ryP NV3ublc2PDhiaB?= NFW1SlVld3ewcnXneYxifGW|IF3jcE0yyqB? NXLPcVN4OjR7OUG3Olg>
A549 MkfHRZBweHSxc3nzJGF{e2G7 Ml\0Nk42KM7:TR?= M1vZV|Q5KGh? NUnkPXNDcW6mdXPld{BieG:ydH;zbZM> NIjxOlYzPDl7MUe2PC=>
A549 NX3HZXBYTnWwY4Tpc44hSXO|YYm= M1zablUh|ryP MUm4JIg> MWfpcoNz\WG|ZYOgUYNtNTFidXLpdZVqfGmwYYTpc44hdGW4ZXzz M37RdlI1QTlzN{[4
A549 M4i1U2Z2dmO2aX;uJGF{e2G7 MmDRNUDDvU1? M{C4WVQwQC9zMj:yOE81QCCq NI[5No1qdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIDoc5NxcG:{eXzheIVlKEGtdDDpckBiKHSrbXWg[IVx\W6mZX70JI1idm6nch?= NYK0RXgxOjR6NEe4OlM>
A549 MYXGeY5kfGmxbjDBd5NigQ>? Mo\iNE4yNzBwMz:xJO69VQ>? MVq0PEBp NHHSWVRqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIDoc5NxcG:{eXzheIVlKEGtdDDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NVnJdnpyOjR6NEe4OlM>
A549 NUiwUZJHSXCxcITvd4l{KEG|c3H5 M{fXTVAvOS9yLkOvNUDPxE1? M{XXdVQ5KGh? MX7pcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NYLL[3Y4OjR6NEe4OlM>
A549 MXTGeY5kfGmxbjDBd5NigQ>? MnzYNE4yNzBwMz:xJO69VQ>? MmHxOFghcA>? M3;wZ4lv[3KnYYPld{B1cGVicnH0bY8hd2ZiUz3wbIF{\SCyb4D1cIF1cW:w MkLiNlQ5PDd6NkO=
PC9 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYO3NkBp MX3JR|UxRTF4LkC1xtEyNjh3IH7N NHjVXXMzPDh2MEi5NS=>
PC9/GR NYHNbGl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rBcFczKGh? NV7nSIFCUUN3ME20Mlk1yrFyLkS0NEDPxE1? MYeyOFg1ODh7MR?=
PC9 MnT5SpVv[3Srb36gRZN{[Xl? Mmq1NVYhdk1? MV[3NkBp MlrrbY5lfWOnczDTMZBp[XOnIHHydoV{fA>? M3jZc|I1QDRyOEmx
PC9/GR NUixNJcxTnWwY4Tpc44hSXO|YYm= NU[1PJkxPC57NDFOwG0> NIHJPHg4OiCq M2nYV4lv\HWlZYOgV{1xcGG|ZTDhdpJme3R? NHnFXoEzPDh2MEi5NS=>
PC9 MUPBdI9xfG:|aYOgRZN{[Xl? MknpNVYhdk1? NXjsWVFHPzJiaB?= NHHtXoJqdmS3Y3XzJFE1NjV278oqJIFxd3C2b4Ppdy=> Mnf0NlQ5PDB6OUG=
PC9/GR NHruWoxCeG:ydH;zbZMhSXO|YYm= MkLTOE46PCEQvF2= NHnhSoE4OiCq NFrjbmFqdmS3Y3XzJFE6NjV278oqJIFxd3C2b4Ppdy=> MXKyOFg1ODh7MR?=
PC9/GR NWi2XJFCTnWwY4Tpc44hSXO|YYm= NGPDbnQ1Njl2IN88US=> MlHZO|IhcA>? MUnpcoNz\WG|ZYOgdE1GWktibHX2[Yx{ NXjZb4w2OjR6NEC4PVE>
PC9/GR M2fKNmZ2dmO2aX;uJGF{e2G7 MmXNOE46PCEQvF2= NU[ydmZXPzJiaB?= NInXSVdqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy| MVmyOFg1ODh7MR?=
H28 NVft[|dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjETWM2OD1yLkC3xtExNjB{IN88US=> MnfBNlQ4OTR5MkK=
211H NW[ybXV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlGxTWM2OD1yLkC3xtExNjBzIN88US=> M4fJVFI1PzF2N{Ky
H2052 M4DlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M373UGlEPTB;MD61O:KyOC5|NDFOwG0> MX2yOFcyPDd{Mh?=
H2452 NWXK[pNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|Ux97zgMUCwJO69VQ>? MorvNlQ4OTR5MkK=
MES01 NISwfoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDTTWM2OO,:nkGwNEDPxE1? MmLHNlQ4OTR5MkK=
MES04 NV3rVJd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|Ux97zgMUCwJO69VQ>? NXPEWlBrOjR5MUS3NlI>
A549 MkHWR4VtdCCYaXHibYxqfHliQYPzZZk> MUSwMlEwOC5|L{CuOU8yKM7:TR?= MY[yOE81QCCq M2nYfmROW09? M{jDbYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MYeyOFYzPjd{Mh?=
A549 NXjsWZpxTnWwY4Tpc44hSXO|YYm= NXrzOVJ3OC5zL{CuN{8xNjVxMTFOwG0> NUHVPIRqOjRxNEigbC=> NITsOIFFVVOR MXvwdo9lfWOnczD0bIUh\m:{bXH0bY9vKG:oIFHWU5MhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXWyOFYzPjd{Mh?=
H1993 MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvkOIxKSzVyPUCuNVch|ryP NX3rXo1LOjR2MUi1NVk>
H1299 M2D5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jDbmlEPTB;MT64OEDPxE1? MVSyOFQyQDVzOR?=
H226 MknER4VtdCCYaXHibYxqfHliQYPzZZk> NYSxVGc4OS1zMDFOwIcwdWx? NH7PTHA4OiCq NFTyVWZKSzVyPkGwJO69\y:vbB?= NXXHXZdGOjR|N{i1O|Y>
H290 NFjhWFZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1n0elEuOTBizsznM41t NIT5d3I4OiCq MXvJR|UxRjFyIN88[{9udA>? NVX4XWFrOjR|N{i1O|Y>
Y-meso14 MoL3R4VtdCCYaXHibYxqfHliQYPzZZk> NW\ESZpnOS1zMDFOwIcwdWx? NWLhVmxWPzJiaB?= NVribYF6UUN3ME6xNEDPxGdxbXy= M2HTZlI1Ozd6NUe2
MSTO-211H NGSwepFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmHuNU0yOCEQvHevcYw> MmTnO|IhcA>? NVy3OINsUUN3MI6wMlA1KM7:Zz;tcC=> Mn7uNlQ{Pzh3N{[=
A549 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LpVFk3KGh? MV;JR|UxRTFwM{Wg{txO MUeyOFM1QDh3NB?=
A549/PEM-1.6 NUfKW3c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYe5OkBp NXK3doN4UUN3ME21MlA{KM7:TR?= NFO5dVYzPDN2OEi1OC=>
A549/PEM-6.4 NGPqb3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfpPVYhcA>? MWjJR|UxRTJ|LkO5JO69VQ>? M1;1NFI1OzR6OEW0
A549/PEM-16 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrvcmo6PiCq NF;hWXhKSzVyPUWxMlQ2KM7:TR?= NXL1VHhlOjR|NEi4OVQ>
HT-29 NFKzNJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoCxO|LDqGkEoB?= M4XTRWROW00EoB?= MUfJR|UxRTFyLkC3JOKyKDBwOUSg{txO M3n3XFI{QTV7NE[w
LoVo MkjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILybFE4OsLiaNMg M1zjdWROW00EoB?= Ml\UTWM2OD1yLkCzNkDDuSByLkCwNkDPxE1? M{e0elI{QTV7NE[w
SW620 NF3WfpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HFWlczyqCqwrC= MUjEUXNQyqB? MWPJR|UxRTFwMEmgxtEhOC5yMTFOwG0> NEHjXHYzOzl3OUS2NC=>
HCT116 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVy3NuKhcMLi MV7EUXNQyqB? NIGwU|NKSzVyPUCuNFQ6KMLzIECuNFE{KM7:TR?= NFPaUFEzOzl3OUS2NC=>
SW1116 NHzKV4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXy3NuKhcMLi NHvY[pBFVVORwrC= M4ezTmlEPTB;MT63NEDDuSByLkCzJO69VQ>? MWmyN|k2QTR4MB?=
WiDr M3LYd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXG3NuKhcMLi NYrDUW9ZTE2VT9Mg NVHCbJRIUUN3ME2wMlAyQSEEsTCwMlAxOiEQvF2= MnT2NlM6PTl2NkC=
HT-29 MoHnSpVv[3Srb36gRZN{[Xl? MmO1NE4xPcLizszN NXLuTFQyPzMEoHi= M1rPcGROW00EoB?= M1HjS4lv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckB1cGViUzDwbIF{\cLi MnnoNlM6PTl2NkC=
LoVo MnP6SpVv[3Srb36gRZN{[Xl? M3W4OFAvODYEoN88US=> M4nsSFczyqCq NG\Ld|BFVVORwrC= NIjaVlVqdmO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hfGinIGOgdIhie2YEoB?= NYPMUm1lOjN7NUm0OlA>
STAV-AB M3vifGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj3[mg1QCCq MnjzdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PU[0MlTDuTJzLkigKS=> MUKyN|g1ODN5Nh?=
M-14-K NGHRenZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\FcGM1QCCq NUfVU3F5eHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVgyNjkEsUGyMlkhLQ>? M4HEUFI{QDRyM{e2
STAV-FCS NF3DWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LMXFQ5KGh? NEjtV49xem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PFgvOcLzOD65JEU> MXWyN|g1ODN5Nh?=
ZL-34 NWO4Vmx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTrVZVOPDhiaB?= MmOzdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm1MlfDuTZwNTCl MYGyN|g1ODN5Nh?=
JL-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWe0PEBp MmL5dJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm4MlLDuTJwMjCl NV;VfndKOjN6NECzO|Y>
DM-3 NV;je2ZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUm0PEBp NHTGdG1xem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9NVAyNjQEsUKuPEAm NVvFepF[OjN6NECzO|Y>
Jurkat NGLWUHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzpOFghcA>? MlX4dJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUe2MlfDuTRwMzCl MUKyN|g1ODN5Nh?=
BXPC-3 NWrjcYV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGf3[lRKSzVyPUO5Mlg3yrFzLk[4JO69VQ>? MXyyNlk4PzZyNx?=
PANC-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[xOGlEPTB;OEOuO|bDuTBwMUmg{txO M3vFZVIzQTd5NkC3
BXPC-3 NYTvOlg1TnWwY4Tpc44hSXO|YYm= NGe4c|M{QS56NjCg{txO NFz1cHEzPCCq NGPjfXZqdmS3Y3XzJHMh[XK{ZYP0JEhRRDBwMEWpJIFv\CCmZXPy[YF{\XNidHjlJI52dWKncjDv[kBk\WyuczDpckB1cGViR{KvUUBxcGG|ZdMg MV2yNlk4PzZyNx?=
BXPC-3 NYHNfYU5TnWwY4Tpc44hSXO|YYm= MUezPU45PiBizszN NG\3NmEzPCCq M3q5V4VvcGGwY3XzJGVITlJicHjvd5Bpd3K7bHH0[YQhdGW4ZXzzMEBidmRidHjlJJBzd3SnaX6gcIV3\Wy|wrC= Mnr4NlI6Pzd4MEe=
PANC-1 MnPwSpVv[3Srb36gRZN{[Xl? NEjpcHo5PCEQvF2= NWWxSmRSOjRiaB?= NVXEWm1k\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> NUT6e3BnOjJ7N{e2NFc>
BXPC-3 NYnuZmlGTnWwY4Tpc44hSXO|YYm= NF3HTJQ{QS56NjCg{txO NVvFVXFoOjRiaB?= M2nOfoVvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| Ml24NlI6Pzd4MEe=
PANC-1 MkHlSpVv[3Srb36gRZN{[Xl? NFLKcpo5PCEQvF2= MlG1NlQhcA>? M321b4VvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NFTKbmgzOjl5N{[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]
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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]
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  • 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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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

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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

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