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 NHTsdoRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHfm[JEyKM7:TR?= M1PWTlQ5KGh? NEnZWpFmdmijbnPld{B{cW24YYP0ZZRqdiCrbnjpZol1\WRidnnhZoltcXS7 NU\mfI9rOjZ|M{SzNlA>
A549 M2\FVmNmdGxiVnnhZoltcXS7IFHzd4F6 M3PkWlEh|ryP NHjHNYU1QCCq M3XVOoVvcGGwY3XzJJNqdX[jc4TheIlvKGmwaHnibZRm\CC4aXHibYxqfHl? MoW4NlY{OzR|MkC=
MSTO-211H MnTiSpVv[3Srb36gRZN{[Xl? M{HObVEh|ryP NVrWUXFUOjRiaB?= NHTMOnpmdmijbnPld{BifXSxcHjh[5kh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> M17lb|I3OzN2M{Kw
A549 NEfm[JJHfW6ldHnvckBCe3OjeR?= MkTaNUDPxE1? NWDq[pBEOjRiaB?= NGO4e|dmdmijbnPld{BifXSxcHjh[5kh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NIDiWZYzPjN|NEOyNC=>
MSTO-211H M3;XT2Fxd3C2b4Ppd{BCe3OjeR?= MXuxJO69VQ>? NHrYRWszPCCq MlvIbY5lfWOnczDhdI9xfG:|aYOgZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= M2DkeVI3OzN2M{Kw
A549 NUn4[HFNSXCxcITvd4l{KEG|c3H5 M37tOlEh|ryP M3GwcFI1KGh? NWjMN4xkcW6mdXPld{BieG:ydH;zbZMh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> MXWyOlM{PDN{MB?=
MSTO-211H MVPGeY5kfGmxbjDBd5NigQ>? NUGxT2dyOSEQvF2= M3HiWFQ5KGh? M3n0SYlv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NXvLU2YxOjZ|M{SzNlA>
A549 NFjKUIFHfW6ldHnvckBCe3OjeR?= M3HodlEh|ryP NUTYNYp[PDhiaB?= M{m0b4lv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NFrOco4zPjN|NEOyNC=>
Vero MoK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\FNE4zOzUEoH3N MX6yOEBp MkXo[5Jwf3SqIHnubIljcXSrb369Og+6sg>? NV;6TlljOjV7N{W2N|c>
A549 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmwMlI{PMLibV2= NEXMPWYzPCCq MYHndo94fGhiaX7obYJqfGmxbk2xNQ+6sg>? MlG5NlU6PzV4M{e=
HeLa MoXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLpSYZjOC5{M{VCpI1O NI\6cHYzPCCq M2THZ4dzd3e2aDDpcohq[mm2aX;uQVXwwap? MnfsNlU6PzV4M{e=
T47D NEn1bWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXQNE4zOzUEoH3N NFHXTVEzPCCq NGX4b3Boem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= MXqyOVk4PTZ|Nx?=
Vero NFvWXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH2[GUxNjJ|NNMgcW0> NG\BUW41QCCq M1L1NYdzd3e2aDDpcohq[mm2aX;uQVEx97ns M3vWWlI2QTd3NkO3
A549 NGHwZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHh[o9{OC5{M{VCpI1O NV7VdWJzPDhiaB?= NH3RTXRoem:5dHigbY5pcWKrdHnvcl0{OO,7qh?= MVeyOVk4PTZ|Nx?=
HeLa NYSwfpJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KzcFAvOjN2wrDtUS=> NVu5[nJiPDhiaB?= M2HrR4dzd3e2aDDpcohq[mm2aX;uQVEx97ns Ml31NlU6PzV4M{e=
T47D NXHPW|I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PXUFAvOjN2wrDtUS=> MYq0PEBp NIjifpRoem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= NXr2eZc3OjV7N{W2N|c>
Vero MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDB[llQOC5{M{VCpI1O M4XFNFczKGh? M1\Bdodzd3e2aDDpcohq[mm2aX;uQVIx97ns M1i4O|I2QTd3NkO3
A549 NY\JUXNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV6zU2ZMOC5{M{VCpI1O MlPFO|IhcA>? NX\FOI8y\3Kxd4ToJIlvcGmkaYTpc44:PTExubq= MVGyOVk4PTZ|Nx?=
HeLa NUn5RnB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3RNE4zOzUEoH3N NGLt[3M4OiCq NWnNVWY{\3Kxd4ToJIlvcGmkaYTpc44:OjExubq= NH7lXJQzPTl5NU[zOy=>
T47D M3fY[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7mNE4zOzUEoH3N NIHIe|A4OiCq M1XHXodzd3e2aDDpcohq[mm2aX;uQVMx97ns M1i2TlI2QTd3NkO3
A459 NVPFelBuTnWwY4Tpc44hSXO|YYm= M1fhZ|EwOi92IN88US=> M{D4ZlI1NzR6IHi= MV;pcoR2[2W|IFexJJBp[XOnIHHydoV{fCCrbjDkc5NmNSCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz NGf4RlgzPTd2M{iyNi=>
A459 NGLr[nBHfW6ldHnvckBCe3OjeR?= MVixM|IwPCEQvF2= NIL3WWE1QCCq MVfk[YNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyLVHreC=> NWT3U2dLOjV5NEO4NlI>
A459 MkHZRZBweHSxc3nzJGF{e2G7 MYW0{txO M3H5fFQ5KGh? M4Hod4lv\HWlZYOgZZBweHSxc3nz MkeyNlU4PDN6MkK=
HepG2 MofMR4VtdCCYaXHibYxqfHliQYPzZZk> MoDINE4y6oDVMUCwxsDPxE1? NUTvUm4xPzJiaB?= MUPobYdpKGOxbnPlcpRz[XSrb37zJI9nKHCnbXX0doV5\WRiYYSgLFExNzFyMNMg{txOMSCxbnz5JJNtcWeqdHz5JIlvcGmkaYTzJGhmeEd{IHPlcIwhe3W{dnn2ZYw> NXzOcoFSOjV2NE[xNFI>
HepG2 NIP2b5VCeG:ydH;zbZMhSXO|YYm= MXWwMlHjiJNzMEFCpO69VQ>? M4jQNVczKGh? NHXpb41qdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfUBifCCqaXfoJINwdmOncn70doF1cW:w MmDZNlU1PDZzMEK=
HepG3 NXG4elQ5TnWwY4Tpc44hSXO|YYm= MmrHNE4y6oDVMUCwxsDPxE1? M1q2e|Q5KGh? M4\1Uolv\HWlZYOgdFYzKGSxd37y[Yd2dGG2aX;uJIF{KHenbHygZZMhSmWlbHnuMVEh[W6mIFzDN2IuUUlidYDy[Yd2dGG2aX;u NWrBfnZ{OjV2NE[xNFI>
HepG3 NYnwR5BETnWwY4Tpc44hSXO|YYm= M1\IcFAvOeLCk{GwNOKh|ryP MlHGOFghcA>? NEi2WIdi[3SrdnH0[ZMh[3m2bz3wdo91\WO2aY\lJIF2fG:yaHHnfeKh M{XUVFI2PDR4MUCy
HepG3 NW\MXWxbTnWwY4Tpc44hSXO|YYm= M3vYOFExyqEQvF2= MX20PEBp MlLmeZBz\We3bHH0[ZMheGixc4Doc5J6dGG2ZXSgLJAuMSCPRVuxM|IhMFOnckKxO{8zOjFrIHHu[EBxNUWUS{GvNkApXGi{MkCyM3R6ejJyNDm= MVOyOVQ1PjFyMh?=
U20S NVv2SYN[S2WubDDWbYFjcWyrdImgRZN{[Xl? NFjteY0xNjBzLUGwNEDPxE1? NVm1cJZtPzJiaB?= M{XJN4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Vl\XCnbnTlcpRtgQ>? NXzYNW8{OjVzNUKzPVk>
MG-63 MlTlR4VtdCCYaXHibYxqfHliQYPzZZk> MmLPNE4xOS1zMECg{txO MmPFO|IhcA>? NFHl[2NqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5Nm\GWyZX7k[Y51dHl? M1zUR|I2OTV{M{m5
A549 NHzvZ5lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnLENU0yODByIH7N M1nYXVczKGh? MkfQTWM2OD1zM{egcm0> NYK5elNLOjVzNEW2Olk>
H1299 M1Tr[GNmdGxiVnnhZoltcXS7IFHzd4F6 NET2VHEyNTFyMECgcm0> NUDLUphNPzJiaB?= NXPiWHYxUUN3ME2xO|ghdk1? M3fjPVI2OTR3Nk[5
MSTO-211 NInkfmRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGeyOXIyKM7:TR?= M1PTcVQ5KGh? MmXvdJJw\HWlZYOgZUB{gW6ncnfpd5Rq[yCrbnjpZol1d3K7IHXm[oVkfCCxbjD0bIUh[2WubDDndo94fGhiY3;tZolv\WRid3n0bEB{cW24YYP0ZZRqdg>? MYGyOVA6Pjl7Mx?=
A549 NXu4TGRDS2WubDDWbYFjcWyrdImgRZN{[Xl? MX:xJO69VQ>? MoT4OFghcA>? MVLwdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv NYfq[IFMOjVyOU[5PVM>
MSTO-211 NX35Tm1oSXCxcITvd4l{KEG|c3H5 NFTrbnkyKM7:TR?= MortOFghcA>? NXfLR3lV\W6qYX7j[ZMh[2G|cHHz[U1l\XCnbnTlcpQh[XCxcITvd4l{KGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MlfwNlUxQTZ7OUO=
A549 NX3zNpJMSXCxcITvd4l{KEG|c3H5 MXexJO69VQ>? NH;0fWs1QCCq M3PxfIVvcGGwY3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu NEfNWY8zPTB7Nkm5Ny=>
MSTO-211 MVnGeY5kfGmxbjDBd5NigQ>? Mnm4NUDPxE1? MoSzOFghcA>? NF24ZnBmdmijbnPld{BqdnS{YXPlcIx2dGG{IGLPV{Bxem:mdXP0bY9vKGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MoHXNlUxQTZ7OUO=
A549 NIDVZlZHfW6ldHnvckBCe3OjeR?= MXGxJO69VQ>? Mk\YOFghcA>? M1ztb4VvcGGwY3XzJIlvfHKjY3XscJVt[XJiUl;TJJBzd2S3Y4Tpc44h[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> NGDDRlAzPTB7Nkm5Ny=>
MSTO-211 MmDNSpVv[3Srb36gRZN{[Xl? NYf5XWZ3OSEQvF2= MnnuOFghcA>? MVHs[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? Mmn2NlUxQTZ7OUO=
A549 MVHGeY5kfGmxbjDBd5NigQ>? NVfMXHNxOSEQvF2= MorGOFghcA>? NInqbWVt\WGmczD0c{BucXSxY3jvcoRzcWGuIHT5d4Z2dmO2aX;uJINwdWKrbnXkJJdqfGhic3nteoF{fGG2aX6= MWCyOVA6Pjl7Mx?=
A549  NXflXZJ{TnWwY4Tpc44hSXO|YYm= NVPl[nR[Oi53L{WvNVAh|ryP NG[2[Jk1QCCq MXHpcoNz\WG|ZYOgUo95[SCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> NYC2WZNoOjR7OUG3Olg>
H1792 MWHGeY5kfGmxbjDBd5NigQ>? NUHFOpBkOi53L{WvNVAh|ryP MVy0PEBp MWfpcoNz\WG|ZYOgUo95[SCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> NVjJ[W9QOjR7OUG3Olg>
A549  Mn\0SpVv[3Srb36gRZN{[Xl? MlnTNk42KM7:TR?= Mn[0OFghcA>? M{jsdolv\HWlZYOgZ4F{eGG|ZT25MEBk[XOyYYPlMVMh[W6mIIDvcJkhMEGGUD3ybYJwe2VrIIDvcJlu\XKjc3WgLHBCWlBrIHPs[YF3[Wen MU[yOFk6OTd4OB?=
H1792 MU\GeY5kfGmxbjDBd5NigQ>? M1rzXVIvPSEQvF2= NHTQUW01QCCq MmnhbY5lfWOnczDjZZNx[XOnLUmsJINie3Cjc3WtN{BidmRicH;sfUApSUSSLYLpZo9{\SlicH;sfY1memG|ZTCoVGFTWCliY3zlZZZi\2V? NFLSVGczPDl7MUe2PC=>
A549  MYrGeY5kfGmxbjDBd5NigQ>? NY\QcmZEOi53L{WvNVAh|ryP NG\NcFQ1QCCq Mn\N[I94dnKnZ4XsZZRmeyCPY3ytNeKh M{LKTFI1QTlzN{[4
H1792 M{npVGZ2dmO2aX;uJGF{e2G7 NETRVY8zNjVxNT:xNEDPxE1? NWjmbVQzPDhiaB?= NHvwU3Fld3ewcnXneYxifGW|IF3jcE0yyqB? Mlq4NlQ6QTF5Nki=
A549 NInvXphCeG:ydH;zbZMhSXO|YYm= MYOyMlUh|ryP NEjUcFM1QCCq MV3pcoR2[2W|IHHwc5B1d3Orcx?= MXuyOFk6OTd4OB?=
A549 MmXzSpVv[3Srb36gRZN{[Xl? NES4cng2KM7:TR?= MUm4JIg> MV3pcoNz\WG|ZYOgUYNtNTFidXLpdZVqfGmwYYTpc44hdGW4ZXzz MnHrNlQ6QTF5Nki=
A549 MVXGeY5kfGmxbjDBd5NigQ>? NVzlcnE6OSEEtV2= MkW4OE85NzF{L{K0M|Q5KGh? NHP6PJlqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIDoc5NxcG:{eXzheIVlKEGtdDDpckBiKHSrbXWg[IVx\W6mZX70JI1idm6nch?= MUiyOFg1Pzh4Mx?=
A549 NX3rZ3h{TnWwY4Tpc44hSXO|YYm= MV:wMlEwOC5|L{Gg{txO Ml\QOFghcA>? M3fjdYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicHjvd5Bpd3K7bHH0[YQhSWu2IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NEXWVpkzPDh2N{i2Ny=>
A549 MWLBdI9xfG:|aYOgRZN{[Xl? NVq4WpRUOC5zL{CuN{8yKM7:TR?= NEXLbIg1QCCq NVe5VVdncW6mdXPld{BieG:ydH;zbZMhcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M4f4SFI1QDR5OE[z
A549 NFn0R5NHfW6ldHnvckBCe3OjeR?= NGTX[XIxNjFxMD6zM|Eh|ryP NYDXfm1uPDhiaB?= M4TwNIlv[3KnYYPld{B1cGVicnH0bY8hd2ZiUz3wbIF{\SCyb4D1cIF1cW:w NHLGPWszPDh2N{i2Ny=>
PC9 M2fZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;WUlczKGh? NV\0XXhQUUN3ME2xOk4xPcLzMT64OUBvVQ>? MVmyOFg1ODh7MR?=
PC9/GR MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\Pc3YyPzJiaB?= NFPoVIhKSzVyPUSuPVTDuTBwNESwJO69VQ>? NYrW[pI5OjR6NEC4PVE>
PC9 MVLGeY5kfGmxbjDBd5NigQ>? NG[4fYoyPiCwTR?= NX21fIVSPzJiaB?= NW\mSXhXcW6mdXPld{BUNXCqYYPlJIFzemW|dB?= MWCyOFg1ODh7MR?=
PC9/GR M4r3V2Z2dmO2aX;uJGF{e2G7 NH7KfFc1Njl2IN88US=> M2j0OlczKGh? MkiwbY5lfWOnczDTMZBp[XOnIHHydoV{fA>? MljnNlQ5PDB6OUG=
PC9 MnnlRZBweHSxc3nzJGF{e2G7 M32yPFE3KG6P MXi3NkBp NFzz[nFqdmS3Y3XzJFE1NjV278oqJIFxd3C2b4Ppdy=> Mn3lNlQ5PDB6OUG=
PC9/GR MluzRZBweHSxc3nzJGF{e2G7 M1XCO|QvQTRizszN Mn3vO|IhcA>? M3PJ[Ilv\HWlZYOgNVkvPTUxubqgZZBweHSxc3nz MYWyOFg1ODh7MR?=
PC9/GR MYHGeY5kfGmxbjDBd5NigQ>? NUjLW2xkPC57NDFOwG0> MlX3O|IhcA>? NGPQNo1qdmO{ZXHz[ZMheC2HUlugcIV3\Wy| NEjvfmgzPDh2MEi5NS=>
PC9/GR NXvnS|dFTnWwY4Tpc44hSXO|YYm= NV;TSW56PC57NDFOwG0> NWDBb446PzJiaB?= MnTJbY5kemWjc3XzJJAuSUuWIHzleoVtew>? MWGyOFg1ODh7MR?=
H28 NUDGU5E4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUexWHY2UUN3ME2wMlA4yrFyLkCyJO69VQ>? NV7WfGU5OjR5MUS3NlI>
211H NGH1R4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMEhCtVAvODFizszN Mnf1NlQ4OTR5MkK=
H2052 M4LpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTBwNUhCtVAvOzRizszN M4qxT|I1PzF2N{Ky
H2452 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|Ux97zgMUCwJO69VQ>? NHP4fZAzPDdzNEeyNi=>
MES01 NXzCUFZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfHTWM2OO,:nkGwNEDPxE1? MWSyOFcyPDd{Mh?=
MES04 NF[2W4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoroTWM2OO,:nkGwNEDPxE1? NHzYNIMzPDdzNEeyNi=>
A549 Mn7xR4VtdCCYaXHibYxqfHliQYPzZZk> NVfxUGt6OC5zL{CuN{8xNjVxMTFOwG0> M2\6[lI1NzR6IHi= M1v3TGROW09? MoDwbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MVKyOFYzPjd{Mh?=
A549 NYfHXJZXTnWwY4Tpc44hSXO|YYm= NYLEcIdCOC5zL{CuN{8xNjVxMTFOwG0> M3jBblI1NzR6IHi= NGL1RW9FVVOR MnrwdJJw\HWlZYOgeIhmKG[xcn3heIlwdiCxZjDBWm9{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVjV[XRiOjR4Mk[3NlI>
H1993 M2nlXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHrSpZNUUN3ME2wMlE4KM7:TR?= MmXLNlQ1OTh3MUm=
H1299 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml21TWM2OD1zLki0JO69VQ>? NInrdJMzPDRzOEWxPS=>
H226 M3XMemNmdGxiVnnhZoltcXS7IFHzd4F6 M2fGOlEuOTBizsznM41t MWO3NkBp M1\x[WlEPTB-MUCg{txoN22u MWmyOFM4QDV5Nh?=
H290 NVywOoVbS2WubDDWbYFjcWyrdImgRZN{[Xl? M3fTeVEuOTBizsznM41t M4rIOlczKGh? NV\FVmVyUUN3ME6xNEDPxGdxbXy= NFzMXZkzPDN5OEW3Oi=>
Y-meso14 NHvKcYdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmjCNU0yOCEQvHevcYw> MYm3NkBp NHHoTmRKSzVyPkGwJO69\y:vbB?= MXyyOFM4QDV5Nh?=
MSTO-211H NHqxeFFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{LSW|EuOTBizsznM41t M{nCZVczKGh? MnP4TWM2OH5yLkC0JO69\y:vbB?= MlfqNlQ{Pzh3N{[=
A549 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXq5OkBp NFfQWoNKSzVyPUGuN|Uh|ryP NITS[FgzPDN2OEi1OC=>
A549/PEM-1.6 MmnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX65OkBp M3fwSWlEPTB;NT6wN{DPxE1? NFrnXm8zPDN2OEi1OC=>
A549/PEM-6.4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUK5OkBp NU[xTGk1UUN3ME2yN{4{QSEQvF2= NG\FWWczPDN2OEi1OC=>
A549/PEM-16 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu5fZU6PiCq NH;qTFJKSzVyPUWxMlQ2KM7:TR?= NHfJPYkzPDN2OEi1OC=>
HT-29 NVHQU3NzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jFcFczyqCqwrC= M4CxU2ROW00EoB?= MUTJR|UxRTFyLkC3JOKyKDBwOUSg{txO Mn\yNlM6PTl2NkC=
LoVo NV;1[mw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLhWXF6PzMEoHlCpC=> NF\5SJRFVVORwrC= M{WwXmlEPTB;MD6wN|IhyrFiMD6wNFIh|ryP M{ezVFI{QTV7NE[w
SW620 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWq3NuKhcMLi M3jSe2ROW00EoB?= MVXJR|UxRTFwMEmgxtEhOC5yMTFOwG0> MXmyN|k2QTR4MB?=
HCT116 NGCwT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\YNnA3PzMEoHlCpC=> M1LCbWROW00EoB?= MWrJR|UxRTBwMES5JOKyKDBwMEGzJO69VQ>? MVyyN|k2QTR4MB?=
SW1116 NGOyeYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX3O|LDqGkEoB?= MnnBSG1UV8Li MkPGTWM2OD1zLkewJOKyKDBwMEOg{txO MkPTNlM6PTl2NkC=
WiDr MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe3NuKhcMLi MmXNSG1UV8Li Mn71TWM2OD1yLkCxPUDDuSByLkCwNkDPxE1? M1TrN|I{QTV7NE[w
HT-29 M13zVGZ2dmO2aX;uJGF{e2G7 MV:wMlA2yqEQvF2= MVW3NuKhcA>? NVzRSmFUTE2VT9Mg M1jW[olv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckB1cGViUzDwbIF{\cLi M1fGOlI{QTV7NE[w
LoVo NV;6NmduTnWwY4Tpc44hSXO|YYm= NE\qSI8xNjB3wrFOwG0> NHHzNnU4OsLiaB?= MWfEUXNQyqB? Mn3MbY5kemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJJRp\SCVIIDoZZNmyqB? MojlNlM6PTl2NkC=
STAV-AB MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnTOFghcA>? NUHPXVh1eHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVY1NjUEsUKxMlghLQ>? MkjyNlM5PDB|N{[=
M-14-K M1rNd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4CxR|Q5KGh? NGKydYZxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PFEvQMLzMUKuPUAm MWWyN|g1ODN5Nh?=
STAV-FCS M4HzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK0PEBp NYG2PVZYeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVg5NjIEsUiuPUAm MmKwNlM5PDB|N{[=
ZL-34 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe0PEBp NIHFVIpxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PVUvP8LzNj61JEU> M{D4ZlI{QDRyM{e2
JL-1 NIq2fZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LZUVQ5KGh? M3HzXZBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{25PE4zyrF{LkKgKS=> NIrqUGczOzh2MEO3Oi=>
DM-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli5OFghcA>? MYDwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;MUCxMlPDuTJwODCl NWG0SFQzOjN6NECzO|Y>
Jurkat NV;HXJZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfXc5lWPDhiaB?= M4f2PZBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{23Ok44yrF2LkOgKS=> Ml3lNlM5PDB|N{[=
BXPC-3 Ml3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvSdZRqUUN3ME2zPU45PsLzMT62PEDPxE1? MVOyNlk4PzZyNx?=
PANC-1 NYjFbnFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfEOI5KSzVyPUizMlc3yrFyLkG5JO69VQ>? NVrVXpdJOjJ7N{e2NFc>
BXPC-3 MkPNSpVv[3Srb36gRZN{[Xl? M3[5[FM6Njh4IDFOwG0> Mm\WNlQhcA>? NUPVOFdJcW6mdXPld{BUKGG{cnXzeEApWDxyLkC1LUBidmRiZHXjdoVie2W|IITo[UBvfW2kZYKgc4Yh[2WubIOgbY4hfGinIFeyM20heGijc3ZCpC=> M{jNe|IzQTd5NkC3
BXPC-3 NY\pXHNGTnWwY4Tpc44hSXO|YYm= NIro[YE{QS56NjCg{txO NX:0XIdiOjRiaB?= NXzC[mZO\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> MUCyNlk4PzZyNx?=
PANC-1 MlTjSpVv[3Srb36gRZN{[Xl? NFTOT3k5PCEQvF2= MUiyOEBp NFz2d25mdmijbnPld{BGT0[UIIDoc5NxcG:{eXzheIVlKGyndnXsd{wh[W6mIITo[UBxem:2ZXnuJIxmfmWuc9Mg MVmyNlk4PzZyNx?=
BXPC-3 NVmy[ZRDTnWwY4Tpc44hSXO|YYm= MYmzPU45PiBizszN MUeyOEBp MlG5[Y5p[W6lZYOgSWdHWixiSFXSN{BidmRiQVvUJJBpd3OyaH;yfYxifGmxbjDs[ZZmdHN? MWCyNlk4PzZyNx?=
PANC-1 M3jK[WZ2dmO2aX;uJGF{e2G7 MkjkPFQh|ryP NHfROpkzPCCq MUTlcohidmOnczDFS2ZTNCCKRWKzJIFv\CCDS2SgdIhwe3Cqb4L5cIF1cW:wIHzleoVtew>? MnS4NlI6Pzd4MEe=

... 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