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 M{DtSWNmdGxiVnnhZoltcXS7IFHzd4F6 Ml\sNUDPxE1? MnnXOFghcA>? NVfGW4RY\W6qYX7j[ZMhe2mvdnHzeIF1cW5iaX7obYJqfGWmII\pZYJqdGm2eR?= MW[yOlM{PDN{MB?=
A549 NX;L[npjS2WubDDWbYFjcWyrdImgRZN{[Xl? NVHqUVhLOSEQvF2= MlGzOFghcA>? M1W5c4VvcGGwY3XzJJNqdX[jc4TheIlvKGmwaHnibZRm\CC4aXHibYxqfHl? MV[yOlM{PDN{MB?=
MSTO-211H NYHpNldETnWwY4Tpc44hSXO|YYm= Ml;0NUDPxE1? MXqyOEBp NVTsfI9x\W6qYX7j[ZMh[XW2b4DoZYd6KGOxdILlZZRm\CC5aYToJJNqdX[jc4TheIlv MlnvNlY{OzR|MkC=
A549 MYfGeY5kfGmxbjDBd5NigQ>? NWG0OWVnOSEQvF2= MWGyOEBp NHvxVplmdmijbnPld{BifXSxcHjh[5kh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NFrPNWwzPjN|NEOyNC=>
MSTO-211H M{jtdGFxd3C2b4Ppd{BCe3OjeR?= MUixJO69VQ>? NFTMepYzPCCq Mn\MbY5lfWOnczDhdI9xfG:|aYOgZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= NVvrT2d2OjZ|M{SzNlA>
A549 NYX0SFlMSXCxcITvd4l{KEG|c3H5 NITTZ5oyKM7:TR?= NUDGcYZIOjRiaB?= MXLpcoR2[2W|IHHwc5B1d3OrczDjc5Rz\WG2ZXSge4l1cCC|aX32ZZN1[XSrbh?= NHq5VIMzPjN|NEOyNC=>
MSTO-211H MVrGeY5kfGmxbjDBd5NigQ>? MUSxJO69VQ>? MUi0PEBp NX:0cHdZcW6lcnXhd4V{KEGPUFugdIhwe3Cqb4L5cIF1cW:wIHHu[EBiKGOxbnPvcYl1[W62IHTlZ5Jm[XOnIHnuJGFMXCCjbnSgcXRQWiCyaH;zdIhwenmuYYTpc44h[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NFXTeIozPjN|NEOyNC=>
A549 NGW1[5RHfW6ldHnvckBCe3OjeR?= NFyyelcyKM7:TR?= MkSzOFghcA>? NHrLeYJqdmO{ZXHz[ZMhSU2SSzDwbI9{eGixconsZZRqd25iYX7kJIEh[2:wY3;tbZRidnRiZHXjdoVie2ViaX6gRWtVKGGwZDDtWG9TKHCqb4PwbI9zgWyjdHnvckBkd3S{ZXH0[YQhf2m2aDDzbY13[XO2YYTpci=> NIPjbWUzPjN|NEOyNC=>
Vero NYXaS4JWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXibWsxNjJ|NNMgcW0> NH\Cb5IzPCCq NUXidIpm\3Kxd4ToJIlvcGmkaYTpc44:Pe,7qh?= MnLoNlU6PzV4M{e=
A549 MnTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXKwXIdROC5{M{VCpI1O Ml3iNlQhcA>? MoD6[5Jwf3SqIHnubIljcXSrb369NVDwwap? M3zCTVI2QTd3NkO3
HeLa MkP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rQfVAvOjN2wrDtUS=> NV\LXZE2OjRiaB?= MV7ndo94fGhiaX7obYJqfGmxbk2189mr M4TRNVI2QTd3NkO3
T47D NH3tS5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIroUJExNjJ|NNMgcW0> MnHpNlQhcA>? MUHndo94fGhiaX7obYJqfGmxbk2xNQ+6sg>? MlXENlU6PzV4M{e=
Vero NEfjOnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrFNE4zOzUEoH3N NID3[201QCCq MnWx[5Jwf3SqIHnubIljcXSrb369NVDwwap? Ml;KNlU6PzV4M{e=
A549 NGD4XHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3P2RVAvOjN2wrDtUS=> MU[0PEBp M3LCPYdzd3e2aDDpcohq[mm2aX;uQVMx97ns MXGyOVk4PTZ|Nx?=
HeLa M37WRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\RVXZuOC5{M{VCpI1O MX20PEBp NEizVYhoem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= NX\qW2lGOjV7N{W2N|c>
T47D M17DPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\QUVAvOjN2wrDtUS=> M{i2T|Q5KGh? MWDndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? NYDYNYtEOjV7N{W2N|c>
Vero MorhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDEeWVpOC5{M{VCpI1O MlTHO|IhcA>? NHPycFZoem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= M2TqeVI2QTd3NkO3
A549 NXnuRYszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmO0NE4zOzUEoH3N NGTUfm04OiCq MV;ndo94fGhiaX7obYJqfGmxbk21NQ+6sg>? NYPsd3V{OjV7N{W2N|c>
HeLa NFTMOXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHaTmIxNjJ|NNMgcW0> NY\j[JpGPzJiaB?= NI\O[|Foem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= NWnUdFE2OjV7N{W2N|c>
T47D NIHB[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37MOlAvOjN2wrDtUS=> NGm0doc4OiCq NU\kTI5R\3Kxd4ToJIlvcGmkaYTpc44:OzExubq= MX[yOVk4PTZ|Nx?=
A459 NVG5T5FsTnWwY4Tpc44hSXO|YYm= NYfseGFZOS9{L{Sg{txO NHq4Z5UzPC92ODDo MYPpcoR2[2W|IFexJJBp[XOnIHHydoV{fCCrbjDkc5NmNSCjbnSgeIlu\SCmZYDlcoRmdnRibXHucoVz Mki5NlU4PDN6MkK=
A459 NVT0[5BRTnWwY4Tpc44hSXO|YYm= MnW5NU8zNzRizszN MW[0PEBp MoPG[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZicD3Bb5Q> MlTXNlU4PDN6MkK=
A459 MkDSRZBweHSxc3nzJGF{e2G7 NGn3Z2k1|ryP NVzNcpZJPDhiaB?= NIS2XHVqdmS3Y3XzJIFxd3C2b4Ppdy=> NVvzTolSOjV5NEO4NlI>
HepG2 Ml2wR4VtdCCYaXHibYxqfHliQYPzZZk> MlryNE4y6oDVMUCwxsDPxE1? NGftW5Y4OiCq MXPobYdpKGOxbnPlcpRz[XSrb37zJI9nKHCnbXX0doV5\WRiYYSgLFExNzFyMNMg{txOMSCxbnz5JJNtcWeqdHz5JIlvcGmkaYTzJGhmeEd{IHPlcIwhe3W{dnn2ZYw> MmLMNlU1PDZzMEK=
HepG2 NXvBU2ZVSXCxcITvd4l{KEG|c3H5 NE\odocxNjIkgKOxNFDDqM7:TR?= NE[1bGo4OiCq MojGbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bImgZZQhcGmpaDDjc45k\XKwdILheIlwdg>? NF65Sm0zPTR2NkGwNi=>
HepG3 MkHmSpVv[3Srb36gRZN{[Xl? Mn7LNE4y6oDVMUCwxsDPxE1? MXG0PEBp NF3PTotqdmS3Y3XzJJA3OiCmb4fudoVofWyjdHnvckBieyC5ZXzsJIF{KEKnY3zpck0yKGGwZDDMR|NDNUmLIIXwdoVofWyjdHnvci=> MVuyOVQ1PjFyMh?=
HepG3 MYrGeY5kfGmxbjDBd5NigQ>? M3jVVlAvOeLCk{GwNOKh|ryP M2rXZlQ5KGh? MXPhZ5RqfmG2ZYOgZ5l1dy2ycn;0[YN1cX[nIHH1eI9xcGGpedMg MWGyOVQ1PjFyMh?=
HepG3 NXPIZpFxTnWwY4Tpc44hSXO|YYm= NVr2OYJzOTEEoN88US=> MlzxOFghcA>? MVT1dJJm\3WuYYTld{BxcG:|cHjvdplt[XSnZDCodE0qKE2HS{GvNkApW2W{MkG3M|IzOSliYX7kJJAuTVKNMT:yJEhVcHJ{MEKvWJlzOjB2KR?= M1e0b|I2PDR4MUCy
U20S MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXXPOJR1OC5yMT2xNFAh|ryP NE\1TYc4OiCq M4r0UolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Vl\XCnbnTlcpRtgQ>? MoqwNlUyPTJ|OUm=
MG-63 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmjWNE4xOS1zMECg{txO MnHiO|IhcA>? NVnqXJUxcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\WSncHXu[IVvfGy7 NIKxcXIzPTF3MkO5PS=>
A549 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlnPNU0yODByIH7N MXK3NkBp NFTYWXpKSzVyPUGzO{BvVQ>? M3LBOVI2OTR3Nk[5
H1299 M3XoRWNmdGxiVnnhZoltcXS7IFHzd4F6 NFrVclIyNTFyMECgcm0> M3jVZlczKGh? M{G0Z2lEPTB;MUe4JI5O M4DyXVI2OTR3Nk[5
MSTO-211 M{HT[mNmdGxiVnnhZoltcXS7IFHzd4F6 MYixJO69VQ>? MXO0PEBp MXvwdo9lfWOnczDhJJN6dmW{Z3nzeIlkKGmwaHnibZRwenliZX\m[YN1KG:wIITo[UBk\WyuIHfyc5d1cCClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv MY[yOVA6Pjl7Mx?=
A549 NWjic3hXS2WubDDWbYFjcWyrdImgRZN{[Xl? MUWxJO69VQ>? M1z4OlQ5KGh? M1u4bJBzd2S3Y3XzJIEhe3mwZYLnbZN1cWNiaX7obYJqfG:{eTDl[oZm[3Rib36geIhmKGOnbHyg[5Jwf3SqIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? M{H5O|I2ODl4OUmz
MSTO-211 M{C0TmFxd3C2b4Ppd{BCe3OjeR?= M2nTXFEh|ryP NEXwNGU1QCCq MX;lcohidmOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= NV3ub4NWOjVyOU[5PVM>
A549 NH7UdWJCeG:ydH;zbZMhSXO|YYm= MmW2NUDPxE1? M3KwflQ5KGh? MX;lcohidmOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= MWOyOVA6Pjl7Mx?=
MSTO-211 NV3DVHduTnWwY4Tpc44hSXO|YYm= NUHsbo1tOSEQvF2= NH7iTXA1QCCq NGX5cZlmdmijbnPld{BqdnS{YXPlcIx2dGG{IGLPV{Bxem:mdXP0bY9vKGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> NXnlcohjOjVyOU[5PVM>
A549 NHHCd49HfW6ldHnvckBCe3OjeR?= MlyxNUDPxE1? MXe0PEBp NYHzZmxz\W6qYX7j[ZMhcW62cnHj[YxtfWyjcjDSU3MheHKxZIXjeIlwdiClb33ibY5m\CC5aYToJJNqdX[jc4TheIlv Mo\CNlUxQTZ7OUO=
MSTO-211 M1TKSWZ2dmO2aX;uJGF{e2G7 M2O1VVEh|ryP MnHJOFghcA>? MlrRcIVi\HNidH:gcYl1d2Oqb37kdolidCCmeYPmeY5kfGmxbjDjc41jcW6nZDD3bZRpKHOrbY\hd5RifGmw NIDZUFAzPTB7Nkm5Ny=>
A549 M4\ON2Z2dmO2aX;uJGF{e2G7 NVTW[nl2OSEQvF2= MoPhOFghcA>? Ml7kcIVi\HNidH:gcYl1d2Oqb37kdolidCCmeYPmeY5kfGmxbjDjc41jcW6nZDD3bZRpKHOrbY\hd5RifGmw MoPxNlUxQTZ7OUO=
A549  NV3PZo1rTnWwY4Tpc44hSXO|YYm= Mn;XNk42NzVxMUCg{txO MmXCOFghcA>? MYDpcoNz\WG|ZYOgUo95[SCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> MUCyOFk6OTd4OB?=
H1792 MVXGeY5kfGmxbjDBd5NigQ>? M4qwZVIvPS93L{GwJO69VQ>? MX60PEBp M1LyN4lv[3KnYYPld{BPd3ijIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NYDD[pRvOjR7OUG3Olg>
A549  NEW2S2ZHfW6ldHnvckBCe3OjeR?= MUGyMlUh|ryP NFPSVYg1QCCq MVfpcoR2[2W|IHPhd5Bie2VvOTygZ4F{eGG|ZT2zJIFv\CCyb3z5JEhCTFBvcnnic5NmMSCyb3z5cYVz[XOnIDjQRXJRMSClbHXheoFo\Q>? NVvtTWpWOjR7OUG3Olg>
H1792 MnuySpVv[3Srb36gRZN{[Xl? NXLKUYdsOi53IN88US=> MV[0PEBp NYrLZYh[cW6mdXPld{Bk[XOyYYPlMVktKGOjc4Dhd4UuOyCjbnSgdI9tgSBqQVTQMZJq[m:|ZTmgdI9tgW2ncnHz[UApWEGUUDmgZ4xm[X[jZ3W= NVP4[4JJOjR7OUG3Olg>
A549  NIn2SJJHfW6ldHnvckBCe3OjeR?= MorRNk42NzVxMUCg{txO M2KzO|Q5KGh? NIXLepFld3ewcnXneYxifGW|IF3jcE0yyqB? Ml7RNlQ6QTF5Nki=
H1792 M3;IdGZ2dmO2aX;uJGF{e2G7 NYnyTIk{Oi53L{WvNVAh|ryP MnG1OFghcA>? M4O4TYRwf26{ZXf1cIF1\XNiTXPsMVHDqA>? NV3nPFQ5OjR7OUG3Olg>
A549 MmLyRZBweHSxc3nzJGF{e2G7 NYD5XVc5Oi53IN88US=> NEPWbpQ1QCCq M4XUZ4lv\HWlZYOgZZBweHSxc3nz MXOyOFk6OTd4OB?=
A549 NISzOppHfW6ldHnvckBCe3OjeR?= MmfTOUDPxE1? MmDmPEBp Ml\CbY5kemWjc3XzJG1kdC1zIIXibZF2cXSrbnH0bY9vKGyndnXsdy=> MX[yOFk6OTd4OB?=
A549 NVHJcZJ4TnWwY4Tpc44hSXO|YYm= MWexJOK2VQ>? MlqyOE85NzF{L{K0M|Q5KGh? NGi4bFVqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIDoc5NxcG:{eXzheIVlKEGtdDDpckBiKHSrbXWg[IVx\W6mZX70JI1idm6nch?= MVqyOFg1Pzh4Mx?=
A549 Ml65SpVv[3Srb36gRZN{[Xl? M1jlWVAvOS9yLkOvNUDPxE1? MVu0PEBp NWO5NWVocW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwbI9{eGixconsZZRm\CCDa4SgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MmfhNlQ5PDd6NkO=
A549 MmrMRZBweHSxc3nzJGF{e2G7 NV7sPYt7OC5zL{CuN{8yKM7:TR?= NHHt[VA1QCCq NHi3[mpqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NEnnTJMzPDh2N{i2Ny=>
A549 M4PGfWZ2dmO2aX;uJGF{e2G7 MmraNE4yNzBwMz:xJO69VQ>? NIn1eVA1QCCq NHHhOo5qdmO{ZXHz[ZMhfGinIILheIlwKG:oIGOtdIhie2VicH;weYxifGmxbh?= M{fVNFI1QDR5OE[z
PC9 Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LifFczKGh? NHTnT5JKSzVyPUG2MlA2yrFzLki1JI5O M{PxTlI1QDRyOEmx
PC9/GR M{PWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{C0NFczKGh? MnjqTWM2OD12Lkm0xtExNjR2MDFOwG0> NX;3S5U{OjR6NEC4PVE>
PC9 NFHUdGdHfW6ldHnvckBCe3OjeR?= MYmxOkBvVQ>? MYq3NkBp MYnpcoR2[2W|IGOtdIhie2ViYYLy[ZN1 MkG3NlQ5PDB6OUG=
PC9/GR NVfWdmc6TnWwY4Tpc44hSXO|YYm= M{TjSFQvQTRizszN MlTXO|IhcA>? NVTKNGR1cW6mdXPld{BUNXCqYYPlJIFzemW|dB?= MmPJNlQ5PDB6OUG=
PC9 Mm[zRZBweHSxc3nzJGF{e2G7 NWn5bohZOTZibl2= MkH1O|IhcA>? NVXxZ2ZycW6mdXPld{AyPC53NP-5rkBieG:ydH;zbZM> M3rGfFI1QDRyOEmx
PC9/GR MUDBdI9xfG:|aYOgRZN{[Xl? MmLPOE46PCEQvF2= NHrtPIc4OiCq Mn;MbY5lfWOnczCxPU42PO,7qjDhdI9xfG:|aYO= M4rJbVI1QDRyOEmx
PC9/GR MlvrSpVv[3Srb36gRZN{[Xl? NUfFeohlPC57NDFOwG0> NXe3bHlxPzJiaB?= NXPGbmhJcW6lcnXhd4V{KHBvRWLLJIxmfmWucx?= MWiyOFg1ODh7MR?=
PC9/GR NVSxZ4doTnWwY4Tpc44hSXO|YYm= Mmq1OE46PCEQvF2= NH;LSmo4OiCq NVLEN4c6cW6lcnXhd4V{KHBvQVvUJIxmfmWucx?= NVG1b5FNOjR6NEC4PVE>
H28 NITtR41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIKybFBKSzVyPUCuNFfDuTBwMEKg{txO NFzNd2UzPDdzNEeyNi=>
211H NEDBN2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwMEhCtVAvODFizszN NFq3fpMzPDdzNEeyNi=>
H2052 M{jnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mly0TWM2OD1yLkW3xtExNjN2IN88US=> MX6yOFcyPDd{Mh?=
H2452 NHLjd5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfUb4xKSzVy78{eNVAxKM7:TR?= M3zPeFI1PzF2N{Ky
MES01 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r5WWlEPTExvK6xNFAh|ryP M2Cye|I1PzF2N{Ky
MES04 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnWzTWM2OO,:nkGwNEDPxE1? NGH0d5QzPDdzNEeyNi=>
A549 NGrESZBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2r2fFAvOS9yLkOvNE42NzFizszN M2WyeFI1NzR6IHi= M1rkTmROW09? MXzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MV[yOFYzPjd{Mh?=
A549 NEjh[41HfW6ldHnvckBCe3OjeR?= M2jDbFAvOS9yLkOvNE42NzFizszN NIPaOW8zPC92ODDo NULiOYRWTE2VTx?= NXu2OploeHKxZIXj[ZMhfGinIH\vdo1ifGmxbjDv[kBCXk:|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MlO5NlQ3OjZ5MkK=
H1993 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Ha[2lEPTB;MD6xO{DPxE1? NWnZV3FEOjR2MUi1NVk>
H1299 M{G4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofFTWM2OD1zLki0JO69VQ>? MlvYNlQ1OTh3MUm=
H226 NYDMUVgzS2WubDDWbYFjcWyrdImgRZN{[Xl? NIjZ[JEyNTFyIN88[{9udA>? NFfueWY4OiCq MWTJR|UxRjFyIN88[{9udA>? M3HVWlI1Ozd6NUe2
H290 M4iwRmNmdGxiVnnhZoltcXS7IFHzd4F6 NE\qdnAyNTFyIN88[{9udA>? M4n6U|czKGh? MWrJR|UxRjFyIN88[{9udA>? MUOyOFM4QDV5Nh?=
Y-meso14 MmLwR4VtdCCYaXHibYxqfHliQYPzZZk> MXWxMVExKM7:Zz;tcC=> NV7TbHd[PzJiaB?= MljZTWM2OD5zMDFOwIcwdWx? NELSRYEzPDN5OEW3Oi=>
MSTO-211H M2[zSGNmdGxiVnnhZoltcXS7IFHzd4F6 NUG4ZWxbOS1zMDFOwIcwdWx? MV63NkBp MY\JR|UxhjBwMESg{txoN22u MnW3NlQ{Pzh3N{[=
A549 M2jOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHEPVYhcA>? Mn7kTWM2OD1zLkO1JO69VQ>? MnXoNlQ{PDh6NUS=
A549/PEM-1.6 NYq0ZoU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPHcoI6PiCq Mn7FTWM2OD13LkCzJO69VQ>? M3jFRlI1OzR6OEW0
A549/PEM-6.4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\JPVYhcA>? MWLJR|UxRTJ|LkO5JO69VQ>? NHewdnUzPDN2OEi1OC=>
A549/PEM-16 NVXlfGpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HG[Vk3KGh? MkDOTWM2OD13MT60OUDPxE1? MWGyOFM1QDh3NB?=
HT-29 M4XnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITqbXc4OsLiaNMg NEXI[mlFVVORwrC= NX3U[JI1UUN3ME2xNE4xPyEEsTCwMlk1KM7:TR?= M13rR|I{QTV7NE[w
LoVo MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfnO|LDqGkEoB?= M1;xSmROW00EoB?= MUfJR|UxRTBwMEOyJOKyKDBwMECyJO69VQ>? NXHqTlhpOjN7NUm0OlA>
SW620 NYj6dXZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moi0O|LDqGkEoB?= MXzEUXNQyqB? Mm\HTWM2OD1zLkC5JOKyKDBwMEGg{txO NHHL[m8zOzl3OUS2NC=>
HCT116 NGDOOXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPjS2g4OsLiaNMg Mnu0SG1UV8Li NGjRW5NKSzVyPUCuNFQ6KMLzIECuNFE{KM7:TR?= Mn7zNlM6PTl2NkC=
SW1116 M4HFb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\HWGU4OsLiaNMg M33ZT2ROW00EoB?= NWLw[GtEUUN3ME2xMlcxKMLzIECuNFMh|ryP NXW4ZZh3OjN7NUm0OlA>
WiDr NEPId|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rjPVczyqCqwrC= MWrEUXNQyqB? NY\HXHA2UUN3ME2wMlAyQSEEsTCwMlAxOiEQvF2= MnrXNlM6PTl2NkC=
HT-29 NIHYOplHfW6ldHnvckBCe3OjeR?= NFjlUYkxNjB3wrFOwG0> MWK3NuKhcA>? NYfvfmJTTE2VT9Mg M3TvbYlv[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckB1cGViUzDwbIF{\cLi M{n0NVI{QTV7NE[w
LoVo MkDjSpVv[3Srb36gRZN{[Xl? M13YblAvODYEoN88US=> NVTjNmV3PzMEoHi= MWLEUXNQyqB? NHy2SGpqdmO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hfGinIGOgdIhie2YEoB?= MnjnNlM6PTl2NkC=
STAV-AB NILZRpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfRT3VMPDhiaB?= MV;wdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;NkSuOOKyOjFwODCl Ml3WNlM5PDB|N{[=
M-14-K Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO0PEBp MUjwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OEGuPOKyOTJwOTCl M1fhV|I{QDRyM{e2
STAV-FCS M1XYZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG0PEBp M4rCbpBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{24PE4yyrF6LkmgKS=> M3npTVI{QDRyM{e2
ZL-34 NIW3OYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\k[JdYPDhiaB?= NXzaNXVqeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVk2NjgEsU[uOUAm MYeyN|g1ODN5Nh?=
JL-1 NIrOZVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXu0PEBp Ml7MdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm4MlLDuTJwMjCl M{LyN|I{QDRyM{e2
DM-3 NH3KPZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWW0PEBp MV3wdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;MUCxMlPDuTJwODCl M2P1fVI{QDRyM{e2
Jurkat NWXpWG05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjwNY41PDhiaB?= NU\WfY1ReHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVc3NjgEsUSuN{Am M3nXZlI{QDRyM{e2
BXPC-3 NX[4OlB2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG3[5ZKSzVyPUO5Mlg3yrFzLk[4JO69VQ>? NInyOXUzOjl5N{[wOy=>
PANC-1 NFm2PY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTh|Lke2xtExNjF7IN88US=> NVLhW4hXOjJ7N{e2NFc>
BXPC-3 M4\H[mZ2dmO2aX;uJGF{e2G7 MXyzPU45PiBizszN M4OyTVI1KGh? MoPUbY5lfWOnczDTJIFzemW|dDCoVFwxNjB3KTDhcoQh\GWlcnXhd4V{KHSqZTDueY1j\XJib3[gZ4VtdHNiaX6geIhmKEd{L12gdIhie2YEoB?= NHrz[XYzOjl5N{[wOy=>
BXPC-3 NVqxbG5HTnWwY4Tpc44hSXO|YYm= MYKzPU45PiBizszN NGPtOVMzPCCq MnX5[Y5p[W6lZYOgSWdHWiCyaH;zdIhwenmuYYTl[EBt\X[nbIOsJIFv\CC2aHWgdJJwfGWrbjDs[ZZmdHQEoB?= Mnz2NlI6Pzd4MEe=
PANC-1 MYnGeY5kfGmxbjDBd5NigQ>? M{HTN|g1KM7:TR?= MWOyOEBp NUjHfZg2\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> Mk\SNlI6Pzd4MEe=
BXPC-3 NH3oVG1HfW6ldHnvckBCe3OjeR?= Mn7SN|kvQDZiIN88US=> NG\1NHgzPCCq MVrlcohidmOnczDFS2ZTNCCKRWKzJIFv\CCDS2SgdIhwe3Cqb4L5cIF1cW:wIHzleoVtew>? NGi4WGkzOjl5N{[wOy=>
PANC-1 MXHGeY5kfGmxbjDBd5NigQ>? M3:5b|g1KM7:TR?= MXmyOEBp M4jIPYVvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| M2XBO|IzQTd5NkC3

... 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(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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03513666 Recruiting NSCLC Shanghai Junshi Bioscience Co.Ltd. April 9 2018 Phase 2
NCT03366064 Recruiting Non-small Cell Lung Cancer Asan Medical Center|Korea Research Institute of Bioscience and Biotechnology November 9 2017 Phase 1
NCT02693717 Recruiting Bladder Cancer|Urothelial Cancer M.D. Anderson Cancer Center|Eli Lilly and Company May 9 2017 Phase 2
NCT01454102 Active not recruiting Non-small Cell Lung Cancer Bristol-Myers Squibb December 9 2011 Phase 1
NCT00248495 Completed Lung Cancer Roswell Park Cancer Institute June 8 2005 Phase 2
NCT03526900 Recruiting 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