Pemetrexed

For research use only.

Catalog No.S1135 Synonyms: LY-231514

24 publications

Pemetrexed  Chemical Structure

Molecular Weight(MW): 471.37

Pemetrexed (LY-231514) 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. Pemetrexed induces autophagy and apoptosis.

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Selleck's Pemetrexed has been cited by 24 publications

Purity & Quality Control

Choose Selective DHFR Inhibitors

Biological Activity

Description Pemetrexed (LY-231514) 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. Pemetrexed induces autophagy and apoptosis.
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 NHTwTmhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1Wz[VEh|ryP M1TT[|Q5KGh? MU\lcohidmOnczDzbY13[XO2YYTpckBqdmirYnn0[YQhfmmjYnnsbZR6 Mor3NlY{OzR|MkC=
A549 NXj1Uok1S2WubDDWbYFjcWyrdImgRZN{[Xl? Mn7ZNUDPxE1? M3XGSlQ5KGh? MnTo[Y5p[W6lZYOgd4lufmG|dHH0bY4hcW6qaXLpeIVlKH[rYXLpcIl1gQ>? Ml62NlY{OzR|MkC=
MSTO-211H M{XG[2Z2dmO2aX;uJGF{e2G7 M1rESlEh|ryP NITzV5ozPCCq MoPo[Y5p[W6lZYOgZZV1d3CqYXf5JINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NULpXnI1OjZ|M{SzNlA>
A549 NFqx[2hHfW6ldHnvckBCe3OjeR?= Mn3wNUDPxE1? MX:yOEBp Mnv5[Y5p[W6lZYOgZZV1d3CqYXf5JINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NYCxUoxUOjZ|M{SzNlA>
MSTO-211H MlL1RZBweHSxc3nzJGF{e2G7 MX2xJO69VQ>? M4S1OFI1KGh? NWXNd4Q1cW6mdXPld{BieG:ydH;zbZMh[2:2cnXheIVlKHerdHigd4lufmG|dHH0bY4> NUHVd5plOjZ|M{SzNlA>
A549 NFvyUnlCeG:ydH;zbZMhSXO|YYm= NHH0cIoyKM7:TR?= MmjUNlQhcA>? M3jIfIlv\HWlZYOgZZBweHSxc3nzJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu NX6zWYx{OjZ|M{SzNlA>
MSTO-211H MlfNSpVv[3Srb36gRZN{[Xl? MV[xJO69VQ>? MV:0PEBp M1vJZYlv[3KnYYPld{BCVVCNIIDoc5NxcG:{eXzheIlwdiCjbnSgZUBkd26lb33peIFvfCCmZXPy[YF{\SCrbjDBT3Qh[W6mIH3UU3IheGixc4Doc5J6dGG2aX;uJINwfHKnYYTl[EB4cXSqIIPpcZZie3SjdHnu M1;E[FI3OzN2M{Kw
A549 NUnlbFhrTnWwY4Tpc44hSXO|YYm= M1W3V|Eh|ryP MoGwOFghcA>? MlHNbY5kemWjc3XzJGFOWEticHjvd5Bpd3K7bHH0bY9vKGGwZDDhJINwdmOxbXn0ZY51KGSnY4LlZZNmKGmwIFHLWEBidmRibWTPVkBxcG:|cHjvdplt[XSrb36gZ491emWjdHXkJJdqfGhic3nteoF{fGG2aX6= MmCzNlY{OzR|MkC=
Vero Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu1OlkxNjJ|NNMgcW0> MnXQNlQhcA>? M{f1fIdzd3e2aDDpcohq[mm2aX;uQVXwwap? MVuyOVk4PTZ|Nx?=
A549 MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfCR4hIOC5{M{VCpI1O NX3mRYVtOjRiaB?= NX7aRWpJ\3Kxd4ToJIlvcGmkaYTpc44:OTExubq= NV7kdYpGOjV7N{W2N|c>
HeLa Ml\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPEWHN6OC5{M{VCpI1O NWTQUItVOjRiaB?= MWTndo94fGhiaX7obYJqfGmxbk2189mr MnjVNlU6PzV4M{e=
T47D M{TC[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfYelVzOC5{M{VCpI1O NYjHZ5FvOjRiaB?= NX3VbJhN\3Kxd4ToJIlvcGmkaYTpc44:OTExubq= MWSyOVk4PTZ|Nx?=
Vero M2rFb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPDTlExNjJ|NNMgcW0> MWO0PEBp NFHYU5hoem:5dHigbY5pcWKrdHnvcl0yOO,7qh?= MX2yOVk4PTZ|Nx?=
A549 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLJeJkxNjJ|NNMgcW0> NXPpTFFkPDhiaB?= MkPi[5Jwf3SqIHnubIljcXSrb369N|Dwwap? MmHxNlU6PzV4M{e=
HeLa NH72OINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fwWFAvOjN2wrDtUS=> NInFV|Q1QCCq NXTTN|lQ\3Kxd4ToJIlvcGmkaYTpc44:OTExubq= MljwNlU6PzV4M{e=
T47D NUnnOGFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XMWlAvOjN2wrDtUS=> NU\Q[5RbPDhiaB?= MV;ndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? NXThTVlGOjV7N{W2N|c>
Vero M2HQV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrCe2ZuOC5{M{VCpI1O NYLUTIN2PzJiaB?= NF\RZ|Foem:5dHigbY5pcWKrdHnvcl0zOO,7qh?= M{L2O|I2QTd3NkO3
A549 NXH5TJl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfRNE4zOzUEoH3N NU\sc3hDPzJiaB?= NGnnUlNoem:5dHigbY5pcWKrdHnvcl02OO,7qh?= NWrCeJFYOjV7N{W2N|c>
HeLa NH6w[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe0PHk3OC5{M{VCpI1O M1XWW|czKGh? NW\NTph2\3Kxd4ToJIlvcGmkaYTpc44:OjExubq= M2nsNFI2QTd3NkO3
T47D MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\4[Zc{OC5{M{VCpI1O NILxN2c4OiCq NUW1b2Zx\3Kxd4ToJIlvcGmkaYTpc44:OzExubq= MnTrNlU6PzV4M{e=
A459 Ml3iSpVv[3Srb36gRZN{[Xl? NE\JdoEyNzJxNDFOwG0> MlHUNlQwPDhiaB?= NHP0R5FqdmS3Y3XzJGcyKHCqYYPlJIFzemW|dDDpckBld3OnLTDhcoQhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ MljiNlU4PDN6MkK=
A459 MoTySpVv[3Srb36gRZN{[Xl? NEXuXlgyNzJxNDFOwG0> NHPEc|E1QCCq MkO0[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZicD3Bb5Q> MX[yOVc1Ozh{Mh?=
A459 NHzN[YtCeG:ydH;zbZMhSXO|YYm= MVm0{txO NILQOnQ1QCCq NVnwOYJHcW6mdXPld{BieG:ydH;zbZM> NUXESHFoOjV5NEO4NlI>
HepG2 NIW1V2JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXGwMlHjiJNzMEFCpO69VQ>? MmfaO|IhcA>? MlfGbIlocCClb37j[Y51emG2aX;ud{Bw\iCyZX3leJJmgGWmIHH0JEgyOC9zMEFCpO69VSlib37sfUB{dGmpaITsfUBqdmirYnn0d{BJ\XCJMjDj[YxtKHO3co\peoFt MUSyOVQ1PjFyMh?=
HepG2 NX\SZnRkSXCxcITvd4l{KEG|c3H5 M4PGd|AvOeLCk{GwNOKh|ryP MWS3NkBp M361NIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5JIF1KGirZ3igZ49v[2W{boTyZZRqd25? Mm\GNlU1PDZzMEK=
HepG3 M{\BVWZ2dmO2aX;uJGF{e2G7 MXiwMlHjiJNzMEFCpO69VQ>? NYTvU2pvPDhiaB?= MofYbY5lfWOnczDwOlIh\G:5boLl[5Vt[XSrb36gZZMhf2WubDDhd{BD\WOuaX6tNUBidmRiTFOzRk1KUSC3cILl[5Vt[XSrb36= NUfTSo9TOjV2NE[xNFI>
HepG3 Ml7RSpVv[3Srb36gRZN{[Xl? MXWwMlHjiJNzMEFCpO69VQ>? M1G4N|Q5KGh? NVPG[mo3[WO2aY\heIV{KGO7dH:tdJJwfGWldHn2[UBifXSxcHjh[5nDqA>? M4LhRlI2PDR4MUCy
HepG3 M1vSWmZ2dmO2aX;uJGF{e2G7 M1HQSVExyqEQvF2= MkXROFghcA>? MonyeZBz\We3bHH0[ZMheGixc4Doc5J6dGG2ZXSgLJAuMSCPRVuxM|IhMFOnckKxO{8zOjFrIHHu[EBxNUWUS{GvNkApXGi{MkCyM3R6ejJyNDm= NYD5XYVJOjV2NE[xNFI>
U20S NFnYPGtE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUKwMlAyNTFyMDFOwG0> MYC3NkBp M{W3WYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Vl\XCnbnTlcpRtgQ>? MV2yOVE2OjN7OR?=
MG-63 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn74NE4xOS1zMECg{txO MWS3NkBp NVf2RpBxcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\WSncHXu[IVvfGy7 MWSyOVE2OjN7OR?=
A549 NED6e4lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFHKN5gyNTFyMECgcm0> Mn3FO|IhcA>? Mmf1TWM2OD1zM{egcm0> NGTHUJAzPTF2NU[2PS=>
H1299 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MonNNU0yODByIH7N NUjUU|dvPzJiaB?= NFGzcpFKSzVyPUG3PEBvVQ>? M{nUc|I2OTR3Nk[5
MSTO-211 MnzIR4VtdCCYaXHibYxqfHliQYPzZZk> NGXyXpMyKM7:TR?= M{Dr[lQ5KGh? MkXIdJJw\HWlZYOgZUB{gW6ncnfpd5Rq[yCrbnjpZol1d3K7IHXm[oVkfCCxbjD0bIUh[2WubDDndo94fGhiY3;tZolv\WRid3n0bEB{cW24YYP0ZZRqdg>? Moe2NlUxQTZ7OUO=
A549 MmDXR4VtdCCYaXHibYxqfHliQYPzZZk> M{fnW|Eh|ryP MoLROFghcA>? M17OUJBzd2S3Y3XzJIEhe3mwZYLnbZN1cWNiaX7obYJqfG:{eTDl[oZm[3Rib36geIhmKGOnbHyg[5Jwf3SqIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? MUCyOVA6Pjl7Mx?=
MSTO-211 M1u3[mFxd3C2b4Ppd{BCe3OjeR?= NU\2[YZTOSEQvF2= MluzOFghcA>? NVraVGlF\W6qYX7j[ZMh[2G|cHHz[U1l\XCnbnTlcpQh[XCxcITvd4l{KGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MXOyOVA6Pjl7Mx?=
A549 M4HkcmFxd3C2b4Ppd{BCe3OjeR?= MlvmNUDPxE1? M1:5VFQ5KGh? MWflcohidmOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= M2PZdFI2ODl4OUmz
MSTO-211 M1fHNmZ2dmO2aX;uJGF{e2G7 NHTwVpkyKM7:TR?= NHLmRYU1QCCq NHnoR|RmdmijbnPld{BqdnS{YXPlcIx2dGG{IGLPV{Bxem:mdXP0bY9vKGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MnrsNlUxQTZ7OUO=
A549 NHzwc3lHfW6ldHnvckBCe3OjeR?= NX\5SHFwOSEQvF2= M2rRS|Q5KGh? M1r2S4VvcGGwY3XzJIlvfHKjY3XscJVt[XJiUl;TJJBzd2S3Y4Tpc44h[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> M4L1ZlI2ODl4OUmz
MSTO-211 NVzCOW5GTnWwY4Tpc44hSXO|YYm= MXGxJO69VQ>? MmXJOFghcA>? NXLRS4N6dGWjZIOgeI8hdWm2b3Poc45lemmjbDDkfZNnfW6ldHnvckBkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu NH;VVnkzPTB7Nkm5Ny=>
A549 NIO2[4lHfW6ldHnvckBCe3OjeR?= M1zieVEh|ryP M4DVU|Q5KGh? MYXs[YFleyC2bzDtbZRw[2ixbnTybYFtKGS7c3\1coN1cW:wIHPvcYJqdmWmIIfpeIghe2mvdnHzeIF1cW5? MVuyOVA6Pjl7Mx?=
A549  M3H2Z2Z2dmO2aX;uJGF{e2G7 Mo\INk42NzVxMUCg{txO M2flbVQ5KGh? NEjSVW5qdmO{ZXHz[ZMhVm:6YTDlfJBz\XO|aX;uJJNq\26rZnnjZY51dHl? NIXZ[okzPDl7MUe2PC=>
H1792 MXXGeY5kfGmxbjDBd5NigQ>? MYiyMlUwPS9zMDFOwG0> MnPDOFghcA>? M1Lkcolv[3KnYYPld{BPd3ijIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NUK3XpY4OjR7OUG3Olg>
A549  NXHWWHZsTnWwY4Tpc44hSXO|YYm= MmTpNk42KM7:TR?= MYi0PEBp NITRS|BqdmS3Y3XzJINie3Cjc3WtPUwh[2G|cHHz[U0{KGGwZDDwc4x6KCiDRGCtdoljd3OnKTDwc4x6dWW{YYPlJEhRSVKSKTDjcIVifmGpZR?= MojLNlQ6QTF5Nki=
H1792 MnLWSpVv[3Srb36gRZN{[Xl? MnTxNk42KM7:TR?= NFf6cXA1QCCq NGTibJNqdmS3Y3XzJINie3Cjc3WtPUwh[2G|cHHz[U0{KGGwZDDwc4x6KCiDRGCtdoljd3OnKTDwc4x6dWW{YYPlJEhRSVKSKTDjcIVifmGpZR?= NHn5W4gzPDl7MUe2PC=>
A549  NE\WVWRHfW6ldHnvckBCe3OjeR?= MYKyMlUwPS9zMDFOwG0> NEjRfo01QCCq MoHP[I94dnKnZ4XsZZRmeyCPY3ytNeKh NFX2bJkzPDl7MUe2PC=>
H1792 NYD4WYg{TnWwY4Tpc44hSXO|YYm= M1LXVVIvPS93L{GwJO69VQ>? MUW0PEBp M3nTcoRwf26{ZXf1cIF1\XNiTXPsMVHDqA>? NFT1O3MzPDl7MUe2PC=>
A549 NFv2UllCeG:ydH;zbZMhSXO|YYm= NXfhZZJDOi53IN88US=> MlK0OFghcA>? NVjaT2hVcW6mdXPld{BieG:ydH;zbZM> MV:yOFk6OTd4OB?=
A549 NH7IeIJHfW6ldHnvckBCe3OjeR?= MWm1JO69VQ>? MoXXPEBp M2POfYlv[3KnYYPld{BO[2xvMTD1ZolyfWm2aX7heIlwdiCuZY\lcJM> M3XWU|I1QTlzN{[4
A549 NUnXOXFFTnWwY4Tpc44hSXO|YYm= MlLvNUDDvU1? M1vwXFQwQC9zMj:yOE81QCCq M1nISYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicHjvd5Bpd3K7bHH0[YQhSWu2IHnuJIEhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ M4HNU|I1QDR5OE[z
A549 NVTiSFZRTnWwY4Tpc44hSXO|YYm= MVSwMlEwOC5|L{Gg{txO NV;SUXNGPDhiaB?= NV;vTXF4cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwbI9{eGixconsZZRm\CCDa4SgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NWW5c4M5OjR6NEe4OlM>
A549 MmnkRZBweHSxc3nzJGF{e2G7 NV\yRppWOC5zL{CuN{8yKM7:TR?= NVjrflBKPDhiaB?= Ml;TbY5lfWOnczDhdI9xfG:|aYOgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NVTqWYQyOjR6NEe4OlM>
A549 M1P4WmZ2dmO2aX;uJGF{e2G7 M{DKfFAvOS9yLkOvNUDPxE1? NX\CXnpIPDhiaB?= MYPpcoNz\WG|ZYOgeIhmKHKjdHnvJI9nKFNvcHjhd4UheG:ydXzheIlwdg>? NHTHTWwzPDh2N{i2Ny=>
PC9 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHIO|IhcA>? NYf0c5ZFUUN3ME2xOk4xPcLzMT64OUBvVQ>? MmjUNlQ5PDB6OUG=
PC9/GR NWLme4M5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HYb|czKGh? MmTJTWM2OD12Lkm0xtExNjR2MDFOwG0> MV:yOFg1ODh7MR?=
PC9 MoL2SpVv[3Srb36gRZN{[Xl? NXq4cIFiOTZibl2= NXezPJNJPzJiaB?= NWHRUHFTcW6mdXPld{BUNXCqYYPlJIFzemW|dB?= M2LvdVI1QDRyOEmx
PC9/GR MXzGeY5kfGmxbjDBd5NigQ>? Ml7YOE46PCEQvF2= MVe3NkBp M4TUTolv\HWlZYOgV{1xcGG|ZTDhdpJme3R? NVHrRXBjOjR6NEC4PVE>
PC9 MY\BdI9xfG:|aYOgRZN{[Xl? NEHJXHMyPiCwTR?= NXLlWnAxPzJiaB?= MXXpcoR2[2W|IEG0MlU197nsIHHwc5B1d3Orcx?= MWeyOFg1ODh7MR?=
PC9/GR NWTQRZNpSXCxcITvd4l{KEG|c3H5 MV:0Mlk1KM7:TR?= NFLme5M4OiCq MWrpcoR2[2W|IEG5MlU197nsIHHwc5B1d3Orcx?= MWqyOFg1ODh7MR?=
PC9/GR NH7MW|VHfW6ldHnvckBCe3OjeR?= NG\DXWk1Njl2IN88US=> MVe3NkBp NGfrRYNqdmO{ZXHz[ZMheC2HUlugcIV3\Wy| M{X4ZVI1QDRyOEmx
PC9/GR M1LwSmZ2dmO2aX;uJGF{e2G7 M4XTdlQvQTRizszN NELMcZo4OiCq MorLbY5kemWjc3XzJJAuSUuWIHzleoVtew>? MnWxNlQ5PDB6OUG=
H28 NET3THFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S2dmlEPTB;MD6wO:KyOC5yMjFOwG0> M1fye|I1PzF2N{Ky
211H Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jLfWlEPTB;MD6wO:KyOC5yMTFOwG0> MVyyOFcyPDd{Mh?=
H2052 NHr4W3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwNUhCtVAvOzRizszN MlzSNlQ4OTR5MkK=
H2452 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XBZ2lEPTExvK6xNFAh|ryP NVrpbWxsOjR5MUS3NlI>
MES01 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfuTWM2OO,:nkGwNEDPxE1? MVGyOFcyPDd{Mh?=
MES04 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvwSY1FUUN3MP-8olExOCEQvF2= MlT4NlQ4OTR5MkK=
A549 MoPpR4VtdCCYaXHibYxqfHliQYPzZZk> MViwMlEwOC5|L{CuOU8yKM7:TR?= M2S4UlI1NzR6IHi= MXHEUXNQ MmTHbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? Ml7jNlQ3OjZ5MkK=
A549 M2rheGZ2dmO2aX;uJGF{e2G7 NWnod21xOC5zL{CuN{8xNjVxMTFOwG0> NFTMR2MzPC92ODDo NF3nTppFVVOR MlH2dJJw\HWlZYOgeIhmKG[xcn3heIlwdiCxZjDBWm9{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYeyOFYzPjd{Mh?=
H1993 NVvke|BGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnSUG1KSzVyPUCuNVch|ryP MkXKNlQ1OTh3MUm=
H1299 NIPDcHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFwOESg{txO NFnQW2szPDRzOEWxPS=>
H226 NVriPGY6S2WubDDWbYFjcWyrdImgRZN{[Xl? NGXZPZkyNTFyIN88[{9udA>? Mlj5O|IhcA>? NHPkRohKSzVyPkGwJO69\y:vbB?= MoDMNlQ{Pzh3N{[=
H290 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVyxMVExKM7:Zz;tcC=> M1f0b|czKGh? NVLnb4lOUUN3ME6xNEDPxGdxbXy= NFrzOWszPDN5OEW3Oi=>
Y-meso14 MoXtR4VtdCCYaXHibYxqfHliQYPzZZk> MY[xMVExKM7:Zz;tcC=> M4[zXlczKGh? MVLJR|UxRjFyIN88[{9udA>? MmDLNlQ{Pzh3N{[=
MSTO-211H MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NH7JUZkyNTFyIN88[{9udA>? MV[3NkBp MXnJR|UxhjBwMESg{txoN22u M2i5VFI1Ozd6NUe2
A549 MknUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjXPVYhcA>? MoDjTWM2OD1zLkO1JO69VQ>? M4\pTlI1OzR6OEW0
A549/PEM-1.6 NGHNOnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TkVlk3KGh? MWfJR|UxRTVwMEOg{txO MX6yOFM1QDh3NB?=
A549/PEM-6.4 NWHlWmh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XMflk3KGh? NUjjcoJ5UUN3ME2yN{4{QSEQvF2= NVvrU5A6OjR|NEi4OVQ>
A549/PEM-16 Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV32[I97QTZiaB?= M2i0TGlEPTB;NUGuOFUh|ryP M4CxfVI1OzR6OEW0
HT-29 NFjD[45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHIUppRPzMEoHlCpC=> M3nHeWROW00EoB?= MYPJR|UxRTFyLkC3JOKyKDBwOUSg{txO NVnHfZRZOjN7NUm0OlA>
LoVo NYnpdYpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fXU|czyqCqwrC= NILRb4lFVVORwrC= Ml\LTWM2OD1yLkCzNkDDuSByLkCwNkDPxE1? NHLwZ|UzOzl3OUS2NC=>
SW620 NI\COlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYC3NuKhcMLi NXvEXWhPTE2VT9Mg Mnj2TWM2OD1zLkC5JOKyKDBwMEGg{txO Mnu0NlM6PTl2NkC=
HCT116 MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr5O|LDqGkEoB?= MUjEUXNQyqB? NUjiPJRuUUN3ME2wMlA1QSEEsTCwMlAyOyEQvF2= Mnj3NlM6PTl2NkC=
SW1116 NHHxcZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe3NuKhcMLi M2WwOmROW00EoB?= MYXJR|UxRTFwN{CgxtEhOC5yMzFOwG0> NV2xZoVEOjN7NUm0OlA>
WiDr Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYS3NuKhcMLi NVmzVHVLTE2VT9Mg NX7oU4drUUN3ME2wMlAyQSEEsTCwMlAxOiEQvF2= M17vTVI{QTV7NE[w
HT-29 MWnGeY5kfGmxbjDBd5NigQ>? MlzINE4xPcLizszN M{e5T|czyqCq NXPqeWM3TE2VT9Mg MmHvbY5kemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJJRp\SCVIIDoZZNmyqB? MmrpNlM6PTl2NkC=
LoVo MmHLSpVv[3Srb36gRZN{[Xl? NWG3SY5KOC5yNdMg{txO NXvlSoVwPzMEoHi= MlK3SG1UV8Li NWi3dXNUcW6lcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKHSqZTDTJJBp[XOnwrC= Mlj0NlM6PTl2NkC=
STAV-AB MnrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2yNWE1QCCq NFr6UHBxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9OlQvPMLzMkGuPEAm NEe3RWszOzh2MEO3Oi=>
M-14-K NHX5bolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvabXJzPDhiaB?= NYHJWWpIeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVgyNjkEsUGyMlkhLQ>? NUL1Z2xWOjN6NECzO|Y>
STAV-FCS MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmX2OFghcA>? M1zPeZBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{24PE4yyrF6LkmgKS=> NXT1[odOOjN6NECzO|Y>
ZL-34 M{nxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL4VmNRPDhiaB?= MnzvdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUm1MlfDuTZwNTCl NF;jdJkzOzh2MEO3Oi=>
JL-1 NEfVepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV20PEBp NIWwbXlxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9PVgvOsLzMj6yJEU> NVK0UHFHOjN6NECzO|Y>
DM-3 M4LFZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:ySlQ5KGh? MXrwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;MUCxMlPDuTJwODCl NU\odXVTOjN6NECzO|Y>
Jurkat M1\lVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn0OFghcA>? M{CzOpBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{23Ok44yrF2LkOgKS=> NFPVSnUzOzh2MEO3Oi=>
BXPC-3 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTN7Lki2xtEyNjZ6IN88US=> NYLL[YRrOjJ7N{e2NFc>
PANC-1 NHnH[mdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLZfoRmUUN3ME24N{44PsLzMD6xPUDPxE1? MVqyNlk4PzZyNx?=
BXPC-3 NWP5OHE2TnWwY4Tpc44hSXO|YYm= M3i3fFM6Njh4IDFOwG0> M4HZVVI1KGh? NX[4bVlZcW6mdXPld{BUKGG{cnXzeEApWDxyLkC1LUBidmRiZHXjdoVie2W|IITo[UBvfW2kZYKgc4Yh[2WubIOgbY4hfGinIFeyM20heGijc3ZCpC=> MVKyNlk4PzZyNx?=
BXPC-3 M4PYUmZ2dmO2aX;uJGF{e2G7 M2S2[|M6Njh4IDFOwG0> NV3Vb4puOjRiaB?= NHvrUmFmdmijbnPld{BGT0[UIIDoc5NxcG:{eXzheIVlKGyndnXsd{wh[W6mIITo[UBxem:2ZXnuJIxmfmWuc9Mg NH36VJQzOjl5N{[wOy=>
PANC-1 MUPGeY5kfGmxbjDBd5NigQ>? MYe4OEDPxE1? M{\ZdFI1KGh? NEPwSldmdmijbnPld{BGT0[UIIDoc5NxcG:{eXzheIVlKGyndnXsd{wh[W6mIITo[UBxem:2ZXnuJIxmfmWuc9Mg NXHyXXVIOjJ7N{e2NFc>
BXPC-3 NV7P[2NnTnWwY4Tpc44hSXO|YYm= MoS4N|kvQDZiIN88US=> NGnwUG0zPCCq NU\ZVWdx\W6qYX7j[ZMhTUeIUjygTGVTOyCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= MVyyNlk4PzZyNx?=
PANC-1 MojnSpVv[3Srb36gRZN{[Xl? M2r3RVg1KM7:TR?= M2izb|I1KGh? NYXOdW05\W6qYX7j[ZMhTUeIUjygTGVTOyCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= M4rlOlIzQTd5NkC3

... 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.
  • 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
Smiles C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)NC(CCC(=O)[O-])C(=O)[O-].[Na+].[Na+]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Molecular Weight Calculator

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04173338 Recruiting Drug: Cabozantinib|Drug: Pemetrexed Non Small Cell Lung Cancer|Non-squamous Non-small-cell Lung Cancer|Urothelial Carcinoma|Malignant Mesothelioma Augusta University January 23 2020 Phase 1
NCT03023319 Recruiting Drug: Bosutinib|Drug: Pemetrexed Carcinoma Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Nagla Abdel Karim|Augusta University December 10 2019 Phase 1
NCT03298763 Recruiting Genetic: MSCTRAIL|Drug: Placebo Adenocarcinoma of Lung University College London March 5 2019 Phase 1|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.

Handling Instructions

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID