Pemetrexed (LY-231514) disodium

For research use only.

Catalog No.S1135

33 publications

Pemetrexed (LY-231514) disodium Chemical Structure

CAS No. 150399-23-8

Pemetrexed (LY-231514) disodium 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.

Selleck's Pemetrexed (LY-231514) disodium has been cited by 33 publications

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Choose Selective DHFR Inhibitors

Biological Activity

Description Pemetrexed (LY-231514) disodium 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
PANC-1 NEjYVWxHfW6ldHnvckBCe3OjeR?= NYO3[3RmQDRizszN MW[yOEBp M4rBNIVvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl5N{[wO{c,OjJ7N{e2NFc9N2F-
BXPC-3 M3XCR2Z2dmO2aX;uJGF{e2G7 M2[xfVM6Njh4IDFOwG0> NX7FTnBJOjRiaB?= MWflcohidmOnczDFS2ZTNCCKRWKzJIFv\CCDS2SgdIhwe3Cqb4L5cIF1cW:wIHzleoVtew>? NGfQc4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm3O|YxPyd-MkK5O|c3ODd:L3G+
PANC-1 NGLybHlHfW6ldHnvckBCe3OjeR?= MlTxPFQh|ryP NHezN40zPCCq MUHlcohidmOnczDFS2ZTKHCqb4PwbI9zgWyjdHXkJIxmfmWuczygZY5lKHSqZTDwdo91\WmwIHzleoVte8Li NVHWb2dLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5O|c3ODdpPkKyPVc4PjB5PD;hQi=>
BXPC-3 NEKy[GVHfW6ldHnvckBCe3OjeR?= NGjwV2k{QS56NjCg{txO M4Xkd|I1KGh? NW\iOYtH\W6qYX7j[ZMhTUeIUjDwbI9{eGixconsZZRm\CCuZY\lcJMtKGGwZDD0bIUheHKxdHXpckBt\X[nbIRCpC=> NWjpZ2ZbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5O|c3ODdpPkKyPVc4PjB5PD;hQi=>
BXPC-3 Ml\PSpVv[3Srb36gRZN{[Xl? MWKzPU45PiBizszN MYSyOEBp MmDsbY5lfWOnczDTJIFzemW|dDCoVFwxNjB3KTDhcoQh\GWlcnXhd4V{KHSqZTDueY1j\XJib3[gZ4VtdHNiaX6geIhmKEd{L12gdIhie2YEoB?= NWnK[JJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5O|c3ODdpPkKyPVc4PjB5PD;hQi=>
PANC-1 NXrFdHdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlewTWM2OD16Mz63OuKyOC5zOTFOwG0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl5N{[wO{c,OjJ7N{e2NFc9N2F-
BXPC-3 NWHVSIJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTN7Lki2xtEyNjZ6IN88US=> NEHxcmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm3O|YxPyd-MkK5O|c3ODd:L3G+
Jurkat M4rLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3nWJk1QCCq M37nOZBzd3CxcoTpc44hd2ZibHn2[UBk\Wyuc{23Ok44yrF2LkOgKS=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2MEO3Okc,OjN6NECzO|Y9N2F-
DM-3 M3;T[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P1flQ5KGh? NFXhUoRxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9NVAyNjQEsUKuPEAm NVvHTZF6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFA{PzZpPkKzPFQxOzd4PD;hQi=>
JL-1 NV;icoxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS2fGdvPDhiaB?= NV3EbIhFeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVk5NjMEsUKuNkAm NVPyenFkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFA{PzZpPkKzPFQxOzd4PD;hQi=>
ZL-34 NWjVPJhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nvXVQ5KGh? MYPwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OUWuO:KyPi53IDW= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2MEO3Okc,OjN6NECzO|Y9N2F-
STAV-FCS MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr4SGhxPDhiaB?= MmXHdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUi4MlHDuThwOTCl M4PHc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OESwN|c3Lz5{M{i0NFM4PjxxYU6=
M-14-K MnOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm0PEBp MoLhdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PUixMljDuTF{LkmgKS=> NEDSWXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0NFM4Pid-MkO4OFA{PzZ:L3G+
STAV-AB MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3NWoc1QCCq NYLUcJZZeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVY1NjUEsUKxMlghLQ>? Mn;DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NECzO|YoRjJ|OESwN|c3RC:jPh?=
LoVo NInBOHlHfW6ldHnvckBCe3OjeR?= NF[0fZYxNjB3wrFOwG0> MkfQO|LDqGh? MXzEUXNQyqB? NGHF[GJqdmO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hfGinIGOgdIhie2YEoB?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3OUS2NEc,OjN7NUm0OlA9N2F-
HT-29 NUH2[JhyTnWwY4Tpc44hSXO|YYm= MlLrNE4xPcLizszN NFnjeo04OsLiaB?= NWjvbGNRTE2VT9Mg NHX1XHVqdmO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hfGinIGOgdIhie2YEoB?= M2TYWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW5OFYxLz5{M{m1PVQ3ODxxYU6=
WiDr NX\yUJVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVu3NuKhcMLi NYDuO|FJTE2VT9Mg MlL1TWM2OD1yLkCxPUDDuSByLkCwNkDPxE1? MnjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUm0OlAoRjJ|OUW5OFYxRC:jPh?=
SW1116 MnPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nN[VczyqCqwrC= M{f5XWROW00EoB?= NUTNUJBmUUN3ME2xMlcxKMLzIECuNFMh|ryP NIHBO4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m1PVQ3OCd-MkO5OVk1PjB:L3G+
HCT116 Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37XbVczyqCqwrC= M1fHXWROW00EoB?= MojhTWM2OD1yLkC0PUDDuSByLkCxN{DPxE1? M2H3Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW5OFYxLz5{M{m1PVQ3ODxxYU6=
SW620 NFvZUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnZOZZsPzMEoHlCpC=> MX\EUXNQyqB? NVTyXZVWUUN3ME2xMlA6KMLzIECuNFEh|ryP MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3OUS2NEc,OjN7NUm0OlA9N2F-
LoVo NXvKWm1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HxU|czyqCqwrC= NG\BdoZFVVORwrC= MWrJR|UxRTBwMEOyJOKyKDBwMECyJO69VQ>? M{XBZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW5OFYxLz5{M{m1PVQ3ODxxYU6=
HT-29 Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;5ZlczyqCqwrC= NVXG[JZGTE2VT9Mg MXrJR|UxRTFyLkC3JOKyKDBwOUSg{txO MnzJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUm0OlAoRjJ|OUW5OFYxRC:jPh?=
A549/PEM-16 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PZRVk3KGh? NFjPbpRKSzVyPUWxMlQ2KM7:TR?= NVfiXlRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFg5PTRpPkK0N|Q5QDV2PD;hQi=>
A549/PEM-6.4 M1y2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXYPVYhcA>? NXXt[FR[UUN3ME2yN{4{QSEQvF2= NWGxVFhERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFg5PTRpPkK0N|Q5QDV2PD;hQi=>
A549/PEM-1.6 Ml2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HRdFk3KGh? MlK0TWM2OD13LkCzJO69VQ>? NITNenc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0PFg2PCd-MkSzOFg5PTR:L3G+
A549 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS1PVYhcA>? M2DlTWlEPTB;MT6zOUDPxE1? Ml\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEi4OVQoRjJ2M{S4PFU1RC:jPh?=
MSTO-211H MlPyR4VtdCCYaXHibYxqfHliQYPzZZk> NEX6blkyNTFyIN88[{9udA>? NVnT[GQxPzJiaB?= NInjRo5KSzVyfkCuNFQh|rypL33s MlvMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|N{i1O|YoRjJ2M{e4OVc3RC:jPh?=
Y-meso14 NFHV[|BE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGeySWMyNTFyIN88[{9udA>? MUW3NkBp MkH2TWM2OD5zMDFOwIcwdWx? NWrjWGpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzO|g2PzZpPkK0N|c5PTd4PD;hQi=>
H290 M33qe2NmdGxiVnnhZoltcXS7IFHzd4F6 NFjJb5kyNTFyIN88[{9udA>? NUe2c49KPzJiaB?= NGTJfnFKSzVyPkGwJO69\y:vbB?= MlvjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|N{i1O|YoRjJ2M{e4OVc3RC:jPh?=
H226 M{HOR2NmdGxiVnnhZoltcXS7IFHzd4F6 MlPxNU0yOCEQvHevcYw> M1HJVlczKGh? M3rJe2lEPTB-MUCg{txoN22u MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN5OEW3Okc,OjR|N{i1O|Y9N2F-
H1299 NV60bmpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFwOESg{txO NIjNZ|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxPFUyQSd-MkS0NVg2OTl:L3G+
H1993 NHfEdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1WxTGlEPTB;MD6xO{DPxE1? NGXDbWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxPFUyQSd-MkS0NVg2OTl:L3G+
A549 M3;DRmZ2dmO2aX;uJGF{e2G7 NYniUWZ[OC5zL{CuN{8xNjVxMTFOwG0> MX6yOE81QCCq Mn;JSG1UVw>? NF7kT5Fxem:mdXPld{B1cGViZn;ycYF1cW:wIH;mJGFXV3NiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIH5S2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[yOlczOid-MkS2NlY4OjJ:L3G+
A549 NHKwZnFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXWwMlEwOC5|L{CuOU8yKM7:TR?= MnvyNlQwPDhiaB?= NUPkOHo4TE2VTx?= NFzHUpNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NY\vSYpSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NlY4OjJpPkK0OlI3PzJ{PD;hQi=>
MES04 M{jsN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrzeYVKSzVy78{eNVAxKM7:TR?= MnHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5MUS3NlIoRjJ2N{G0O|IzRC:jPh?=
MES01 MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XyeWlEPTExvK6xNFAh|ryP MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDdzNEeyNkc,OjR5MUS3NlI9N2F-
H2452 MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\mS2lEPTExvK6xNFAh|ryP M4PaVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{G0O|IzLz5{NEexOFczOjxxYU6=
H2052 NH7x[JJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDvOIJKSzVyPUCuOVfDuTBwM{Sg{txO MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDdzNEeyNkc,OjR5MUS3NlI9N2F-
211H MnvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;PTZNKSzVyPUCuNFfDuTBwMEGg{txO M13vXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{G0O|IzLz5{NEexOFczOjxxYU6=
H28 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17IU2lEPTB;MD6wO:KyOC5yMjFOwG0> MljHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5MUS3NlIoRjJ2N{G0O|IzRC:jPh?=
PC9/GR MlXxSpVv[3Srb36gRZN{[Xl? MoGxOE46PCEQvF2= NVrJ[3czPzJiaB?= NGfOT2RqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy| NXHXRZRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OFA5QTFpPkK0PFQxQDlzPD;hQi=>
PC9/GR NIrKe2lHfW6ldHnvckBCe3OjeR?= MmfIOE46PCEQvF2= M2TZdVczKGh? M3ruT4lv[3KnYYPld{BxNUWUSzDs[ZZmdHN? M2f4PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OESwPFkyLz5{NEi0NFg6OTxxYU6=
PC9/GR Mo\PRZBweHSxc3nzJGF{e2G7 NX\rOIFNPC57NDFOwG0> NYPLb3R{PzJiaB?= M3XLeIlv\HWlZYOgNVkvPTUxubqgZZBweHSxc3nz MnLZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NEC4PVEoRjJ2OESwPFkyRC:jPh?=
PC9 NFq2dVBCeG:ydH;zbZMhSXO|YYm= NELWZ2EyPiCwTR?= MUW3NkBp NFf3fpBqdmS3Y3XzJFE1NjV278oqJIFxd3C2b4Ppdy=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh2MEi5NUc,OjR6NEC4PVE9N2F-
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... 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 N/A
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)

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    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID