Pemetrexed (LY-231514) disodium

Catalog No.S1135

For research use only.

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.

Pemetrexed (LY-231514) disodium Chemical Structure

CAS No. 150399-23-8

Selleck's Pemetrexed (LY-231514) disodium has been cited by 39 publications

Purity & Quality Control

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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 NWH6bWE6TnWwY4Tpc44hSXO|YYm= NXXYXYlVQDRizszN NHe0[XIzPCCq NFTiT5VmdmijbnPld{BGT0[ULDDISXI{KGGwZDDBT3QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= MlzZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7N{e2NFcoRjJ{OUe3OlA4RC:jPh?=
BXPC-3 MmniSpVv[3Srb36gRZN{[Xl? M4DmTFM6Njh4IDFOwG0> M17EcVI1KGh? M{LYbYVvcGGwY3XzJGVITlJuIFjFVlMh[W6mIFHLWEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| M1XOT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUe3OlA4Lz5{Mkm3O|YxPzxxYU6=
PANC-1 NY\EfFNHTnWwY4Tpc44hSXO|YYm= NUDNNZFIQDRizszN M3HkclI1KGh? M3\4TYVvcGGwY3XzJGVITlJicHjvd5Bpd3K7bHH0[YQhdGW4ZXzzMEBidmRidHjlJJBzd3SnaX6gcIV3\Wy|wrC= MmK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7N{e2NFcoRjJ{OUe3OlA4RC:jPh?=
BXPC-3 M3G5VGZ2dmO2aX;uJGF{e2G7 NIjyUJU{QS56NjCg{txO MkHSNlQhcA>? Mnza[Y5p[W6lZYOgSWdHWiCyaH;zdIhwenmuYYTl[EBt\X[nbIOsJIFv\CC2aHWgdJJwfGWrbjDs[ZZmdHQEoB?= M4XUTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUe3OlA4Lz5{Mkm3O|YxPzxxYU6=
BXPC-3 NWjFOoNXTnWwY4Tpc44hSXO|YYm= M2\6ZVM6Njh4IDFOwG0> M13RfVI1KGh? MXnpcoR2[2W|IGOgZZJz\XO2IDjQQFAvODVrIHHu[EBl\WO{ZXHz[ZMhfGinIH71cYJmeiCxZjDj[YxteyCrbjD0bIUhTzJxTTDwbIF{\cLi NYLZZ2xKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5O|c3ODdpPkKyPVc4PjB5PD;hQi=>
PANC-1 NWPOb3FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrtRnZKSzVyPUizMlc3yrFyLkG5JO69VQ>? MnTCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7N{e2NFcoRjJ{OUe3OlA4RC:jPh?=
BXPC-3 Ml;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X4d2lEPTB;M{muPFbDuTFwNkig{txO Mof4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7N{e2NFcoRjJ{OUe3OlA4RC:jPh?=
Jurkat MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWK0PEBp MXTwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;N{[uO:KyPC5|IDW= M32ydFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OESwN|c3Lz5{M{i0NFM4PjxxYU6=
DM-3 NUO0dndyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:0PEBp NGOxWXRxem:yb4L0bY9vKG:oIHzpeoUh[2WubIO9NVAyNjQEsUKuPEAm MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2MEO3Okc,OjN6NECzO|Y9N2F-
JL-1 M3u1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLUOFghcA>? NVKxXndoeHKxcH;yeIlwdiCxZjDsbZZmKGOnbHzzQVk5NjMEsUKuNkAm NUDxRVZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFA{PzZpPkKzPFQxOzd4PD;hQi=>
ZL-34 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGj6e3c1QCCq MXTwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OUWuO:KyPi53IDW= NHL2V|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0NFM4Pid-MkO4OFA{PzZ:L3G+
STAV-FCS MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XodlQ5KGh? MXXwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OEiuNeKyQC57IDW= NVPqN2NTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFA{PzZpPkKzPFQxOzd4PD;hQi=>
M-14-K M135O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnWOFghcA>? MWTwdo9xd3K2aX;uJI9nKGyrdnWgZ4VtdHN;OEGuPOKyOTJwOTCl MmXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NECzO|YoRjJ|OESwN|c3RC:jPh?=
STAV-AB NH3jRodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP3OFghcA>? MonDdJJweG:{dHnvckBw\iCuaY\lJINmdGy|PU[0MlTDuTJzLkigKS=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2MEO3Okc,OjN6NECzO|Y9N2F-
LoVo MVvGeY5kfGmxbjDBd5NigQ>? NYDrWYxYOC5yNdMg{txO MYq3NuKhcA>? MYjEUXNQyqB? MlrybY5kemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJJRp\SCVIIDoZZNmyqB? M4[wW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW5OFYxLz5{M{m1PVQ3ODxxYU6=
HT-29 MXjGeY5kfGmxbjDBd5NigQ>? NHHTXHExNjB3wrFOwG0> MXS3NuKhcA>? NX3iZ4pJTE2VT9Mg NE\0O2RqdmO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hfGinIGOgdIhie2YEoB?= Mm\BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUm0OlAoRjJ|OUW5OFYxRC:jPh?=
WiDr M13Yb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDnN404OsLiaNMg NX7xeo5[TE2VT9Mg Mo\CTWM2OD1yLkCxPUDDuSByLkCwNkDPxE1? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3OUS2NEc,OjN7NUm0OlA9N2F-
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HCT116 NYLjUoY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW3NuKhcMLi MXXEUXNQyqB? M1nGT2lEPTB;MD6wOFkhyrFiMD6wNVMh|ryP MnrFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUm0OlAoRjJ|OUW5OFYxRC:jPh?=
SW620 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPaO|LDqGkEoB?= MmDySG1UV8Li NXi0[oY5UUN3ME2xMlA6KMLzIECuNFEh|ryP NVLnd|RERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OVk1PjBpPkKzPVU6PDZyPD;hQi=>
LoVo NYHqTpBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX23NuKhcMLi NELuOlVFVVORwrC= MlzGTWM2OD1yLkCzNkDDuSByLkCwNkDPxE1? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3OUS2NEc,OjN7NUm0OlA9N2F-
HT-29 M4DaSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVz4TXRDPzMEoHlCpC=> NF3EZpBFVVORwrC= NXXQcWZKUUN3ME2xNE4xPyEEsTCwMlk1KM7:TR?= NHXSRVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m1PVQ3OCd-MkO5OVk1PjB:L3G+
A549/PEM-16 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknqPVYhcA>? M2\uUGlEPTB;NUGuOFUh|ryP NX72NFBZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFg5PTRpPkK0N|Q5QDV2PD;hQi=>
A549/PEM-6.4 M4jadGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHmT5U6PiCq NWnjepZZUUN3ME2yN{4{QSEQvF2= MlnmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEi4OVQoRjJ2M{S4PFU1RC:jPh?=
A549/PEM-1.6 NF3lNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvHPVYhcA>? NIr5XXpKSzVyPUWuNFMh|ryP MlztQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NEi4OVQoRjJ2M{S4PFU1RC:jPh?=
A549 M1\5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\mUoZGQTZiaB?= M{TuS2lEPTB;MT6zOUDPxE1? NGXIOo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO0PFg2PCd-MkSzOFg5PTR:L3G+
MSTO-211H MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MX2xMVExKM7:Zz;tcC=> NVrBTY1GPzJiaB?= M1\BZWlEPTC-MD6wOEDPxGdxbXy= NXHncGN4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzO|g2PzZpPkK0N|c5PTd4PD;hQi=>
Y-meso14 NVTRc2M2S2WubDDWbYFjcWyrdImgRZN{[Xl? M{DFSFEuOTBizsznM41t NWrjdIZRPzJiaB?= MkLsTWM2OD5zMDFOwIcwdWx? NXLmc45ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzO|g2PzZpPkK0N|c5PTd4PD;hQi=>
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H226 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYKxMVExKM7:Zz;tcC=> NF3VSYk4OiCq NX[xfXNFUUN3ME6xNEDPxGdxbXy= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN5OEW3Okc,OjR|N{i1O|Y9N2F-
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H1993 M1m5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q0WWlEPTB;MD6xO{DPxE1? MnfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUi1NVkoRjJ2NEG4OVE6RC:jPh?=
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MES01 M3HrdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLzVYxiUUN3MP-8olExOCEQvF2= NX\UV5lyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3NVQ4OjJpPkK0O|E1PzJ{PD;hQi=>
H2452 NHj1NVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjOTWM2OO,:nkGwNEDPxE1? M{ftZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{G0O|IzLz5{NEexOFczOjxxYU6=
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PC9/GR NWjvN5lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrOOWE4OiCq MWrJR|UxRTRwOUVCtVAvPDRyIN88US=> MoPJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NEC4PVEoRjJ2OESwPFkyRC:jPh?=
PC9 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPGO2xEPzJiaB?= MVnJR|UxRTF4LkC1xtEyNjh3IH7N MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh2MEi5NUc,OjR6NEC4PVE9N2F-
A549 NXPUUo1tTnWwY4Tpc44hSXO|YYm= MoXuNE4yNzBwMz:xJO69VQ>? MnrQOFghcA>? MV;pcoNz\WG|ZYOgeIhmKHKjdHnvJI9nKFNvcHjhd4UheG:ydXzheIlwdg>? M1LHS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OES3PFY{Lz5{NEi0O|g3OzxxYU6=
A549 MXHBdI9xfG:|aYOgRZN{[Xl? MU[wMlEwOC5|L{Gg{txO NHfjZnc1QCCq NEPV[|NqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MlnxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NEe4OlMoRjJ2OES3PFY{RC:jPh?=
A549 MWPGeY5kfGmxbjDBd5NigQ>? NHfQR3YxNjFxMD6zM|Eh|ryP MWW0PEBp M4Cxb4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZicHjvd5Bpd3K7bHH0[YQhSWu2IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MkXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NEe4OlMoRjJ2OES3PFY{RC:jPh?=
A549 MUjGeY5kfGmxbjDBd5NigQ>? NWDJeIJFOSEEtV2= NEnkR3o1NzhxMUKvNlQwPDhiaB?= NULvUnNZcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwbI9{eGixconsZZRm\CCDa4SgbY4h[SC2aX3lJIRmeGWwZHXueEBu[W6wZYK= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh2N{i2N{c,OjR6NEe4OlM9N2F-
A549 MUjGeY5kfGmxbjDBd5NigQ>? M4j6flUh|ryP M3X2S|ghcA>? M3;VUIlv[3KnYYPld{BO[2xvMTD1ZolyfWm2aX7heIlwdiCuZY\lcJM> NFnsTZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm5NVc3QCd-MkS5PVE4Pjh:L3G+
A549 M1Ozb2Fxd3C2b4Ppd{BCe3OjeR?= MWKyMlUh|ryP MVm0PEBp MVHpcoR2[2W|IHHwc5B1d3Orcx?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl7MUe2PEc,OjR7OUG3Olg9N2F-
H1792 MnPPSpVv[3Srb36gRZN{[Xl? NVnrZ2t[Oi53L{WvNVAh|ryP NYHP[29FPDhiaB?= MWnkc5dvemWpdXzheIV{KE2lbD2xxsA> Mon2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7OUG3OlgoRjJ2OUmxO|Y5RC:jPh?=
A549  MYfGeY5kfGmxbjDBd5NigQ>? MYWyMlUwPS9zMDFOwG0> NXn5Nm1FPDhiaB?= MUXkc5dvemWpdXzheIV{KE2lbD2xxsA> NVvoW|VvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5PVE4PjhpPkK0PVkyPzZ6PD;hQi=>
H1792 MnfTSpVv[3Srb36gRZN{[Xl? NX\Q[HRMOi53IN88US=> MmPZOFghcA>? NX3CbGNwcW6mdXPld{Bk[XOyYYPlMVktKGOjc4Dhd4UuOyCjbnSgdI9tgSBqQVTQMZJq[m:|ZTmgdI9tgW2ncnHz[UApWEGUUDmgZ4xm[X[jZ3W= NUK3[FNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5PVE4PjhpPkK0PVkyPzZ6PD;hQi=>
A549  NX7LXpFTTnWwY4Tpc44hSXO|YYm= MUWyMlUh|ryP MkjlOFghcA>? MVTpcoR2[2W|IHPhd5Bie2VvOTygZ4F{eGG|ZT2zJIFv\CCyb3z5JEhCTFBvcnnic5NmMSCyb3z5cYVz[XOnIDjQRXJRMSClbHXheoFo\Q>? M1;RcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUmxO|Y5Lz5{NEm5NVc3QDxxYU6=
H1792 NFXXOGhHfW6ldHnvckBCe3OjeR?= MW[yMlUwPS9zMDFOwG0> NIXJSlQ1QCCq M1rSNolv[3KnYYPld{BPd3ijIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl7MUe2PEc,OjR7OUG3Olg9N2F-
A549  MULGeY5kfGmxbjDBd5NigQ>? MoH2Nk42NzVxMUCg{txO NY\HdnF[PDhiaB?= NYfrTI5qcW6lcnXhd4V{KE6xeHGg[ZhxemW|c3nvckB{cWewaX\pZ4FvfGy7 NGiwUYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm5NVc3QCd-MkS5PVE4Pjh:L3G+
A549 NUHJPYk5TnWwY4Tpc44hSXO|YYm= MkPmNUDPxE1? MVW0PEBp M{O5boxm[WS|IITvJI1qfG:laH;u[JJq[WxiZInz[pVv[3Srb36gZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= NXHRSYliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVY6QTNpPkK1NFk3QTl|PD;hQi=>
MSTO-211 MX3GeY5kfGmxbjDBd5NigQ>? M2TL[|Eh|ryP M4nIN|Q5KGh? MlOxcIVi\HNidH:gcYl1d2Oqb37kdolidCCmeYPmeY5kfGmxbjDjc41jcW6nZDD3bZRpKHOrbY\hd5RifGmw NVv6cYQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVY6QTNpPkK1NFk3QTl|PD;hQi=>
A549 NHTzTm1HfW6ldHnvckBCe3OjeR?= MlLkNUDPxE1? NXTCWpZPPDhiaB?= MmrI[Y5p[W6lZYOgbY51emGlZXzseYxieiCUT2OgdJJw\HWldHnvckBkd22kaX7l[EB4cXSqIIPpcZZie3SjdHnu NHjJTJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5Olk6Oyd-MkWwPVY6QTN:L3G+
MSTO-211 NYnLXmRqTnWwY4Tpc44hSXO|YYm= M1XvZlEh|ryP NXzCdW1XPDhiaB?= M{HBfoVvcGGwY3XzJIlvfHKjY3XscJVt[XJiUl;TJJBzd2S3Y4Tpc44h[2:vYnnu[YQhf2m2aDDzbY13[XO2YYTpci=> NUTrfZo6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVY6QTNpPkK1NFk3QTl|PD;hQi=>
A549 MknQRZBweHSxc3nzJGF{e2G7 MV2xJO69VQ>? NUD2Oos1PDhiaB?= NXjDV3FF\W6qYX7j[ZMh[2G|cHHz[U1l\XCnbnTlcpQh[XCxcITvd4l{KGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> NGG3V4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5Olk6Oyd-MkWwPVY6QTN:L3G+
MSTO-211 MkDKRZBweHSxc3nzJGF{e2G7 MUCxJO69VQ>? M1nPXFQ5KGh? NVW5bGFC\W6qYX7j[ZMh[2G|cHHz[U1l\XCnbnTlcpQh[XCxcITvd4l{KGOxbXLpcoVlKHerdHigd4lufmG|dHH0bY4> MknGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOU[5PVMoRjJ3MEm2PVk{RC:jPh?=
A549 M4LPV2NmdGxiVnnhZoltcXS7IFHzd4F6 MlfxNUDPxE1? NGnJUms1QCCq NFTPW2xxem:mdXPld{BiKHO7bnXy[4l{fGmlIHnubIljcXSxcomg[YZn\WO2IH;uJJRp\SClZXzsJIdzd3e2aDDjc41jcW6nZDD3bZRpKHOrbY\hd5RifGmw NUjCOXNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPVY6QTNpPkK1NFk3QTl|PD;hQi=>
MSTO-211 Mnf6R4VtdCCYaXHibYxqfHliQYPzZZk> NV\ZblBPOSEQvF2= NXHqWpN1PDhiaB?= NVTy[Fk2eHKxZIXj[ZMh[SC|eX7ldodqe3SrYzDpcohq[mm2b4L5JIVn\mWldDDvckB1cGViY3XscEBoem:5dHigZ49u[mmwZXSge4l1cCC|aX32ZZN1[XSrbh?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7Nkm5N{c,OjVyOU[5PVM9N2F-
H1299 MmXLR4VtdCCYaXHibYxqfHliQYPzZZk> MonjNU0yODByIH7N M4jUS|czKGh? MULJR|UxRTF5ODDuUS=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF2NU[2PUc,OjVzNEW2Olk9N2F-
A549 NWLobnE{S2WubDDWbYFjcWyrdImgRZN{[Xl? NH3ueVcyNTFyMECgcm0> MUS3NkBp M2T4ZmlEPTB;MUO3JI5O Mk\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzNEW2OlkoRjJ3MUS1OlY6RC:jPh?=
MG-63 NH\JRXVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYewMlAyNTFyMDFOwG0> NEfyb5E4OiCq MXvpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4Pl[IVx\W6mZX70cJk> NEHZVII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG1NlM6QSd-MkWxOVI{QTl:L3G+
U20S Mo\SR4VtdCCYaXHibYxqfHliQYPzZZk> M4LxT|AvODFvMUCwJO69VQ>? NIDDSnQ4OiCq M4jMR4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Vl\XCnbnTlcpRtgQ>? NICyc5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG1NlM6QSd-MkWxOVI{QTl:L3G+
HepG3 MYTGeY5kfGmxbjDBd5NigQ>? NIrWcZcyOMLizszN MmPkOFghcA>? M1;jZ5VxemWpdXzheIV{KHCqb4PwbI9zgWyjdHXkJEhxNSliTVXLNU8zKCiVZYKyNVcwOjJzKTDhcoQheC2HUluxM|IhMFSqckKwNk9VgXJ{MESp MnHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NE[xNFIoRjJ3NES2NVAzRC:jPh?=
HepG3 MmjzSpVv[3Srb36gRZN{[Xl? NUnXTnEyOC5z4pETNVAxyqEQvF2= MWC0PEBp NXzSc5F7[WO2aY\heIV{KGO7dH:tdJJwfGWldHn2[UBifXSxcHjh[5nDqA>? NX[0SohyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OFYyODJpPkK1OFQ3OTB{PD;hQi=>
HepG3 MlfXSpVv[3Srb36gRZN{[Xl? Mke0NE4y6oDVMUCwxsDPxE1? MV20PEBp NH3DU2NqdmS3Y3XzJJA3OiCmb4fudoVofWyjdHnvckBieyC5ZXzsJIF{KEKnY3zpck0yKGGwZDDMR|NDNUmLIIXwdoVofWyjdHnvci=> NY\nRopZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OFYyODJpPkK1OFQ3OTB{PD;hQi=>
HepG2 MnWwRZBweHSxc3nzJGF{e2G7 NFLCboExNjIkgKOxNFDDqM7:TR?= Mn\DO|IhcA>? NVf6e45ncW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJkh[XRiaHnnbEBkd26lZYLueJJifGmxbh?= NG\ZSY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS0OlExOid-MkW0OFYyODJ:L3G+
HepG2 NX74NWw6S2WubDDWbYFjcWyrdImgRZN{[Xl? MnfFNE4y6oDVMUCwxsDPxE1? M1nPXlczKGh? NWjWNmlRcGmpaDDjc45k\W62cnH0bY9veyCxZjDw[Y1mfHKneHXkJIF1KChzMD:xNFDDqM7:TTmgc45tgSC|bHnnbJRtgSCrbnjpZol1eyCKZYDHNkBk\WyuIIP1dpZqfmGu MoDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NE[xNFIoRjJ3NES2NVAzRC:jPh?=
A459 NFXTUWxCeG:ydH;zbZMhSXO|YYm= NFf2b4Q1|ryP MlzIOFghcA>? MWXpcoR2[2W|IHHwc5B1d3Orcx?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2M{iyNkc,OjV5NEO4NlI9N2F-
A459 M17rS2Z2dmO2aX;uJGF{e2G7 NWD0PHloOS9{L{Sg{txO MnvuOFghcA>? MVzk[YNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyLVHreC=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2M{iyNkc,OjV5NEO4NlI9N2F-
A459 NGX3Z|hHfW6ldHnvckBCe3OjeR?= MYSxM|IwPCEQvF2= Mlz3NlQwPDhiaB?= MnGwbY5lfWOnczDHNUBxcGG|ZTDhdpJme3RiaX6g[I9{\S1iYX7kJJRqdWViZHXw[Y5l\W62IH3hco5meg>? MlnIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEO4NlIoRjJ3N{SzPFIzRC:jPh?=
T47D MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jp[lAvOjN2wrDtUS=> M4rrelczKGh? NE\FZ5poem:5dHigbY5pcWKrdHnvcl0{OO,7qh?= NEW3eos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm3OVY{Pyd-MkW5O|U3Ozd:L3G+
HeLa M4jo[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3RUJMxNjJ|NNMgcW0> MWC3NkBp NUPNNZpz\3Kxd4ToJIlvcGmkaYTpc44:OjExubq= NX:3XW9vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|U3OzdpPkK1PVc2PjN5PD;hQi=>
A549 Mn7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTm[21XOC5{M{VCpI1O Mnf5O|IhcA>? MVLndo94fGhiaX7obYJqfGmxbk21NQ+6sg>? NXS0eGl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|U3OzdpPkK1PVc2PjN5PD;hQi=>
Vero MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2wMlI{PMLibV2= Mk\lO|IhcA>? M{H1codzd3e2aDDpcohq[mm2aX;uQVIx97ns MmnoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7N{W2N|coRjJ3OUe1OlM4RC:jPh?=
T47D NG\QPWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTJW3lDOC5{M{VCpI1O M2KxdlQ5KGh? MWfndo94fGhiaX7obYJqfGmxbk2yNQ+6sg>? Mne5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7N{W2N|coRjJ3OUe1OlM4RC:jPh?=
HeLa MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDHNE4zOzUEoH3N MV20PEBp MnfC[5Jwf3SqIHnubIljcXSrb369NVDwwap? M{KyS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe1OlM4Lz5{NUm3OVY{PzxxYU6=
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TC32 MXrxTHRUKGG|c3H5 NE\XOY1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?= NHG0fJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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SK-N-MC MnvhdWhVWyCjc4PhfS=> M3rl[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NXzsfJhkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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IGROV1 MX7GeY5kfGmxbjDhd5NigQ>? NVnjcWRJTW[oZXP0JI9vKFSVIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBpfW2jbjDJS3JQXjFiY3XscJMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB|NUW0NUc,OzByM{W1OFE9N2F-
IGROV1 NYK1ZpRXTnWwY4Tpc44h[XO|YYm= M1qwc2Vn\mWldDDvckBFUE[UIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBpfW2jbjDJS3JQXjFiY3XscJMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NEj3[W89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOVU1OSd-M{CwN|U2PDF:L3G+
IGROV1 Ml\QSpVv[3Srb36gZZN{[Xl? MULF[oZm[3Rib36gTHNRQTBicILveIVqdiCneIDy[ZN{cW:wIHnuJIh2dWGwIFnHVm9XOSClZXzsd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB|NUW0NUc,OzByM{W1OFE9N2F-
Assay
Methods Test Index PMID
Western blot p-Chk1 / Chk1 / Cyclin D / Cyclin E / p-Histone H3 / Histone H3 / Cyclin B1 / p-Cdc2 / Cdc2 ; Topo IIα / Topo I / γH2AX / Cleaved PARP / Survivin ; AKT / p-AKT / GSK3β / p-GSK3β ; EGFR / p-EGFR 22237209 24847863 30953548
Immunofluorescence p-AKT 24847863
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[3]
  • 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.

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

Chemical Information

Molecular Weight 471.37
Formula

C20H19N5Na2O6

CAS No. 150399-23-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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