Catalog No.S1192 Synonyms: ZD-1694

Raltitrexed Chemical Structure

Molecular Weight(MW): 458.49

Raltitrexed is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.

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In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
USD 470 In stock
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Cited by 5 Publications

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  • Fig. 1. Raltitrexed dose-response curve. HEK293 parental and MRP5 transfected cells were plated in a 96-well plate at a density of 4000 cells/well in complete DMEM (10% FBS, 1% Pencillin/streptomycin) and allowed to incubate for 24h at 37°C,  5% CO2. Raltirexed was added and the cells allowed to incubate for 72h. Total DNA present in each well was then quantified using Cyquant® cell proliferation assay. Results show Total DNA as % of the DMSO-only control wells. Experiment was done in triplicate.

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Biological Activity

Description Raltitrexed is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.
In vitro

Raltitrexed induces a concentration-dependent amount of double-stranded DNA breaks. Raltitrexed increases the level of Bax protein up to a factor 5 in the Lovo and LS174T cell lines containing wt p53. [1] Raltitrexed leads to an increase of intracellular phosphoribosyl pyrophosphate (PRPD) in the case of the HCT-8 cell line, which suggests that the cytotoxic effects of raltitrexed combined with 5-FU may be due to the increased formation of 5-FU nucleotides. [2] Raltitrexed combined with SN-38 results in synergistic cytotoxicity at broad dose-effect ranges in human colon cancer cells. [3] Raltitrexed is actively taken up into cells and then undergoes rapid, extensive metabolism to a series of polyglutamates, which results in potent thymidylate synthase inhibition. Raltitrexed is delivered to the brain very quickly, and could be detected at 5 min in all brain tissues. [4] Raltitrexed combined folinic acid (5FU-FA) shows a clear schedule-dependent synergistic antiproliferative interaction as demonstrated by calculating combination indexes. Raltitrexed combined with Vorinostat produces synergistic effect paralleled by evident cell cycle perturbations with major S-phase arrest. [5] Raltitrexed is a specific, folate-based inhibitor of thymidylate synthase with activity in advanced colorectal cancer comparable with that of fluorouracil (5-fluorouracil) plus folinic acid. Raltitrexed‘s activity is enhanced by rapid cellular entry and polyglutamation, with the polyglutamated derivatives having approximately 100-fold greater inhibitory potency than the parent compound. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human KB cells M2XCdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFvnN2U6PiCq MlTHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGK7IFPlcIx1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> MXyyOVI{PDF{OB?=
PC43-10 cells NXnOT21qTnWwY4Tpc44h[XO|YYm= M2CwWFk3KGh? MUjJcohq[mm2aX;uJI9nKFKIQzCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBEcGmwZYPlJIhidXO2ZYKgVGM1Oy1zMDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGmwY4XiZZRm\CC3cDD0c{A6PiCqcoOgZpkhS2WubITpeIVzNWKudXWgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4{KG6P NX;MU5NOOjV{M{SxNlg>
L1210 cell line NY[zWpdCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXO2bmIzT3Kxd4ToJIlvcGmkaYTpc44hd2ZibYXybY5mKHS3bX;yJGwyOjFyIHPlcIwhdGmwZTygTWM2OD17IH7N M1XNWVExPTB6NEOw
human IGROV1 cells M4H4dnBzd2yrZnXyZZRqd25iYYPzZZk> NVezcGxtSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSSmMh[W6mIF\SZYxxcGFiZYjwdoV{e2mwZzDoeY1idiCLR2LPWlEh[2WubIOsJGlEPTB;MUKuOkBvVQ>? MoWwNVg3QDB{N{W=
RT16 cells NHXTPJZRem:uaX\ldoF1cW:wIHHzd4F6 M{DtO|k3KGh? NE\uUHdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JINpcW6nc3WgbIFue3SncjDSWFE3KGOnbHzzJIV5eHKnc4PpcochcHWvYX6gSnJidHCqYTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZidnnhZoxmKGOnbHzzJIFnfGW{IEm2JIhzeyxiSVO1NF0yPSCwTR?= M2jjWVIyQDd7N{W3
chinese hamster D4 cells M2j1Z3Bzd2yrZnXyZZRqd25iYYPzZZk> M{myOVk3KGh? MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPobY5me2ViaHHtd5RmeiCGNDDj[YxteyCneIDy[ZN{cW6pIHj1cYFvKE[UYnX0ZUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[geoli[mynIHPlcIx{KGGodHXyJFk3KGi{czygTWM2OD1{MjDuUS=> NETQd3UzOTh5OUe1Oy=>
human KB cells MkTGR5l1d3SxeHnjbZR6KGG|c3H5 MWWyNFAhdk1? MofMPVYhcA>? MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnuZ5Vj[XSnZDD1dEB1dyB7NjDodpMhcW5icILld4Vv[2Vib3[gNlAxKG6PIH\vcIlkKGGlaXSgZpkhS2WubITpeIVzNWKudXWgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIhdk1? NVrUW5NTOjV{M{SxNlg>
R2/PCFT4 cells M2PZOmZ2dmO2aX;uJIF{e2G7 MnLKPVYhcA>? MUPJcohq[mm2aX;uJI9nKFCFRmSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hS2irbnXz[UBp[W2|dHXyJHIzN1CFRmS0JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7jeYJifGWmIIXwJJRwKDl4IHjyd{BjgSCFZXzseIl1\XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB7OUWg{txO M1;rSlI2OjN2MUK4
R2 cells NG[1cYpEgXSxdH;4bYNqfHliYYPzZZk> MXK5OkBp M2Dke2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGOqaX7ld4UhcGGvc4TldkBTOiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJHBETlR2IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1emVvQnz1[UBndHWxcnXzZ4Vv[2ViYYPzZZk> MXeyOFI2PjRzMB?=
R2 cells Moe4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUXXWpJiQTZiaB?= NVXiVYRGT3Kxd4ToJIlvcGmkaYTpc44hd2ZiQ3jpcoV{\SCqYX3zeIVzKFJ{IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWEOIVESgZYZ1\XJiOU[gbJJ{KGK7IFPlcIxVcXSncj3icJVmKGG|c3H5MEBKSzVyPUCuNFk6PSEQvF2= MYSyOFEyOTl2Mh?=
L1210 mouse leukemia cells MVTGeY5kfGmxbjDhd5NigQ>? Mn\uR49ueG:3bnSge4F{KGW4YXz1ZZRm\CCob4KgbY5pcWKrdHnvckBw\iC2aIntbYR6dGG2ZTDzfY51cGG|ZTygdIFzfGmjbHz5JJB2emmoaXXkJIZzd21iTEGyNVAhdW:3c3WgcIV2c2WvaXGgZ4VtdHNidHjheEBwfmW{cILv[JVk\SC2aIntbYR6dGG2ZTDzfY51cGG|ZTDkeYUhfG9iYX3wcIlncWOjdHnvckBw\iCWUzDn[Y5mNCCNaU2wMlQyQCEQvF2= NX[4TXJtOTN5MkO1PC=>
human HepG2 cells MmXBR5l1d3SxeHnjbZR6KGG|c3H5 NYnrPY5LPDhiaB?= M1HUdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4{KM7:TR?= M1qwOlI{PDlyMUW5
SGC7901 cells MVnDfZRwfG:6aXPpeJkh[XO|YYm= MV[0PEBp NVrYR|Q5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0eFN{mwNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRThwNzFOwG0> NIHTWHEzOzR7MEG1PS=>
MCF7 cells NGXpeY9EgXSxdH;4bYNqfHliYYPzZZk> NFfuPFk1QCCq MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUKuOkDPxE1? NUjpe4l3OjN2OUCxOVk>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 30820189     

Raltitrexed (Ral) inhibited cell viability of esophageal squamous cancer cell lines and potentiated the inhibitory effect on cell viability and colony formation by irradiation (IR). The effects of different doses of Ral on the cell viability 24, 48 or 72 h’ treatment were determined in TE-13 (a) and Kyse150 cell lines (b)

Western blot
Cleaved caspase-3 / Bax; 

PubMed: 30820189     

Expression of apoptosis related proteins after different treatments was studied in TE-13 and Kyse150.

In vivo Raltitrexed could be directly transported into the brain via the olfactory pathway in rats. [4]


Solubility (25°C)

In vitro DMSO 91 mg/mL (198.47 mM)
Water Insoluble
Ethanol Insoluble

* 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 458.49


CAS No. 112887-68-0
Storage powder
in solvent
Synonyms ZD-1694

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID