For research use only.

Catalog No.S1192 Synonyms: ZD-1694

10 publications

Raltitrexed Chemical Structure

CAS No. 112887-68-0

Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.

Selleck's Raltitrexed has been cited by 10 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.

    Raltitrexed purchased from Selleck.

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Choose Selective Thymidylate Synthase Inhibitors

Biological Activity

Description Raltitrexed (ZD-1694) 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 MWLDfZRwfG:6aXPpeJkh[XO|YYm= MYG5OkBp NEXWTYpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIlv[3WkYYTl[EB2eCC2bzC5OkBpenNiYomgR4VtdHSrdHXyMYJtfWViY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT65JI5O MnTaNlUzOzRzMki=
PC43-10 cells M{XMRmZ2dmO2aX;uJIF{e2G7 NXLzTmVbQTZiaB?= M2Pvc2lvcGmkaYTpc44hd2ZiUl\DJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEOqaX7ld4UhcGGvc4TldkBRSzR|LUGwJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7jeYJifGWmIIXwJJRwKDl4IHjyd{BjgSCFZXzseIl1\XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjNibl2= NHn2XJgzPTJ|NEGyPC=>
L1210 cell line NEm1OnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkXNS5Jwf3SqIHnubIljcXSrb36gc4YhdXW{aX7lJJR2dW:{IFyxNlExKGOnbHygcIlv\SxiSVO1NF06KG6P Mm\oNVA2ODh2M{C=
human IGROV1 cells M1TCRXBzd2yrZnXyZZRqd25iYYPzZZk> MlzNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCURlOgZY5lKE[UYXzwbIEh\XiycnXzd4lv\yCqdX3hckBKT1KRVkGgZ4VtdHNuIFnDOVA:OTJwNjDuUS=> M3j4TVE5PjhyMke1
RT16 cells MknkVJJwdGmoZYLheIlwdiCjc4PhfS=> NGPQbJc6PiCq MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPobY5me2ViaHHtd5RmeiCUVEG2JINmdGy|IHX4dJJme3OrbnegbJVu[W5iRmLhcJBp[SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhfmmjYnzlJINmdGy|IHHmeIVzKDl4IHjyd{whUUN3ME2xOUBvVQ>? Mnz4NlE5Pzl5NUe=
chinese hamster D4 cells NUTPWJRYWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVG5OkBp NX;oXGVQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgSFQh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDGVoJmfGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKH[rYXLs[UBk\WyuczDh[pRmeiB7NjDodpMtKEmFNUC9NlIhdk1? NVHDNHlnOjF6N{m3OVc>
human KB cells NIDqUGZEgXSxdH;4bYNqfHliYYPzZZk> NUjjfWhKOjByIH7N MlrOPVYhcA>? M161VWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gbY5kfWKjdHXkJJVxKHSxIEm2JIhzeyCrbjDwdoV{\W6lZTDv[kAzODBibl2g[o9tcWNiYXPp[EBjgSCFZXzseIl1\XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOiCwTR?= M4HWTVI2OjN2MUK4
R2/PCFT4 cells MWrGeY5kfGmxbjDhd5NigQ>? MlLYPVYhcA>? NEDBUYxKdmirYnn0bY9vKG:oIGDDSnQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ3jpcoV{\SCqYX3zeIVzKFJ{L2DDSnQ1KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gbY5kfWKjdHXkJJVxKHSxIEm2JIhzeyCkeTDD[YxtfGm2ZYKtZox2\SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5PVUh|ryP M3P6WVI2OjN2MUK4
R2 cells NYexd3BmS3m2b4TvfIlkcXS7IHHzd4F6 MWW5OkBp MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgVlIh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDQR2ZVPCCjZoTldkA6PiCqcoOgZpkhS2WubGTpeJJmNUKudXWg[ox2d3Knc3PlcoNmKGG|c3H5 NYWyblVWOjR{NU[0NVA>
R2 cells M13uRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfYcYdyQTZiaB?= M1vGeWdzd3e2aDDpcohq[mm2aX;uJI9nKEOqaX7ld4UhcGGvc4TldkBTOiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJHBETlR2IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1\XJvYnz1[UBie3OjeTygTWM2OD1yLkC5PVUh|ryP NWHqN5Q1OjRzMUG5OFI>
L1210 mouse leukemia cells NITHT3RHfW6ldHnvckBie3OjeR?= NH\YTGhEd22yb4Xu[EB4[XNiZY\hcJVifGWmIH\vdkBqdmirYnn0bY9vKG:oIITofY1q\HmuYYTlJJN6dnSqYYPlMEBx[XK2aXHscJkheHW{aX\p[YQh\nKxbTDMNVIyOCCvb4Xz[UBt\XWtZX3pZUBk\WyuczD0bIF1KG:4ZYLwdo9lfWOnIITofY1q\HmuYYTlJJN6dnSqYYPlJIR2\SC2bzDhcZBtcW[rY3H0bY9vKG:oIGTTJIdmdmVuIFvpQVAvPDF6IN88US=> NE\pPVgyOzd{M{W4
human HepG2 cells NUnQUmZvS3m2b4TvfIlkcXS7IHHzd4F6 M37VT|Q5KGh? M{fES2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4{KM7:TR?= MnTxNlM1QTBzNUm=
MCF7 cells NVjYW3NuS3m2b4TvfIlkcXS7IHHzd4F6 M4nRPVQ5KGh? MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUKuOkDPxE1? M2rKcFI{PDlyMUW5

... 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
Smiles CC1=NC2=C(C=C(C=C2)CN(C)C3=CC=C(S3)C(=O)NC(CCC(=O)O)C(=O)O)C(=O)N1

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02618356 Unknown status Drug: Raltitrexed and S-1 Metastatic Colon Cancer Fudan University December 25 2015 Phase 2
NCT02821559 Completed Drug: TOMOX|Drug: Bevacizumab Metastatic Colorectal Cancer Centre Hospitalier Universitaire de Besancon|Hospira now a wholly owned subsidiary of Pfizer July 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID