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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  • 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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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 M4DO[2N6fG:2b4jpZ4l1gSCjc4PhfS=> NXvQ[FJmQTZiaB?= M1LFTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gbY5kfWKjdHXkJJVxKHSxIEm2JIhzeyCkeTDD[YxtfGm2ZYKtZox2\SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lkmgcm0> MUGyOVI{PDF{OB?=
PC43-10 cells NE\mWoZHfW6ldHnvckBie3OjeR?= MV:5OkBp MmL4TY5pcWKrdHnvckBw\iCURlOgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hS2irbnXz[UBp[W2|dHXyJHBEPDNvMUCgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCrbnP1ZoF1\WRidYCgeI8hQTZiaILzJIJ6KEOnbHz0bZRmei2kbIXlJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOyCwTR?= M4XIOlI2OjN2MUK4
L1210 cell line MlfXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnWwS5Jwf3SqIHnubIljcXSrb36gc4YhdXW{aX7lJJR2dW:{IFyxNlExKGOnbHygcIlv\SxiSVO1NF06KG6P NYXoRXJsOTB3MEi0N|A>
human IGROV1 cells MUfQdo9tcW[ncnH0bY9vKGG|c3H5 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKIQzDhcoQhTlKjbIDoZUBmgHC{ZYPzbY5oKGi3bXHuJGlIWk:YMTDj[YxteyxiSVO1NF0yOi54IH7N MnHoNVg3QDB{N{W=
RT16 cells Mn[yVJJwdGmoZYLheIlwdiCjc4PhfS=> NFHXU5Q6PiCq MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPobY5me2ViaHHtd5RmeiCUVEG2JINmdGy|IHX4dJJme3OrbnegbJVu[W5iRmLhcJBp[SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhfmmjYnzlJINmdGy|IHHmeIVzKDl4IHjyd{whUUN3ME2xOUBvVQ>? NWDvVY44OjF6N{m3OVc>
chinese hamster D4 cells MoDYVJJwdGmoZYLheIlwdiCjc4PhfS=> NVHoUox3QTZiaB?= NUPYZWRRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgSFQh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDGVoJmfGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKH[rYXLs[UBk\WyuczDh[pRmeiB7NjDodpMtKEmFNUC9NlIhdk1? NIfH[GQzOTh5OUe1Oy=>
human KB cells NF3ZS3hEgXSxdH;4bYNqfHliYYPzZZk> NHy5N4YzODBibl2= M{XjO|k3KGh? MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnuZ5Vj[XSnZDD1dEB1dyB7NjDodpMhcW5icILld4Vv[2Vib3[gNlAxKG6PIH\vcIlkKGGlaXSgZpkhS2WubITpeIVzNWKudXWgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIhdk1? M2i3UlI2OjN2MUK4
R2/PCFT4 cells MnXwSpVv[3Srb36gZZN{[Xl? MYS5OkBp MW\Jcohq[mm2aX;uJI9nKFCFRmSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hS2irbnXz[UBp[W2|dHXyJHIzN1CFRmS0JINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7jeYJifGWmIIXwJJRwKDl4IHjyd{BjgSCFZXzseIl1\XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB7OUWg{txO NVH2[WpVOjV{M{SxNlg>
R2 cells NYW1OJJ3S3m2b4TvfIlkcXS7IHHzd4F6 Ml7iPVYhcA>? NYf2c3pJS3m2b4TvfIlkcXS7IHHnZYlve3RiY3jpcoV{\SCqYX3zeIVzKFJ{IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWEOIVESgZYZ1\XJiOU[gbJJ{KGK7IFPlcIxVcXS{ZT3CcJVmKG[udX;y[ZNk\W6lZTDhd5NigQ>? M1To[lI1OjV4NEGw
R2 cells MlPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXO5OkBp NXvEfoVFT3Kxd4ToJIlvcGmkaYTpc44hd2ZiQ3jpcoV{\SCqYX3zeIVzKFJ{IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hWEOIVESgZYZ1\XJiOU[gbJJ{KGK7IFPlcIxVcXSncj3icJVmKGG|c3H5MEBKSzVyPUCuNFk6PSEQvF2= NGjLPYczPDFzMUm0Ni=>
L1210 mouse leukemia cells NHrhUlhHfW6ldHnvckBie3OjeR?= MX\Dc41xd3WwZDD3ZZMh\X[jbIXheIVlKG[xcjDpcohq[mm2aX;uJI9nKHSqeX3p[Jlt[XSnIIP5cpRp[XOnLDDwZZJ1cWGubImgdJVzcW[rZXSg[pJwdSCOMUKxNEBud3W|ZTDs[ZVs\W2rYTDj[YxteyC2aHH0JI93\XKycn;keYNmKHSqeX3p[Jlt[XSnIIP5cpRp[XOnIHT1[UB1dyCjbYDsbYZq[2G2aX;uJI9nKFSVIHflcoUtKEurPUCuOFE5KM7:TR?= MXKxN|czOzV6
human HepG2 cells NXnDRXd3S3m2b4TvfIlkcXS7IHHzd4F6 NGXRVog1QCCq NWnXXpNnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjNizszN M1zUVlI{PDlyMUW5
SGC7901 cells MkfkR5l1d3SxeHnjbZR6KGG|c3H5 MonzOFghcA>? MlmyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2dEPzlyMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVgvPyEQvF2= Mom2NlM1QTBzNUm=
MCF7 cells NFLmdoJEgXSxdH;4bYNqfHliYYPzZZk> NFTiSHo1QCCq M4TMN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNk43KM7:TR?= M33COlI{PDlyMUW5

... Click to View More Cell Line Experimental Data

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
Synonyms ZD-1694

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03053167 Recruiting ColoRectal Cancer China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region December 2016 Phase 2
NCT02965248 Recruiting Locally Advanced Colorectal Cancer Fudan University November 2016 Phase 2
NCT02992886 Recruiting Rectal Neoplasms Malignant Chinese Academy of Medical Sciences September 2016 Phase 2
NCT02618356 Not yet recruiting Metastatic Colon Cancer Fudan University December 2015 Phase 2
NCT02562599 Recruiting Nasopharyngeal Carcinoma Hubei Cancer Hospital August 2015 Phase 2
NCT02485548 Recruiting Head and Neck Squamous Cell Cancer Jiangsu Cancer Institute & Hospital|Wuxi Cancer Hospital|Changzhou Cancer Hospital|Nanjing Cancer Hospital|Northern Jiangsu Province Peoples Hospital|The Second Hospital of Nanjing Medical University|Nanjing BenQ Hospital June 2015 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID