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 MWXDfZRwfG:6aXPpeJkh[XO|YYm= MkjiPVYhcA>? MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnuZ5Vj[XSnZDD1dEB1dyB7NjDodpMh[nliQ3XscJRqfGW{LXLseYUh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N Ml\TNlUzOzRzMki=
PC43-10 cells NHjndlhHfW6ldHnvckBie3OjeR?= MWG5OkBp M3zzVGlvcGmkaYTpc44hd2ZiUl\DJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEOqaX7ld4UhcGGvc4TldkBRSzR|LUGwJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7jeYJifGWmIIXwJJRwKDl4IHjyd{BjgSCFZXzseIl1\XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjNibl2= Ml;nNlUzOzRzMki=
L1210 cell line NIO1VWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml;kS5Jwf3SqIHnubIljcXSrb36gc4YhdXW{aX7lJJR2dW:{IFyxNlExKGOnbHygcIlv\SxiSVO1NF06KG6P MYCxNFUxQDR|MB?=
human IGROV1 cells NEfMfItRem:uaX\ldoF1cW:wIHHzd4F6 M1PaNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUl\DJIFv\CCIUnHsdIhiKGW6cILld5NqdmdiaIXtZY4hUUeUT2[xJINmdGy|LDDJR|UxRTF{Lk[gcm0> NGrFd5MyQDZ6MEK3OS=>
RT16 cells M1f5dHBzd2yrZnXyZZRqd25iYYPzZZk> NILrfmI6PiCq NWDRRVA5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgVnQyPiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGZT[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oII\pZYJt\SClZXzsd{Bi\nSncjC5OkBpenNuIFnDOVA:OTVibl2= NULGWI1pOjF6N{m3OVc>
chinese hamster D4 cells M2DyRnBzd2yrZnXyZZRqd25iYYPzZZk> NIHIW5E6PiCq MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPobY5me2ViaHHtd5RmeiCGNDDj[YxteyCneIDy[ZN{cW6pIHj1cYFvKE[UYnX0ZUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[geoli[mynIHPlcIx{KGGodHXyJFk3KGi{czygTWM2OD1{MjDuUS=> M1XVT|IyQDd7N{W3
human KB cells NV7m[4hiS3m2b4TvfIlkcXS7IHHzd4F6 M2rmd|IxOCCwTR?= NYXNUnF6QTZiaB?= Mli2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGmwIIDy[ZNmdmOnIH;mJFIxOCCwTTDmc4xq[yCjY3nkJIJ6KEOnbHz0bZRmei2kbIXlJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzKG6P M1H1TlI2OjN2MUK4
R2/PCFT4 cells MYDGeY5kfGmxbjDhd5NigQ>? NVXOO4JHQTZiaB?= M2nh[GlvcGmkaYTpc44hd2ZiUFPGWEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCFaHnu[ZNmKGijbYP0[ZIhWjJxUFPGWFQh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGK7IFPlcIx1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEm5OUDPxE1? NIDjVHAzPTJ|NEGyPC=>
R2 cells MmDDR5l1d3SxeHnjbZR6KGG|c3H5 MV[5OkBp MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgVlIh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDQR2ZVPCCjZoTldkA6PiCqcoOgZpkhS2WubGTpeJJmNUKudXWg[ox2d3Knc3PlcoNmKGG|c3H5 NWTWNYV1OjR{NU[0NVA>
R2 cells MmmyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkG2PVYhcA>? MYfHdo94fGhiaX7obYJqfGmxbjDv[kBEcGmwZYPlJIhidXO2ZYKgVlIh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDQR2ZVPCCjZoTldkA6PiCqcoOgZpkhS2WubGTpeIVzNWKudXWgZZN{[XluIFnDOVA:OC5yOUm1JO69VQ>? NYPSdnN4OjRzMUG5OFI>
L1210 mouse leukemia cells MnHLSpVv[3Srb36gZZN{[Xl? MWnDc41xd3WwZDD3ZZMh\X[jbIXheIVlKG[xcjDpcohq[mm2aX;uJI9nKHSqeX3p[Jlt[XSnIIP5cpRp[XOnLDDwZZJ1cWGubImgdJVzcW[rZXSg[pJwdSCOMUKxNEBud3W|ZTDs[ZVs\W2rYTDj[YxteyC2aHH0JI93\XKycn;keYNmKHSqeX3p[Jlt[XSnIIP5cpRp[XOnIHT1[UB1dyCjbYDsbYZq[2G2aX;uJI9nKFSVIHflcoUtKEurPUCuOFE5KM7:TR?= NUjOUJFbOTN5MkO1PC=>
human HepG2 cells NVnvOY5yS3m2b4TvfIlkcXS7IHHzd4F6 NUO5elJpPDhiaB?= M3PDcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4{KM7:TR?= NYPyWoJKOjN2OUCxOVk>
SGC7901 cells NEjWVGhEgXSxdH;4bYNqfHliYYPzZZk> M4njZlQ5KGh? NXSyOodIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0eFN{mwNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRThwNzFOwG0> NE\wc4wzOzR7MEG1PS=>
MCF7 cells Mlj4R5l1d3SxeHnjbZR6KGG|c3H5 MnfHOFghcA>? NUHvU2tsS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEzNjZizszN MUGyN|Q6ODF3OR?=

... 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