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 M3HVcmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHXEUlI6PiCq NIrPS4pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIlv[3WkYYTl[EB2eCC2bzC5OkBpenNiYomgR4VtdHSrdHXyMYJtfWViY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT65JI5O MkO1NlUzOzRzMki=
PC43-10 cells MV;GeY5kfGmxbjDhd5NigQ>? M3vNZlk3KGh? NXrPb2F{UW6qaXLpeIlwdiCxZjDSSmMhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ3jpcoV{\SCqYX3zeIVzKFCFNEOtNVAh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGK7IFPlcIx1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwMzDuUS=> M4LoN|I2OjN2MUK4
L1210 cell line MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmTqS5Jwf3SqIHnubIljcXSrb36gc4YhdXW{aX7lJJR2dW:{IFyxNlExKGOnbHygcIlv\SxiSVO1NF06KG6P Mmr4NVA2ODh2M{C=
human IGROV1 cells M4DmdXBzd2yrZnXyZZRqd25iYYPzZZk> MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKIQzDhcoQhTlKjbIDoZUBmgHC{ZYPzbY5oKGi3bXHuJGlIWk:YMTDj[YxteyxiSVO1NF0yOi54IH7N NEO5TVgyQDZ6MEK3OS=>
RT16 cells M4HL[HBzd2yrZnXyZZRqd25iYYPzZZk> NWXsU4lLQTZiaB?= NWLXV|NkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgVnQyPiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGZT[WyyaHGgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oII\pZYJt\SClZXzsd{Bi\nSncjC5OkBpenNuIFnDOVA:OTVibl2= NYPMS4RXOjF6N{m3OVc>
chinese hamster D4 cells MoC2VJJwdGmoZYLheIlwdiCjc4PhfS=> MYq5OkBp MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPobY5me2ViaHHtd5RmeiCGNDDj[YxteyCneIDy[ZN{cW6pIHj1cYFvKE[UYnX0ZUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[geoli[mynIHPlcIx{KGGodHXyJFk3KGi{czygTWM2OD1{MjDuUS=> NGPyfGczOTh5OUe1Oy=>
human KB cells NVTUSXZ{S3m2b4TvfIlkcXS7IHHzd4F6 NWrDTZFWOjByIH7N NHLSdHI6PiCq M3rrcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gbY5kfWKjdHXkJJVxKHSxIEm2JIhzeyCrbjDwdoV{\W6lZTDv[kAzODBibl2g[o9tcWNiYXPp[EBjgSCFZXzseIl1\XJvYnz1[UBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOiCwTR?= M1fV[VI2OjN2MUK4
R2/PCFT4 cells M2HwS2Z2dmO2aX;uJIF{e2G7 NGj1bFA6PiCq NV;ZdndkUW6qaXLpeIlwdiCxZjDQR2ZVKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFPobY5me2ViaHHtd5RmeiCUMj;QR2ZVPCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIlv[3WkYYTl[EB2eCC2bzC5OkBpenNiYomgR4VtdHSrdHXyMYJtfWViY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wPVk2KM7:TR?= NUDVZWhVOjV{M{SxNlg>
R2 cells NWPhU49OS3m2b4TvfIlkcXS7IHHzd4F6 MWS5OkBp NHm4OZhEgXSxdH;4bYNqfHliYXfhbY5{fCClaHnu[ZNmKGijbYP0[ZIhWjJiY3XscJMh\XiycnXzd4lv\yCqdX3hckBRS0[WNDDh[pRmeiB7NjDodpMh[nliQ3XscHRqfHKnLVLseYUh\my3b4Lld4NmdmOnIHHzd4F6 Mn75NlQzPTZ2MUC=
R2 cells NH32bYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWjleY9CQTZiaB?= MWHHdo94fGhiaX7obYJqfGmxbjDv[kBEcGmwZYPlJIhidXO2ZYKgVlIh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDQR2ZVPCCjZoTldkA6PiCqcoOgZpkhS2WubGTpeIVzNWKudXWgZZN{[XluIFnDOVA:OC5yOUm1JO69VQ>? M4TRe|I1OTFzOUSy
L1210 mouse leukemia cells MVrGeY5kfGmxbjDhd5NigQ>? NH;ZeZNEd22yb4Xu[EB4[XNiZY\hcJVifGWmIH\vdkBqdmirYnn0bY9vKG:oIITofY1q\HmuYYTlJJN6dnSqYYPlMEBx[XK2aXHscJkheHW{aX\p[YQh\nKxbTDMNVIyOCCvb4Xz[UBt\XWtZX3pZUBk\WyuczD0bIF1KG:4ZYLwdo9lfWOnIITofY1q\HmuYYTlJJN6dnSqYYPlJIR2\SC2bzDhcZBtcW[rY3H0bY9vKG:oIGTTJIdmdmVuIFvpQVAvPDF6IN88US=> NHfJT4kyOzd{M{W4
human HepG2 cells Mn\HR5l1d3SxeHnjbZR6KGG|c3H5 M4TmWFQ5KGh? NYnrTll6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjNizszN MkLWNlM1QTBzNUm=
SGC7901 cells Mn3hR5l1d3SxeHnjbZR6KGG|c3H5 NF71[Ig1QCCq MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTS2M4QTBzIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9PE44KM7:TR?= Mkj6NlM1QTBzNUm=
MCF7 cells M2rk[GN6fG:2b4jpZ4l1gSCjc4PhfS=> MWG0PEBp M3:xbWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNk43KM7:TR?= MkTCNlM1QTBzNUm=

... 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
in solvent
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