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.

Size Price Stock Quantity  
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 MV3DfZRwfG:6aXPpeJkh[XO|YYm= MlPuPVYhcA>? MnvPR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGK7IFPlcIx1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> M2DvWVI2OjN2MUK4
PC43-10 cells M1[1N2Z2dmO2aX;uJIF{e2G7 MVy5OkBp MVHJcohq[mm2aX;uJI9nKFKIQzCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBEcGmwZYPlJIhidXO2ZYKgVGM1Oy1zMDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGmwY4XiZZRm\CC3cDD0c{A6PiCqcoOgZpkhS2WubITpeIVzNWKudXWgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4{KG6P MmXJNlUzOzRzMki=
L1210 cell line NFrqUWhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYPnWm91T3Kxd4ToJIlvcGmkaYTpc44hd2ZibYXybY5mKHS3bX;yJGwyOjFyIHPlcIwhdGmwZTygTWM2OD17IH7N NXX0R3lTOTB3MEi0N|A>
human IGROV1 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKIQzDhcoQhTlKjbIDoZUBmgHC{ZYPzbY5oKGi3bXHuJGlIWk:YMTDj[YxteyxiSVO1NF0yOi54IH7N M{i3PVE5PjhyMke1
RT16 cells NWrp[GxuWHKxbHnm[ZJifGmxbjDhd5NigQ>? NULCfJZVQTZiaB?= M{fLdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgZ4hqdmW|ZTDoZY1{fGW{IGLUNVYh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDGVoFteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC4aXHicIUh[2WubIOgZYZ1\XJiOU[gbJJ{NCCLQ{WwQVE2KG6P NY\VfZJPOjF6N{m3OVc>
chinese hamster D4 cells MnPsVJJwdGmoZYLheIlwdiCjc4PhfS=> NIjoXY46PiCq NWr2cY1YSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBkcGmwZYPlJIhidXO2ZYKgSFQh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDGVoJmfGFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKH[rYXLs[UBk\WyuczDh[pRmeiB7NjDodpMtKEmFNUC9NlIhdk1? NIDpc3gzOTh5OUe1Oy=>
human KB cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= MYiyNFAhdk1? M2\QcVk3KGh? MoPQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGmwIIDy[ZNmdmOnIH;mJFIxOCCwTTDmc4xq[yCjY3nkJIJ6KEOnbHz0bZRmei2kbIXlJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzKG6P MYqyOVI{PDF{OB?=
R2/PCFT4 cells NI\l[nRHfW6ldHnvckBie3OjeR?= NIKyRoY6PiCq NHT4cmNKdmirYnn0bY9vKG:oIGDDSnQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ3jpcoV{\SCqYX3zeIVzKFJ{L2DDSnQ1KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gbY5kfWKjdHXkJJVxKHSxIEm2JIhzeyCkeTDD[YxtfGm2ZYKtZox2\SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC5PVUh|ryP MojUNlUzOzRzMki=
R2 cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= NXj1PVNGQTZiaB?= M4P2eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGOqaX7ld4UhcGGvc4TldkBTOiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJHBETlR2IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1emVvQnz1[UBndHWxcnXzZ4Vv[2ViYYPzZZk> MVOyOFI2PjRzMB?=
R2 cells MojoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIXtNFg6PiCq NF7ZfZhIem:5dHigbY5pcWKrdHnvckBw\iCFaHnu[ZNmKGijbYP0[ZIhWjJiY3XscJMh\XiycnXzd4lv\yCqdX3hckBRS0[WNDDh[pRmeiB7NjDodpMh[nliQ3XscHRqfGW{LXLseYUh[XO|YYmsJGlEPTB;MD6wPVk2KM7:TR?= MVKyOFEyOTl2Mh?=
L1210 mouse leukemia cells MVTGeY5kfGmxbjDhd5NigQ>? Mm\1R49ueG:3bnSge4F{KGW4YXz1ZZRm\CCob4KgbY5pcWKrdHnvckBw\iC2aIntbYR6dGG2ZTDzfY51cGG|ZTygdIFzfGmjbHz5JJB2emmoaXXkJIZzd21iTEGyNVAhdW:3c3WgcIV2c2WvaXGgZ4VtdHNidHjheEBwfmW{cILv[JVk\SC2aIntbYR6dGG2ZTDzfY51cGG|ZTDkeYUhfG9iYX3wcIlncWOjdHnvckBw\iCWUzDn[Y5mNCCNaU2wMlQyQCEQvF2= M4\OTFE{PzJ|NUi=
human HepG2 cells NUTuT2F4S3m2b4TvfIlkcXS7IHHzd4F6 NFvzdFU1QCCq NHPReIlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvOyEQvF2= MYGyN|Q6ODF3OR?=
MCF7 cells M3nhNmN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3COFghcA>? MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUKuOkDPxE1? NVKwe|FSOjN2OUCxOVk>

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID