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
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • 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.

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

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 MXHDfZRwfG:6aXPpeJkh[XO|YYm= MlS3PVYhcA>? MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnuZ5Vj[XSnZDD1dEB1dyB7NjDodpMh[nliQ3XscJRqfGW{LXLseYUh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N MUOyOVI{PDF{OB?=
PC43-10 cells M3PaT2Z2dmO2aX;uJIF{e2G7 NH;zfXo6PiCq NHPRdY1KdmirYnn0bY9vKG:oIGLGR{ApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCFaHnu[ZNmKGijbYP0[ZIhWEN2Mz2xNEBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnuZ5Vj[XSnZDD1dEB1dyB7NjDodpMh[nliQ3XscJRqfGW{LXLseYUh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5|IH7N MVeyOVI{PDF{OB?=
L1210 cell line M1PHXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3v6OWdzd3e2aDDpcohq[mm2aX;uJI9nKG23cnnu[UB1fW2xcjDMNVIyOCClZXzsJIxqdmVuIFnDOVA:QSCwTR?= MWSxNFUxQDR|MB?=
human IGROV1 cells NETiblFRem:uaX\ldoF1cW:wIHHzd4F6 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKIQzDhcoQhTlKjbIDoZUBmgHC{ZYPzbY5oKGi3bXHuJGlIWk:YMTDj[YxteyxiSVO1NF0yOi54IH7N MV[xPFY5ODJ5NR?=
RT16 cells MmPLVJJwdGmoZYLheIlwdiCjc4PhfS=> NFTzPI06PiCq M136[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgZ4hqdmW|ZTDoZY1{fGW{IGLUNVYh[2WubIOg[ZhxemW|c3nu[{BpfW2jbjDGVoFteGijIHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC4aXHicIUh[2WubIOgZYZ1\XJiOU[gbJJ{NCCLQ{WwQVE2KG6P MVOyNVg4QTd3Nx?=
chinese hamster D4 cells NFK0RXRRem:uaX\ldoF1cW:wIHHzd4F6 NV\zRmVRQTZiaB?= NF7MSY5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JINpcW6nc3WgbIFue3SncjDEOEBk\WyuczDlfJBz\XO|aX7nJIh2dWGwIF\SZoV1[SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhfmmjYnzlJINmdGy|IHHmeIVzKDl4IHjyd{whUUN3ME2yNkBvVQ>? NEf0fGczOTh5OUe1Oy=>
human KB cells M170d2N6fG:2b4jpZ4l1gSCjc4PhfS=> M2nXZVIxOCCwTR?= NESzV2s6PiCq NHjzSHJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIlv[3WkYYTl[EB2eCC2bzC5OkBpenNiaX6gdJJme2WwY3Wgc4YhOjByIH7NJIZwdGmlIHHjbYQh[nliQ3XscJRqfGW{LXLseYUh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjJibl2= NGXGZYMzPTJ|NEGyPC=>
R2/PCFT4 cells M2r5XWZ2dmO2aX;uJIF{e2G7 NHTnRlE6PiCq M4fJd2lvcGmkaYTpc44hd2ZiUFPGWEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCFaHnu[ZNmKGijbYP0[ZIhWjJxUFPGWFQh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDpcoN2[mG2ZXSgeZAhfG9iOU[gbJJ{KGK7IFPlcIx1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEm5OUDPxE1? NUHCempyOjV{M{SxNlg>
R2 cells MmnXR5l1d3SxeHnjbZR6KGG|c3H5 MnfUPVYhcA>? MkDqR5l1d3SxeHnjbZR6KGGpYXnud5Qh[2irbnXz[UBp[W2|dHXyJHIzKGOnbHzzJIV5eHKnc4PpcochcHWvYX6gVGNHXDRiYX\0[ZIhQTZiaILzJIJ6KEOnbHzUbZRz\S2EbIXlJIZtfW:{ZYPj[Y5k\SCjc4PhfS=> MlLvNlQzPTZ2MUC=
R2 cells NF:yOo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmXJPVYhcA>? M1Tve2dzd3e2aDDpcohq[mm2aX;uJI9nKEOqaX7ld4UhcGGvc4TldkBTOiClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJHBETlR2IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1\XJvYnz1[UBie3OjeTygTWM2OD1yLkC5PVUh|ryP NFWyU4EzPDFzMUm0Ni=>
L1210 mouse leukemia cells NID5SXpHfW6ldHnvckBie3OjeR?= M1nFfGNwdXCxdX7kJJdieyCndnHseYF1\WRiZn;yJIlvcGmkaYTpc44hd2ZidHj5cYllgWyjdHWgd5lvfGijc3WsJJBienSrYXzsfUBxfXKrZnnl[EBnem:vIFyxNlExKG2xdYPlJIxmfWunbXnhJINmdGy|IIToZZQhd3[ncoDyc4R2[2VidHj5cYllgWyjdHWgd5lvfGijc3Wg[JVmKHSxIHHtdIxq\mmlYYTpc44hd2ZiVGOg[4Vv\SxiS3m9NE41OThizszN Ml7zNVM4OjN3OB?=
human HepG2 cells M2fwO2N6fG:2b4jpZ4l1gSCjc4PhfS=> MlrsOFghcA>? NUmz[VlHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjNizszN MY[yN|Q6ODF3OR?=
MCF7 cells MmKyR5l1d3SxeHnjbZR6KGG|c3H5 NHj0VI01QCCq MkjFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGyMlYh|ryP MWSyN|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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Related Antibodies

DNA/RNA Synthesis Signaling Pathway Map

Related DNA/RNA Synthesis Products

Tags: buy Raltitrexed | Raltitrexed supplier | purchase Raltitrexed | Raltitrexed cost | Raltitrexed manufacturer | order Raltitrexed | Raltitrexed distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID