1. Apoptosis
    Cell Cycle/DNA Damage
  2. Thymidylate Synthase
    Nucleoside Antimetabolite/Analog

Raltitrexed (Synonyms: ZD1694; D1694; ICI-D1694)

Cat. No.: HY-10821 Purity: 99.21%
Data Sheet SDS Handling Instructions

Raltitrexed is an inhibitor of thymidylate synthase and an antimetabolite drug used for cancer treatment.

For research use only. We do not sell to patients.
Raltitrexed Chemical Structure

Raltitrexed Chemical Structure

CAS No. : 112887-68-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
10 mg USD 72 In-stock
50 mg USD 276 In-stock
100 mg USD 474 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Raltitrexed is an inhibitor of thymidylate synthase and an antimetabolite drug used for cancer treatment.

IC50 & Target

Raltitrexed (0, 5, 10, 11.5, 13.5, 15 mg/kg b/w, i.p.) increases the rates of resorbed embryos and growth retardation of murine model of NTDs in a dose dependent manner. Raltitrexed (11.5 mg/kg b/w) maximally inhibits the thymidylate synthase (TS) activity in embryonic tissue, decreases dTMP levels and while increases dUMP levels[2].

In Vitro

Raltitrexed inhibits HepG2 proliferation by arresting the cell cycle at G0/G1, and the cell cycle is mediated via downregulation of cyclin A and CDK2[1]. Raltitrexed (0.1, 0.5, 2.5 μg/mL) decreases the viability of SGC7901 cells in a dose- and time-dependent manner. Raltitrexed (0.5 μg/mL) shows typical apoptotic morphology, including nuclear shrinkage, fragmentation, chromatin condensation and apoptotic bodies in SGC7901 cells. Raltitrexed blocks the cell cycle at the G0/G1 phase, decreases in the mitochondrial membrane potential. Raltitrexed also increases the level of ROS, induces caspase-3-dependent apoptosis via activation of the mitochondria, and increases TS protein and mRNA expression levels[3]. Raltitrexed (1.5 nM) reduces the number of GM00637 cells, selectively induces gene conversions, but does not affect DSB-induced HR or NHEJ[4].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1811 mL 10.9054 mL 21.8107 mL
5 mM 0.4362 mL 2.1811 mL 4.3621 mL
10 mM 0.2181 mL 1.0905 mL 2.1811 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[4]

To assess the effect of Raltitrexed on cell viability and/or growth, GM00637 cells are plated into 25 cm2 flasks at a density of 3.3×105 cells per flask. Twenty four hours later, the medium is replaced with medium supplemented with various doses of Raltitrexed over a broad range of concentrations ranging from less than 1 nM to greater than 1 µM. Three flasks of cells are used for each dose tested. Cells are exposed to Raltitrexed for 24 hours, at which time the cells are refed with medium containing no Raltitrexed. Forty-eight hours after feeding with drug-free medium, cells are harvested and counted. The cell counts for the cells exposed to the various Raltitrexed doses are compared with the cell count for control cells not exposed to Raltitrexed as a measure of the impact of Raltitrexed on cell viability and/or growth rate. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Raltitrexed is dissolved in 0.9 % NaCl.

The adult (7-8 week, 19-20 g) C57BL/6 mice are used in the experiment. Mice are maintained under 22°C with a 12 h light/day cycle and fed with standard mouse chow and tap water ad libitum. Female mice are mated with male overnight and vaginal plugs are examined in the following morning. The presence of vaginal plug in the pregnant mice is considered as gestational day 0.5. Pregnant mice are randomly divided into 6 groups with 10 mice in each group. Raltitrexed is dissolved in 0.9 % NaCl, and five groups are intraperitoneally injected with different doses of Raltitrexed (5, 10, 11.5, 13.5, 15 mg/kg b/w) on gestational day 7.5. The control group is intraperitoneally injected with 0.9 % NaCl at the same volume on gestational day 7.5. On gestational day 11.5, pregnant mice are sacrificed, and embryos are examined under dissect microscope. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

458.49

Formula

C₂₁H₂₂N₄O₆S

CAS No.

112887-68-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 29 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.21%

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Raltitrexed
Cat. No.:
HY-10821
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