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Raltitrexed

Catalog No. T6632 CAS 112887-68-0

Synonyms: ZD1694, D1694, ICI-D1694, Tomudex

Raltitrexed (D1694)(IC50 of 9 nM), a thymidylate synthase inhibitor, is used for the inhibition of L1210 cell growth.

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Raltitrexed, CAS 112887-68-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 34.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 89.00
50 mg	In stock	$ 158.00
100 mg	In stock	$ 293.00
200 mg	In stock	$ 495.00
500 mg	In stock	$ 783.00
1 mL * 10 mM (in DMSO)	In stock	$ 38.00

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Purity: 99.06%

Purity: 98.96%

Biological Description

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Description	Raltitrexed (D1694)(IC50 of 9 nM), a thymidylate synthase inhibitor, is used for the inhibition of L1210 cell growth.
Targets&IC50	TS:9 nM
In vitro	Raltitrexed induces double-stranded DNA breaks in a concentration-dependent manner. In Lovo cells and LS174T cell lines containing wild-type p53, Raltitrexed increases the levels of the Bax protein up to 5-fold. In human colon cancer cells, Raltitrexed is actively absorbed into cells and is then rapidly and extensively metabolized into a series of polyglutamates, which results in the effective inhibition of thymidylate synthase. Raltitrexed is delivered to the brain very quickly and can be detected in all brain tissues within 5 minutes. In human colon cancer cells, the combination of Raltitrexed and SN-38 results in a synergistic cytotoxic effect within a range of concentrations. Raltitrexed is a specific folate-based inhibitor of thymidylate synthase. The effect on the activity of advanced rectal cancer is similar to fluorouracil (5-fluorouracil) plus leucovorin. Raltitrexed produces activity by rapid cell entry and glutamination. The glutaminated derivatives are more than 100 times more active than the parent compound. In the HCT-8 cell line, Raltitrexed results in an increase in intracellular phosphoribosyl pyrophosphate (PRPD) indicating that the cytotoxic effect of Raltitrexed in combination with 5-FU is due to increased nucleotide formation of 5-FU. Combinations of Raltitrexed and folinic acid (5FU-FA) show a combination of mode-dependent, synergistic inhibition of proliferation, which is determined by measuring the combination series. Raltitrexed combined with Vorinostat produced significant synergistic effects of cell cycle perturbation and S-phase arrest.
In vivo	Raltitrexed can be transported directly into the brain through the olfactory pathway in rats.

Synonyms	ZD1694, D1694, ICI-D1694, Tomudex
Molecular Weight	458.49
Formula	C21H22N4O6S
CAS No.	112887-68-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 84 mg/mL (183.2 mM)

References and Literature

1. Peters GJ, et al. Eur J Cancer, 2000, 36(7), 916-924. 2. Van Cutsem E, et al. Ann Oncol, 2002, 13(4), 513-522. 3. Aschele C, et al. Clin Cancer Res, 1998, 4(5), 1323-1330. 4. Wang D, et al. Cancer Chemother Pharmacol, 2006, 57(1), 97-104. 5. Di Gennaro E, et al. Cancer Biol Ther, 2009, 8(9), 782-791. 6. Dong Y, et al. Raltitrexed's effect on the development of neural tube defects in mice is associated with DNA damage, apoptosis, and proliferation. Mol Cell Biochem. 2015 Jan;398(1-2):223-31. 7. Zhao H, et al. Raltitrexed Inhibits HepG2 Cell Proliferation via G0/G1 Cell Cycle Arrest. Oncol Res. 2016;23(5):237-48

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Liver Cancer Compound Library Bioactive Compound Library Clinical Compound Library Human Metabolite Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Raltitrexed 112887-68-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA/RNA Synthesis ZD1694 Thymidylate Synthase ICI-D-1694 D-1694 ZD-1694 D1694 inhibit D 1694 Inhibitor ICI-D1694 ICI-D 1694 ZD 1694 Tomudex inhibitor

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