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Cat. No. Name Size Price Add Cart
KI1107Raltitrexed10 mg$112
Raltitrexed100 mg$752

Chemical Characteristic

Product NameRaltitrexed
SynonymsTomudex, ZD1694
CAS No.112887-68-0
Molecular Weight 458.49
FormulaC21H22N4O6S
Chemical Name(2S)-2-[[5-[methyl-[(2-methyl-4-oxo-1H-quinazolin-6-yl)methyl]amino]thiophene-2-carbonyl]amino]pentanedioic acid
SmilesC(=O)([C@H](CCC(=O)O)NC(=O)c1ccc(s1)N(Cc1cc2c(=O)[nH]c(nc2cc1)C)C)O
Chemical Structure

Biological activities

Raltitrexed is an inhibitor of thymidylate synthase with a Ki of approximately 60 nM.[1] Raltitrexed is an antimetabolite drug used in cancer chemotherapy. Raltitrexed is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. Raltitrexed prevents the formation of DNA and RNA. Raltitrexed blocks the production of thymidine monophosphate from deoxyuridine monophosphate in a reaction-specific manner.[2] Raltitrexed inhibits dihydrofolate reductase, but is approximately 100-times more specific for thymidylate synthase than for dihydrofolate reductase. The IC50 of raltitrexed for the growth of mouse or human cells in culture is ranging from l to 10 nM. Raltitrexed inhibits the growth of a panel of human colon tumor cell lines (including HT29, LoVo, SW480, SW620, MaWi and BE) with IC50 values in a narrow concentration range (1.3-3.9 nM).[3] In nude mice bearing human head and neck squamous cell carcinoma A253 and FaDu xenografts, antitumor activity of raltitrexed is schedule-dependent in both tumors. Raltitrexed at the maximum tolerated doses (MTDs: 150 mg/kg/course) produces 20% complete tumor regression and 20% partial tumor regression (PR) against FaDu xenografts.[4]

Protocols

In vitro: Raltitrexed is dissolved in water.[3]

References

[1] Jackman AL, et al. ICI D1694, a quinazoline antifolate thymidylate synthase inhibitor that is a potent inhibitor of L1210 tumor cell growth in vitro and in vivo: a new agent for clinical study. Cancer Res. 1991, 51(20): 5579-5586.
[2] Reni M, et al. Raltitrexed-eloxatin salvage chemotherapy in gemcitabine-resistant metastatic pancreatic cancer. Br J Cancer. 2006, 94(6): 785-791.
[3] Jackman AL, et al. ZD1694 (Tomudex): a new thymidylate synthase inhibitor with activity in colorectal cancer. Eur J Cancer. 1995, 31A(7-8): 1277-1282.
[4] Cao S, et al. Antitumor activity of ZD1694 (tomudex) against human head and neck cancer in nude mouse models: role of dosing schedule and plasma thymidine. Clin Cancer Res. 1999, 5(7): 1925-1934.

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