Raltitrexed
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Raltitrexed
structure -
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CAS No:
112887-68-0
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Formula:
C21H22N4O6S
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Chemical Name:
Raltitrexed
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Synonyms:
L-Glutamic acid,N-[[5-[[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-;L-Glutamic acid,N-[[5-[[(1,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-;N-[[5-[[(3,4-Dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-L-glutamic acid;ICI-D 1694;D 1694;ZD 1694;Tomudex;Raltitrexed;TDX
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CAS No:
Description
Yellow Crystalline PowderTomudex was launched in Ireland, France, Luxembourg and the UK for advanced colorectal cancer and it was prepared in a convergent manner (6 steps) from diethyl L-glutamate and 6-bromomethyi-2-methyl-quinazolin4(3H)-one. Tomudex is a highly selective inhibitor of thymidylate synthase (TS), the key enzyme in the biochemical conversion of dUMP to dTMP. It enters the cell via the reduced folatefmethotrexate cell membrane carrier and is converted to the polyglutamate s
Characteristics
177
1.4
off-white to light yellow
1.49±0.1 g/cm3(Predicted)
180-184 °C
1.692
H2O: ≥10mg/mL
Hygroscopic, -20°C Freezer, Under Inert Atmosphere
Safety Information
II
8
UN 2811 6.1 / PGIII
2
36/38-25-61
26-37/39-45-53
Xi,T
P201, P202, P281, P308+P313, P405, P501
H341
Raltitrexed Use and Manufacturing
Folate-based inhibitor of thymidylate synthase; rapidly and extensively metabolized to its more potent polyglutamate derivatives. Antineoplastic
Drug Function and Efficacy
Raltitrexed is an antimetabolite folic acid analog that specifically inhibits thymidylate synthase (TS). Inhibition of TS leads to DNA fragmentation and cell apoptosis. Raltitrexed polyglutamate improves its anti-tumor activity by enhancing TS inhibition ability and prolonging inhibition time.
Registered Holders
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Yuanda Wuyao (Jiangsu) Pharmaceutical Co., Ltd.
Active
China
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Zhejiang Haoge Pharmaceutical Co., Ltd.
Active
China
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Jiangsu Purun Biopharmaceutical Co., Ltd.
Active
China
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