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Raltitrexed

Raltitrexed structure

CAS No:
112887-68-0
Formula:
C21H22N4O6S
Chemical Name:
Raltitrexed
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
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

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

Raltitrexed Basic Attributes

Molecular Weight：

458.49

Exact Mass：

458.49

EC Number：

1533716-785-6

Characteristics

PSA：

177

XLogP3：

1.4

Appearance：

off-white to light yellow

Density：

1.49±0.1 g/cm3(Predicted)

Melting Point：

180-184 °C

Refractive Index：

1.692

Water Solubility：

H2O: ≥10mg/mL

Storage Conditions：

Hygroscopic, -20°C Freezer, Under Inert Atmosphere

Safety Information

Packing level：

Hazard category：

Transport codes：

UN 2811 6.1 / PGIII

wgk germany：

hazard class code：

36/38-25-61

safety instructions：

26-37/39-45-53

Marks：

Xi,T

Precautionary statement(s)：

P201, P202, P281, P308+P313, P405, P501

Hazard Statements：

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.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Raltitrexed for injection
Ingredients	The active ingredient of this product is raltitrexed. Its chemical name: N-[5-[N-methyl-N-(2-methyl-4-oxo-3,4-dihydroquinazoline-6-methyl)amino]thiophene-2-carbonyl]-L-glutamic acid. Chemical structure: Molecular formula: C21H22N4O6S Molecular weight: 458.49 Excipients: mannitol, disodium hydrogen phosphate and sodium hydroxide.
Indication	Drug interactions may occur if used with other drugs. Please consult your doctor or pharmacist for details.
Specifications	2mg
Manufacturer	Nanjing Chia Tai-tianqing Pharmaceutical Co., Ltd.

Raltitrexed

Registered Holders

Yuanda Wuyao (Jiangsu) Pharmaceutical Co., Ltd.

China
Active
Zhejiang Haoge Pharmaceutical Co., Ltd.

China
Active
Jiangsu Purun Biopharmaceutical Co., Ltd.

China
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Guide of Raltitrexed

Description
Basic Attributes
Characteristics
Safety Information
Use and Manufacturing
Drug Function and Efficacy
Related Drugs
Registered Holders
Recommended Suppliers
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Raltitrexed

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