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Raltitrexed

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Raltitrexed Basic information

Product Name:
Raltitrexed
CAS:
112887-68-0
MF:
C21H22N4O6S
MW:
458.49
EINECS:
652-997-2
Mol File:
112887-68-0.mol
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Raltitrexed Chemical Properties

Melting point:
176-1800C
Density 
1.49±0.1 g/cm3(Predicted)
storage temp. 
Hygroscopic, -20°C Freezer, Under Inert Atmosphere
solubility 
H2O: ≥10mg/mL
pka
3.50±0.10(Predicted)
form 
solid
color 
off-white to light yellow
InChIKey
IVTVGDXNLFLDRM-HNNXBMFYSA-N
CAS DataBase Reference
112887-68-0(CAS DataBase Reference)
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Safety Information

Hazard Codes 
Xi,T
Risk Statements 
36/38-25-61
Safety Statements 
26-37/39-45-53
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
2
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Raltitrexed Usage And Synthesis

Description

Tomudex 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 species by folylpolyglutamate synthase within 4h where it then binds to the folate substrate site of TS. Clinically, it had a 29% response rate in patients with advanced colorectal cancer. It is water soluble, can be administered as a single dose every three weeks and had no hepto- or nephrotoxicity.

Chemical Properties

Yellow Crystalline Powder

Originator

Zeneca (UK)

Uses

Folate-based inhibitor of thymidylate synthase; rapidly and extensively metabolized to its more potent polyglutamate derivatives. Antineoplastic

brand name

Tomudex (Zeneca).

Raltitrexed Preparation Products And Raw materials

Raw materials

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BOC Sciences Gold
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Jinan Zhongke Yitong Chemical Co., Ltd. Gold
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0531-88658009;88956078
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lxxcs@163.com;lxxcs@163.com
Nanjing Feihao Technology Co., Ltd. Gold
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025-58855213-
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J & K SCIENTIFIC LTD.
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010-82848833- ;010-82848833-
Email:
jkinfo@jkchemical.com;market6@jkchemical.com
Chemvon Biotechnology Co., Ltd
Tel:
021-50790412
Email:
info@chemvon.com
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