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Raltitrexed

Product Name
Raltitrexed
CAS No.
112887-68-0
Chemical Name
Raltitrexed
Synonyms
Tomudex;TDX;D1694;CS-664;ZD-1694;Retitrose;ICI-D-1694;ZEN-D-1694;Raltirexed;Raltitrexe
CBNumber
CB1222070
Molecular Formula
C21H22N4O6S
Formula Weight
458.49
MOL File
112887-68-0.mol
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Raltitrexed Property

Melting point:
176-1800C
Density 
1.49±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
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

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
HS Code 
2934.99.4700
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H300Fatal if swallowed

H360May damage fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
R9156
Product name
Raltitrexed monohydrate
Purity
≥98% (HPLC), solid
Packaging
10mg
Price
$158
Updated
2024/03/01
Sigma-Aldrich
Product number
R9156
Product name
Raltitrexed monohydrate
Purity
≥98% (HPLC), solid
Packaging
50mg
Price
$628
Updated
2024/03/01
TCI Chemical
Product number
R0208
Product name
Raltitrexed
Purity
>98.0%(HPLC)
Packaging
50mg
Price
$310
Updated
2024/03/01
TCI Chemical
Product number
R0208
Product name
Raltitrexed
Purity
>98.0%(HPLC)
Packaging
250mg
Price
$1081
Updated
2024/03/01
Cayman Chemical
Product number
26079
Product name
Raltitrexed
Packaging
10mg
Price
$62
Updated
2024/03/01
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Raltitrexed Chemical Properties,Usage,Production

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

Definition

ChEBI: ICI D1694 is a N-acyl-amino acid.

brand name

Tomudex (Zeneca).

Biochem/physiol Actions

Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.

Clinical Use

Treatment of colorectal cancer when fluorouracil and folinic acid cannot be used

Drug interactions

Potentially hazardous interactions with other drugs
Antipsychotics: avoid with clozapine, increased risk of agranulocytosis.
Folic and folinic acid: impairs cytotoxic action - avoid.

Metabolism

Raltitrexed is actively transported into cells and metabolised to active polyglutamate forms.
The remainder of a dose is not metabolised and is excreted unchanged, about 50% of a dose appearing in the urine, and about 15% in the faeces.

Raltitrexed Preparation Products And Raw materials

Raw materials

Preparation Products

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Raltitrexed Suppliers

Jinan Zhongke Yitong Chemical Co., Ltd.
Tel
0531-88658009
Fax
0531-88956078
Email
lxxcs@163.com
Country
China
ProdList
85
Advantage
58
Nanjing Feihao Technology Co., Ltd.
Tel
025-58855213 15366065068
Email
hongjiling@feihongtec.com
Country
China
ProdList
743
Advantage
58
Zibo ChemYuan Pharmaceutical Co., Ltd.
Tel
0533-2766162 13011630869
Fax
0533-2766162
Email
zbchemyuan@163.com
Country
China
ProdList
56
Advantage
58
Nanjing hongshenghuo Biotechnology Co., Ltd
Tel
025-58311670 18020159086
Email
54604129@qq.com
Country
China
ProdList
180
Advantage
58
Jiangsu Xinglin Pharmaceutical Co., Ltd
Tel
18036652731
Email
2843986978@qq.com
Country
China
ProdList
54
Advantage
58
FarmaSino Pharmaceuticals (Jiangsu) Co.,Ltd
Tel
25-8690-7345 18651693585
Email
zfx@farmasino.com
Country
China
ProdList
129
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chemvon Biotechnology Co., Ltd
Tel
021-50790412
Fax
+86-21-50790419
Email
info@chemvon.com
Country
China
ProdList
371
Advantage
57
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Jia Xing Isenchem Co.,Ltd
Tel
0573-85285100 18627885956
Fax
0573-85285100
Email
isenchem@163.com
Country
China
ProdList
9413
Advantage
66
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View Lastest Price from Raltitrexed manufacturers

Nanjing Fred Technology Co., Ltd
Product
Raltitrexed 112887-68-0
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%, Single impurity<0.1
Supply Ability
1 ton
Release date
2023-12-26
Guangzhou PI PI BIOTECH INC
Product
Raltitrexed 112887-68-0
Price
US $0.00-0.00/mg
Min. Order
10mg
Purity
90%+
Supply Ability
10g
Release date
2021-09-20
Zhuozhou Wenxi import and Export Co., Ltd
Product
Raltitrexed 112887-68-0
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-08-11

112887-68-0, RaltitrexedRelated Search:


  • RALTITREXED
  • (s)-2-[(1-{5-[methyl-(2-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylmethyl)-amino]-thiophen-2-yl}-methanoyl)-amino]-pentanedioic acid
  • ICI-D-1694
  • N-[[5-[[(1,4-Dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-L-glutamic Acid
  • Tomudex
  • ZD-1694
  • L-Glutamic acid, N-[[5-[[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]-
  • (S)-2-(5-(METHYL((2-METHYL-4-OXO-3,4-DIHYDROQUINAZOLIN-6-YL)METHYL)AMINO)THIOPHENE-2-CARBOXAMIDO)PENTANEDIOIC ACID
  • 4-nitro-2-thiohenic acid
  • CS-664
  • (2s)-2-[[5-[methyl-[(2-methyl-4-oxo-1h-quinazolin-6-yl)methyl]amino]thiophene-2-carbonyl]amino]pentanedioic Acid
  • (2S)-2-[5-[N-Methyl-N-[[(3,4-dihydro-2-methyl-4-oxoquinazolin)-6-yl]methyl]amino]-2-thienylcarbonylamino]glutaric acid
  • (S)-2-[5-[N-Methyl-N-[[(3,4-dihydro-2-methyl-4-oxoquinazolin)-6-yl]methyl]amino]-2-thienylcarbonylamino]glutaric acid
  • ZEN-D-1694
  • Raltitrexed(ToMudex)
  • Raltirexed
  • (S)-2-(5-(Methyl((2-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)-methyl)amino)thiophene-2-carboxam
  • D1694
  • Raltitrexed (ZD1694
  • N-[[5-[[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]- L-glutamic acid
  • L-Glutamic acid, N-((5-(((1,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl)methylamino)-2-thienyl)carbonyl)- monohydrate
  • Raltitrexed monohydrate
  • Raltitrexed, >=99%
  • Raltitrexed USP/EP/BP
  • (S)-2-(5-(Methyl((2-methyl-4-oxo-1,4-dihydroquinazolin-6-yl)methyl)amino)thiophene-2-carboxamido)pentanedioic acid
  • (S)-2-[(1-{5-[Methyl-(2-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylmethyl)-amino]-thiophen-2-yl}-methanoyl)-amino]-pentanedioic acid
  • Raltitrexe
  • Retitrose
  • TDX
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  • C21H22N4O6S
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  • 112887-68-0