ChemicalBook >> CAS DataBase List >>Raltitrexed

Raltitrexed

CAS No.
112887-68-0
Chemical Name:
Raltitrexed
Synonyms
Tomudex;TDX;D1694;CS-664;ZD-1694;Retitrose;ZEN-D-1694;ICI-D-1694;Raltirexed;Raltitrexe
CBNumber:
CB1222070
Molecular Formula:
C21H22N4O6S
Molecular Weight:
458.49
MDL Number:
MFCD00864168
MOL File:
112887-68-0.mol
MSDS File:
SDS
Last updated:2023-12-27 16:49:21

Raltitrexed Properties

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)
NCI Dictionary of Cancer Terms ICI D1694; raltitrexed
FDA UNII FCB9EGG971
NCI Drug Dictionary raltitrexed
ATC code L01BA03

Pharmacokinetic data

Protein binding 93%
Excreted unchanged in urine 40-50%
Volume of distribution 548 Litres
Biological half-life 198 / Increased

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS06,GHS08
Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS06,GHS08
Signal word  Danger
Signal word  Danger
Hazard statements  H300-H360
Hazard statements  H300-H360
Precautionary statements  P201-P301+P310+P330
Precautionary statements  P201-P301+P310+P330
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
NFPA 704
0
2 0

Raltitrexed price More Price(53)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich R9156 Raltitrexed monohydrate ≥98% (HPLC), solid 112887-68-0 10mg $158 2024-03-01 Buy
Sigma-Aldrich R9156 Raltitrexed monohydrate ≥98% (HPLC), solid 112887-68-0 50mg $628 2024-03-01 Buy
TCI Chemical R0208 Raltitrexed >98.0%(HPLC) 112887-68-0 50mg $310 2024-03-01 Buy
TCI Chemical R0208 Raltitrexed >98.0%(HPLC) 112887-68-0 250mg $1081 2024-03-01 Buy
Cayman Chemical 26079 Raltitrexed 112887-68-0 10mg $62 2024-03-01 Buy
Product number Packaging Price Buy
R9156 10mg $158 Buy
R9156 50mg $628 Buy
R0208 50mg $310 Buy
R0208 250mg $1081 Buy
26079 10mg $62 Buy

Raltitrexed Chemical Properties,Uses,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.

132463-02-6
112887-68-0
Synthesis of Raltitrexed from Diethyl N-[5-[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N-methylamino]-2-thenoyl]-L-glutamate

Raltitrexed Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 353)Suppliers
Supplier Tel Email Country ProdList Advantage
Hangzhou MolCore BioPharmatech Co.,Ltd.
+86-057181025280; +8617767106207 sales@molcore.com China 49739 58
Henan Tengmao Chemical Technology Co. LTD
+8615238638457 salesvip2@hntmhg.com China 415 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21691 55
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 967 58
Jilin Chinese Academy of Sciences - Yanshen Technology Co., Ltd.
0431-80514535 13634302652 Extension@chemextension.com CHINA 967 58
Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28180 58
Casorganics US Corp
+17326109938 sales@casorganics.com CHINA 174 58
Xiamen AmoyChem Co., Ltd
+86-592-6051114 +8618959220845 sales@amoychem.com China 6387 58
Hubei xin bonus chemical co. LTD
86-13657291602 linda@hubeijusheng.com CHINA 22968 58

View Lastest Price from Raltitrexed manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Raltitrexed pictures 2024-04-10 Raltitrexed
112887-68-0
US $0.00-0.00 / mg 10mg 90%+ 10g Guangzhou PI PI BIOTECH INC
Raltitrexed pictures 2023-12-27 Raltitrexed
112887-68-0
US $110.00-90.00 / kilogram 1kilogram 99% 10 tons/per week Henan Tengmao Chemical Technology Co. LTD
Raltitrexed pictures 2023-12-26 Raltitrexed
112887-68-0
US $0.00-0.00 / kg 1kg 99%, Single impurity<0.1 1 ton Nanjing Fred Technology Co., Ltd
  • Raltitrexed pictures
  • Raltitrexed
    112887-68-0
  • US $0.00-0.00 / mg
  • 90%+
  • Guangzhou PI PI BIOTECH INC
  • Raltitrexed pictures
  • Raltitrexed
    112887-68-0
  • US $110.00-90.00 / kilogram
  • 99%
  • Henan Tengmao Chemical Technology Co. LTD
  • Raltitrexed pictures
  • Raltitrexed
    112887-68-0
  • US $0.00-0.00 / kg
  • 99%, Single impurity<0.1
  • Nanjing Fred Technology Co., Ltd

Raltitrexed Spectrum

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 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 (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 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% CS-664 (2s)-2-[[5-[methyl-[(2-methyl-4-oxo-1h-quinazolin-6-yl)methyl]amino]thiophene-2-carbonyl]amino]pentanedioic Acid D1694 Raltitrexed (ZD1694 Raltitrexed USP/EP/BP (S)-2-(5-(Methyl((2-methyl-4-oxo-1,4-dihydroquinazolin-6-yl)methyl)amino)thiophene-2-carboxamido)pentanedioic acid Tomudex (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 112887-68-0 12887-68-0 112887-68-7 C21H22N4O6S C21H22N4O6SxH2O Active Pharmaceutical Ingredients Raltitrexed Intermediates & Fine Chemicals Pharmaceuticals Inhibitors 112887-68-0