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R9156

Raltitrexed

Name: Raltitrexed
Brand: SIGMA

≥98% (HPLC), solid

别名:

L-Glutamic acid, N-((5-(((1,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl)methylamino)-2-thienyl)carbonyl), ICI-D-1694, ZD-1694

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关于此项目

经验公式（希尔记法）:

C₂₁H₂₂N₄O₆S

化学文摘社编号:

112887-68-0

分子量:

458.49

UNSPSC Code:

12352200

PubChem Substance ID:

329824044

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

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属性

Quality Level

100

assay

≥98% (HPLC)

form

solid

color

off-white to light yellow

solubility

H₂O: ≥10 mg/mL, DMSO: ≥40 mg/mL

originator

AstraZeneca

storage temp.

2-8°C

SMILES string

O=C1NC(C)=NC2=C1C=C(CN(C3=CC=C(C(N[C@H](CCC(O)=O)C(O)=O)=O)S3)C)C=C2

说明

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.

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.

Features and Benefits

This compound is a featured product for Apoptosis research. Click here to discover more featured Apoptosis products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

GHS06,GHS08

signalword

Danger

hcodes

H300,H360

pcodes

P201 - P301 + P310 + P330

Hazard Classifications

Acute Tox. 2 Oral - Repr. 1B

存储类别

6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

0000465216

0000062720

0000050063

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Discover Bioactive Small Molecules for Cell Cycle

Cell cycle phases (G1, S, G2, M) regulate cell growth, DNA replication, and division in proliferating cells.

Bioactive Molecules for Apoptosis

Apoptosis regulation involves multiple pathways and molecules for cellular homeostasis.

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CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil.

Helena Almqvist et al.

Nature communications, 7, 11040-11040 (2016-03-25)

Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery. We report here the first compound library screen based on

Thymidylate synthase inhibitor raltitrexed can induce high levels of DNA damage in MYCN-amplified neuroblastoma cells.

Ken Yamashita et al.

Cancer science, 111(7), 2431-2439 (2020-05-18)

MYCN gene amplification is consistently associated with poor prognosis in patients with neuroblastoma, a pediatric tumor arising from the sympathetic nervous system. Conventional anticancer drugs, such as alkylating agents and platinum compounds, have been used for the treatment of high-risk

全球贸易项目编号

货号	GTIN
R9156-10MG	04061833221204
R9156-50MG	04061833221211