Raltitrexed

別名：ZD-1694, ICI-D1694, D1694

製品コード：S1192 純度：99.92%

Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.

CAS No. 112887-68-0

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
100mg	JPY 85500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（14）

カスタマーフィードバック1例

製品安全説明書

現在のバッチを見る：純度： 99.92%

99.92

Raltitrexed関連製品

関連製品	TAS-102	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

Thymidylate Synthase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
human KB cells	Cytotoxicity assay	200 nM	96 h	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay, IC50=22 nM	25234128
human KB cells	Cytotoxicity assay		96 h	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay, IC50=5.9 nM	25234128
PC43-10 cells	Function assay		96 h	Inhibition of RFC (unknown origin) expressed in Chinese hamster PC43-10 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay, IC50=6.3 nM	25234128
RT16 cells	Proliferation assay		96 h	Antiproliferative activity against chinese hamster RT16 cells expressing human FRalpha assessed as reduction of viable cells after 96 hrs, IC50=15 nM	21879757
chinese hamster D4 cells	Proliferation assay		96 h	Antiproliferative activity against chinese hamster D4 cells expressing human FRbeta assessed as reduction of viable cells after 96 hrs, IC50=22 nM	21879757
R2/PCFT4 cells	Function assay		96 h	Inhibition of PCFT (unknown origin) expressed in Chinese hamster R2/PCFT4 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay, IC50=0.0995 μM	25234128
R2 cells	Cytotoxicity assay		96 h	Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay	24256410
R2 cells	Growth inhibition assay		96 h	Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay, IC50=0.0995 μM	24111942
human HepG2 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=1.3 μM	23490159
SGC7901 cells	Cytotoxicity assay		48 h	Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay, IC50=8.7 μM	23490159
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=12.6 μM	23490159
L1210 cell line	Growth inhibition assay			Growth inhibition of murine tumor L1210 cell line, IC50=9 nM	10508430
human IGROV1 cells	Proliferation assay			Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells, IC50=12.6 nM	18680275
L1210 mouse leukemia cells	Function assay			Compound was evaluated for inhibition of thymidylate synthase, partially purified from L1210 mouse leukemia cells that overproduce thymidylate synthase due to amplification of TS gene, Ki=0.418 μM	1372358
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明	Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.

In Vitro
In vitro	Raltitrexed induces a concentration-dependent amount of double-stranded DNA breaks. Raltitrexed increases the level of Bax protein up to a factor 5 in the Lovo and LS174T cell lines containing wt p53. ^[1] Raltitrexed leads to an increase of intracellular phosphoribosyl pyrophosphate (PRPD) in the case of the HCT-8 cell line, which suggests that the cytotoxic effects of raltitrexed combined with 5-FU may be due to the increased formation of 5-FU nucleotides. ^[2] Raltitrexed combined with SN-38 results in synergistic cytotoxicity at broad dose-effect ranges in human colon cancer cells. ^[3] Raltitrexed is actively taken up into cells and then undergoes rapid, extensive metabolism to a series of polyglutamates, which results in potent thymidylate synthase inhibition. Raltitrexed is delivered to the brain very quickly, and could be detected at 5 min in all brain tissues. ^[4] Raltitrexed combined folinic acid (5FU-FA) shows a clear schedule-dependent synergistic antiproliferative interaction as demonstrated by calculating combination indexes. Raltitrexed combined with Vorinostat produces synergistic effect paralleled by evident cell cycle perturbations with major S-phase arrest. ^[5] Raltitrexed is a specific, folate-based inhibitor of thymidylate synthase with activity in advanced colorectal cancer comparable with that of fluorouracil (5-fluorouracil) plus folinic acid. Raltitrexed‘s activity is enhanced by rapid cellular entry and polyglutamation, with the polyglutamated derivatives having approximately 100-fold greater inhibitory potency than the parent compound. ^[6]
実験結果図	Methods	Biomarkers	結果図	PMID
	Growth inhibition assay	Cell viability		30820189
	Western blot	Cleaved caspase-3 / Bax		30820189

In Vivo
In Vivo	Raltitrexed could be directly transported into the brain via the olfactory pathway in rats. ^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02618356	Unknown status	Metastatic Colon Cancer	Fudan University	December 25 2015	Phase 2
NCT02821559	Completed	Metastatic Colorectal Cancer	Centre Hospitalier Universitaire de Besancon\|Hospira now a wholly owned subsidiary of Pfizer	July 2012	Phase 2

参考
[1] Peters GJ, et al. Eur J Cancer, 2000, 36(7), 916-924. [2] Van Cutsem E, et al. Ann Oncol, 2002, 13(4), 513-522. [3] Aschele C, et al. Clin Cancer Res, 1998, 4(5), 1323-1330. [4] Wang D, et al. Cancer Chemother Pharmacol, 2006, 57(1), 97-104. [5] Di Gennaro E, et al. Cancer Biol Ther, 2009, 8(9), 782-791. + 展開

参考

+ 展開

化学情報

分子量	458.49	化学式	C₂₁H₂₂N₄O₆S
CAS No.	112887-68-0	SDF	Download Raltitrexed SDFをダウンロードする
Smiles	CC1=NC2=C(C=C(C=C2)CN(C)C3=CC=C(S3)C(=O)NC(CCC(=O)O)C(=O)O)C(=O)N1
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 92 mg/mL ( (200.65 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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