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胸苷合成酶 凋亡 类器官培养添加剂
/ Raltitrexed/雷替曲塞

Raltitrexed/雷替曲塞 {[allProObj[0].p_purity_real_show]}

货号：A222261 同义名： ZD1694; D1694

Raltitrexed是一种胸苷酸合成酶抑制剂，IC50 值为 9 nM，用于 L1210 细胞。

Raltitrexed/雷替曲塞 化学结构 CAS号：112887-68-0
Raltitrexed/雷替曲塞 化学结构
CAS号：112887-68-0
Raltitrexed/雷替曲塞 3D分子结构
CAS号：112887-68-0
Raltitrexed/雷替曲塞 化学结构 CAS号：112887-68-0
Raltitrexed/雷替曲塞 3D分子结构 CAS号：112887-68-0
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Raltitrexed/雷替曲塞 纯度/质量文件 产品仅供科研

货号：A222261 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Oxolinic acid ✔ 98+%
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 95%
Favipiravir ✔ 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Raltitrexed/雷替曲塞 生物活性

描述 Thymidylate synthase (TS) is critical enzyme for the synthesis of DNA- it converts dUMP (2′-deoxyuridine-5′-monophosphate) into dTMP (2′-deoxythymidine-5′-monophosphate). Raltitrexed is an antimetabolite drug used in chemotherapy, and was developed as a direct and specific inhibitor of TS[3]. Raltitrexed (0.5 μg/mL) shows typical apoptotic morphology, including nuclear shrinkage, fragmentation, chromatin condensation and apoptotic bodies in SGC7901 cells. Raltitrexed blocks the cell cycle at the G0/G1 phase, decreases in the mitochondrial membrane potential. Raltitrexed also increases the level of ROS, induces caspase-3-dependent apoptosis via activation of the mitochondria, and increases TS protein and mRNA expression levels[4]. Raltitrexed (1.5 nM) reduces the number of GM00637 cells, selectively induces gene conversions, but does not affect DSB-induced HR or NHEJ[5]. Raltitrexed (0, 5, 10, 11.5, 13.5, 15 mg/kg b/w, i.p.) increases the rates of resorbed embryos and growth retardation of murine model of NTDs in a dose dependent manner. Raltitrexed (11.5 mg/kg b/w) maximally inhibits the thymidylate synthase (TS) activity in embryonic tissue, decreases dTMP levels and while increases dUMP levels[6].

Raltitrexed/雷替曲塞 细胞实验

Cell Line
Concentration Treated Time Description References
Kyse150 cells 4 nM 24 hours To evaluate the inhibitory effect of Raltitrexed on Kyse150 cell proliferation and its radiosensitization effect. The results showed that Raltitrexed significantly enhanced the radiosensitivity of Kyse150 cells, increasing DNA double-strand breaks, G2/M arrest, and apoptosis. Cancer Cell Int. 2019 Feb 18;19:36.
TE-13 cells 4 nM 24 hours To evaluate the inhibitory effect of Raltitrexed on TE-13 cell proliferation and its radiosensitization effect. The results showed that Raltitrexed significantly enhanced the radiosensitivity of TE-13 cells, increasing DNA double-strand breaks, G2/M arrest, and apoptosis. Cancer Cell Int. 2019 Feb 18;19:36.
LAN-1 54 ± 11 nM (IC50) 72 hours To evaluate the growth inhibitory activity of Raltitrexed on MYCN-amplified neuroblastoma cells, the results showed that Raltitrexed had significant growth inhibitory effects on LAN-1 cells. Cancer Sci. 2020 Jul;111(7):2431-2439.
LAN-5 25 ± 7.8 nM (IC50) 72 hours To evaluate the growth inhibitory activity of Raltitrexed on MYCN-amplified neuroblastoma cells, the results showed that Raltitrexed had significant growth inhibitory effects on LAN-5 cells. Cancer Sci. 2020 Jul;111(7):2431-2439.
NB-39 16 ± 3.2 nM (IC50) 72 hours To evaluate the growth inhibitory activity of Raltitrexed on MYCN-amplified neuroblastoma cells, the results showed that Raltitrexed had significant growth inhibitory effects on NB-39 cells. Cancer Sci. 2020 Jul;111(7):2431-2439.
KELLY 8.9 ± 0.64 nM (IC50) 72 hours To evaluate the growth inhibitory activity of Raltitrexed on MYCN-amplified neuroblastoma cells, the results showed that Raltitrexed had significant growth inhibitory effects on KELLY cells. Cancer Sci. 2020 Jul;111(7):2431-2439.
SK-N-BE(2) 6.1 ± 2.1 nM (IC50) 72 hours To evaluate the growth inhibitory activity of Raltitrexed on MYCN-amplified neuroblastoma cells, the results showed that Raltitrexed had significant growth inhibitory effects on SK-N-BE(2) cells. Cancer Sci. 2020 Jul;111(7):2431-2439.
IMR-32 5.7 ± 1.8 nM (IC50) 72 hours To evaluate the growth inhibitory activity of Raltitrexed on MYCN-amplified neuroblastoma cells, the results showed that Raltitrexed had significant growth inhibitory effects on IMR-32 cells. Cancer Sci. 2020 Jul;111(7):2431-2439.
COLO 205 0, 0.2, 2, 20, 200, 2000 µM 90 minutes Evaluate the synergistic effect of Raltitrexed under hyperthermia conditions, results showed Raltitrexed had the highest HCSER score under hyperthermia. Cancer Biol Med. 2021 Mar 12;18(3):750–62.
DLD-1 0, 0.2, 2, 20, 200, 2000 µM 90 minutes Evaluate the synergistic effect of Raltitrexed under hyperthermia conditions, results showed Raltitrexed had the highest HCSER score under hyperthermia. Cancer Biol Med. 2021 Mar 12;18(3):750–62.
SW480 0, 0.2, 2, 20, 200, 2000 µM 90 minutes Evaluate the synergistic effect of Raltitrexed under hyperthermia conditions, results showed Raltitrexed had a high HCSER score under hyperthermia. Cancer Biol Med. 2021 Mar 12;18(3):750–62.
SW620 0, 0.2, 2, 20, 200, 2000 µM 90 minutes Evaluate the synergistic effect of Raltitrexed under hyperthermia conditions, results showed Raltitrexed had the highest HCSER score under hyperthermia. Cancer Biol Med. 2021 Mar 12;18(3):750–62.

Raltitrexed/雷替曲塞 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Swine Swine model Hepatic arterial infusion 1 mg/4 mg Not specified To study the pharmacokinetic characteristics of Raltitrexed in a swine model to determine the appropriate concentration and infusion time for hepatic arterial infusion chemotherapy. World J Gastroenterol. 2018 Jun 21;24(23):2501-2507
Caenorhabditis elegans CL2006 transgenic worms Treatment in liquid medium 1-50 μM Not specified Raltitrexed significantly reduced H3K9me2 levels in CL2006 worms, enhanced locomotive function, and reduced Aβ aggregates by up to 47%. ACS Med Chem Lett. 2023 Oct 12;14(11):1531-1536
BALB/C nude mice TE-13 xenograft model Intraperitoneal injection 7.5 mg/kg/day Continuous for 5 days, followed by a 2-day interval and another 5 days To evaluate the radiosensitization effect of Raltitrexed on TE-13 xenograft tumors. The results showed that Raltitrexed significantly enhanced the inhibitory effect of radiation on tumor growth, reducing tumor volume and weight, and decreasing the expression of Ki-67 and PCNA. Cancer Cell Int. 2019 Feb 18;19:36.

Raltitrexed/雷替曲塞 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02678806 HepatoCellular Carcinoma Not Applicable Recruiting November 1, 2022 China, Guangxi ... 展开 >> TaoBai Recruiting Nanning, Guangxi, China, 530000 Contact: Bai Tao, MD    +86 13878862632    25859373@qq.com 收起 <<
NCT01703910 Adenocarcinoma of Colon ... 展开 >> Adenocarcinoma of Rectum Metastatic Disease 收起 << Phase 2 Completed - Spain ... 展开 >> Hospital Universitario de Fuenlabrada Fuenlabrada, Madrid, Spain, 28950 Hospital Madrid Norte Sanchinarro Madrid, Spain, 28050 收起 <<
NCT01481545 Rectal Cancer Phase 2 Unknown July 2018 -

Raltitrexed/雷替曲塞 参考文献

[1]Van Cutsem E, Cunningham D, et al. Raltitrexed: current clinical status and future directions. Ann Oncol. 2002 Apr;13(4):513-22.

[2]Peters GJ, van Triest B, et al. Molecular downstream events and induction of thymidylate synthase in mutant and wild-type p53 colon cancer cell lines after treatment with 5-fluorouracil and the thymidylate synthase inhibitor raltitrexed. Eur J Cancer. 2000 May;36(7):916-24.

[3]Wilson KS, Malfair Taylor SC. Raltitrexed: optimism and reality. Expert Opin Drug Metab Toxicol. 2009;5(11):1447-1454.

[4]Xue S, Chen YX, Qin SK, et al. Raltitrexed induces mitochondrial‑mediated apoptosis in SGC7901 human gastric cancer cells. Mol Med Rep. 2014;10(4):1927-1934.

[5]Waldman BC, Wang Y, Kilaru K, et al. Induction of intrachromosomal homologous recombination in human cells by raltitrexed, an inhibitor of thymidylate synthase. DNA Repair (Amst). 2008;7(10):1624-1635.

[6]Dong Y, Wang X, Zhang J, et al. Raltitrexed's effect on the development of neural tube defects in mice is associated with DNA damage, apoptosis, and proliferation. Mol Cell Biochem. 2015;398(1-2):223-231.

Raltitrexed/雷替曲塞 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.91mL

2.18mL

1.09mL

21.81mL

4.36mL

2.18mL

Raltitrexed/雷替曲塞 技术信息

CAS号112887-68-0
分子式C21H22N4O6S
分子量 458.49
SMILES Code O=C(O)[C@@H](NC(C1=CC=C(N(C)CC2=CC3=C(N=C(C)NC3=O)C=C2)S1)=O)CCC(O)=O
MDL No. MFCD00864168
别名 ZD1694; D1694; TDX; ICI-D1694
运输蓝冰
InChI Key IVTVGDXNLFLDRM-HNNXBMFYSA-N
Pubchem ID 135400182
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 30 mg/mL(65.43 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Raltitrexed | ZD1694;D1694;TDX;ICI-D1694 | Apoptosis | Thymidylate Synthase | DNA/RNA Synthesis | AmBeed-信号通路专用抑制剂 | Raltitrexed/雷替曲塞 纯度/质量文件 | Raltitrexed/雷替曲塞 亚型比较 | Raltitrexed/雷替曲塞 生物活性 | Raltitrexed/雷替曲塞 临床数据 | Raltitrexed/雷替曲塞 参考文献 | Raltitrexed/雷替曲塞 实验方案 | Raltitrexed/雷替曲塞 技术信息

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