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Chemical Structure| 112887-68-0 Chemical Structure| 112887-68-0

Structure of Raltitrexed
CAS No.: 112887-68-0

Chemical Structure| 112887-68-0

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Raltitrexed is an inhibitor of thymidylate synthase with IC50 of 9 nM in L1210 cell.

Synonyms: ZD1694; D1694; TDX

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Product Details of Raltitrexed

CAS No. :112887-68-0
Formula : C21H22N4O6S
M.W : 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
Synonyms :
ZD1694; D1694; TDX
MDL No. :MFCD00864168
InChI Key :IVTVGDXNLFLDRM-HNNXBMFYSA-N
Pubchem ID :135400182

Safety of Raltitrexed

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Raltitrexed

DNA

Isoform Comparison

Biological Activity

In Vitro:

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. PMC6378748
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. PMC6378748
LAN-1 54 ± 11 nM 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. PMC7385364
LAN-5 25 ± 7.8 nM 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. PMC7385364
NB-39 16 ± 3.2 nM 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. PMC7385364
KELLY 8.9 ± 0.64 nM 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. PMC7385364
SK-N-BE(2) 6.1 ± 2.1 nM 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. PMC7385364
IMR-32 5.7 ± 1.8 nM 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. PMC7385364
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. PMC8330527
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. PMC8330527
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. PMC8330527
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. PMC8330527

In Vivo:

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. PMC6010942
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%. PMC10641905
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. PMC6378748

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02678806 HepatoCellular Carcinoma Not Applicable Recruiting November 1, 2022 China, Guangxi ... More >> TaoBai Recruiting Nanning, Guangxi, China, 530000 Contact: Bai Tao, MD    +86 13878862632    25859373@qq.com Less <<
NCT01703910 Adenocarcinoma of Colon ... More >> Adenocarcinoma of Rectum Metastatic Disease Less << Phase 2 Completed - Spain ... More >> Hospital Universitario de Fuenlabrada Fuenlabrada, Madrid, Spain, 28950 Hospital Madrid Norte Sanchinarro Madrid, Spain, 28050 Less <<
NCT01481545 Rectal Cancer Phase 2 Unknown July 2018 -
NCT00797719 Malignant Pleural Mesothelioma Phase 1 Phase 2 Recruiting July 2019 Canada, Ontario ... More >> University Health Network Recruiting Toronto, Ontario, Canada, M5G 2M9 Contact: John Cho, MD    416 946 2124    john.cho@rmp.uhn.on.ca    Principal Investigator: John Cho, MD Less <<
NCT03191487 Colorectal Neoplasms Not Applicable Withdrawn(no Financial agreeme... More >>nt) Less << November 2019 France ... More >> Institut Sainte Catherine Avignon Cedex 9, France, 84918 Institut de Cancérologie Montpellier Montpellier Cedex 5, France, 34298 CHRU de Nîmes - Hôpital Universitaire Carémeau Nîmes, France, 30029 CHRU de Strasbourg - Hôpital de Hautepierre Strasbourg, France, 67098 CHRU de Toulouse - Hôpital de Rangueil Toulouse Cedex 9, France, 31059 IUCT-Oncopole Toulouse, France, 31100 Less <<
NCT01869023 Advanced Malignant Pleural Mes... More >>othelioma Less << Phase 2 Active, not recruiting December 2017 Mexico ... More >> Instituto Nacional de Cancerología Mexico City, Mexico Less <<
NCT03179579 Gastric Cancer ... More >> Peritoneal Carcinomatosis Less << Phase 3 Not yet recruiting August 1, 2022 China, Guangdong ... More >> Department of Abdominal Surgery (Section 2), Affiliated Tumor Hospital of Guangzhou Medical University Not yet recruiting Guangzhou, Guangdong, China, 510095 Contact: Xianzi Yang, M.D    8602066673666    7097359@qq.com    Principal Investigator: shuzhong cui, M.D Less <<
NCT02376452 Colorectal Carcinoma Phase 2 Unknown December 2016 China, Shanghai ... More >> Fudan University Cancer Hospital Recruiting ShangHai, Shanghai, China Contact: Jin Li, PhD, M.D    862164175590 ext 1108    fudanlijin@163.com Less <<
NCT02723253 Rectal Neoplasms Phase 2 Completed - -
NCT00002902 Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << Phase 1 Completed - United States, Pennsylvania ... More >> University of Pennsylvania Cancer Center Philadelphia, Pennsylvania, United States, 19104 Less <<
NCT00004254 Malignant Mesothelioma Phase 2 Completed - Italy ... More >> Ospedale Bellaria Bologna, Italy, I-40139 Istituto Nazionale per la Ricerca sul Cancro Genoa, Italy, 16132 Istituto Nazionale per lo Studio e la Cura dei Tumori Naples, Italy, 80131 Universita Degli Studi di Udine Udine, Italy, 33100 Netherlands Antoni van Leeuwenhoekhuis Amsterdam, Netherlands, 1066 CX Vrije Universiteit Medisch Centrum Amsterdam, Netherlands, 1117 MB Less <<
NCT00003109 Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << Phase 1 Completed - United States, Pennsylvania ... More >> Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 Less <<
NCT01532804 Metastatic Colorectal Cancer Phase 2 Active, not recruiting December 2018 France ... More >> Val d'Aurelle Cancer Institute Montpellier, France, 34298 Less <<
NCT00002828 Colorectal Cancer Phase 1 Completed - United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less <<
NCT00001341 Neoplasm Phase 1 Completed - United States, Maryland ... More >> National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 Less <<
NCT00004920 Malignant Mesothelioma Phase 3 Completed - -
NCT02965248 Locally Advanced Colorectal Ca... More >>ncer Less << Phase 3 Recruiting November 2023 China, Shanghai ... More >> Fudan University Shanghai Cancer Center Recruiting Shanghai, Shanghai, China, 200032 Contact: Guoxiang Cai, M.D. Ph.D.    +86 13611831623    gxcai@fudan.edu.cn Less <<
NCT02453490 Colorectal Cancer ... More >> Liver Metastasis Less << Phase 3 Recruiting September 2018 China, Guangdong ... More >> The Affiliated Tumor Hospital of Zhongshan University Not yet recruiting Guangzhou, Guangdong, China, 510060 Principal Investigator: Zhi-Zhong Pan, MD/PHD          China, Hubei Wuhan Union Hospital Not yet recruiting Wuhan, Hubei, China, 430022 Principal Investigator: Kai-Xiong Tao, MD/PHD          Zhongnan Hospital Affiliated to Wuhan University Not yet recruiting Wuhan, Hubei, China, 430071 Principal Investigator: Bing Xiong, MD          China, Shanghai Changhai Hospital of Shanghai Recruiting Shanghai, Shanghai, China, 200433 Principal Investigator: Wei Zhang, MD          China, Zhejiang The First Affiliated Hospital of College of Medicine Zhejiang University Not yet recruiting Hangzhou, Zhejiang, China, 310003 Principal Investigator: Jianjiang Lin, M.D.          Second Affiliated Hospitalof Zhejiang University School of Medicine Recruiting Hangzhou, Zhejiang, China, 310009 Contact: Ke-Feng Ding, PhD/MD    86-571-87784827    dingkefeng@zju.edu.cn    Principal Investigator: Ke-Feng Ding, PhD/MD          Sir Run Run Shaw Hospital, Zhejiang University School of Medicine Recruiting Hangzhou, Zhejiang, China, 310016 Principal Investigator: Xuefeng Huang, M.D.          Jinhua People's Hospital Recruiting Jinhua, Zhejiang, China, 321000 Principal Investigator: Jinlin Du, M.D.          The second hospital of Ningbo City Recruiting Ningbo, Zhejiang, China, 315010 Principal Investigator: Xiao-Yu Dai, MD Less <<
NCT02631564 - Unknown December 2018 China, Shanghai ... More >> Fudan University Zhongshan Hospital Recruiting Shanghai, Shanghai, China, 200032 Contact: Bo Zhou, M.D,Ph.D    8621-18616880602 Less <<
NCT00590278 Inoperable or Recurrent Rectal... More >> Cancer Less << Phase 2 Completed - Turkey ... More >> Research Site Istanbul, Turkey Less <<
NCT00234429 Colorectal Cancer Phase 2 Phase 3 Completed - Spain ... More >> Research Site A Coruna, Spain Research Site Barcelona, Spain Research Site Burgos, Spain Research Site Gijon, Spain Research Site Leon, Spain Research Site Madrid, Spain Research Site Oviedo, Spain Research Site Pamplona, Spain Research Site Valladolid, Spain Less <<
NCT02821559 Metastatic Colorectal Cancer Phase 2 Completed - France ... More >> CHRU de Besançon Besançon, France Less <<
NCT00003528 Recurrent Childhood Acute Lymp... More >>hoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Less << Phase 1 Completed - Switzerland ... More >> Swiss Pediatric Oncology Group - Geneva Geneva, Switzerland, 1205 Less <<
NCT02485548 Head and Neck Squamous Cell Ca... More >>ncer Less << Phase 3 Unknown June 2018 China, Jiangsu ... More >> Jiangsu Cancer Hospital Recruiting Nanjing, Jiangsu, China, 210009 Contact: Xuesong Jiang, M.D.       13851700790@126.com    Sub-Investigator: Xuesong Jiang, M.D. Less <<
NCT01959061 Colorectal Cancer Metastatic Phase 4 Recruiting December 2017 China, Shanghai ... More >> Zhongshan Hospital Fudan University Recruiting Shanghai, Shanghai, China, 2000032 Contact: Jianhua Wang Less <<
NCT02992886 Rectal Neoplasms Malignant Phase 2 Recruiting September 2022 China, Beijing ... More >> Department of Radiation Oncology, Cancer Institute and Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College Recruiting Beijing, Beijing, China, 100021 Contact: Wenyang Liu, MD       liuwenyang26@163.com Less <<
NCT01732380 Inoperable Esophageal Cancer S... More >>tage I-III Less << Phase 2 Unknown July 2013 China, Jiangsu ... More >> The First People`s Hospital of Lianyungang Recruiting Lianyungang, Jiangsu, China, 222002 Contact: Xiaodong Jiang, Doctor       jxdysy1970@163.com Less <<
NCT03126071 Advanced Colorectal Cancer Phase 2 Recruiting February 15, 2020 China, Jiangsu ... More >> Jiangsu Cancer Institute & Hospital Recruiting Nanjing, Jiangsu, China, 210009 Contact: Liangjun Zhu    +8613905199123    zhulj98@foxmail.com    Contact: Yuejiao Zhong    +861370575447    zhongyuejiao@163.com    Nantong Tumor Hospital Active, not recruiting Nantong, Jiangsu, China, 226000 The First Affiliated Hospital of Soochow University Recruiting Suzhou, Jiangsu, China, 215000 Contact: Chunrong Zhu, M.D.    +8613063870566    zcr050311@163.com    Contact: Feng Xiong    +8613270971002    greenlemontea@126.com    China, Shanghai Rui Jin Hospital Shanghai Jiao Tong University School of Medicine Not yet recruiting Shanghai, Shanghai, China, 200025 Contact: Jun Zhang, M.D. Less <<
NCT01836120 Gastric Cancer Phase 2 Unknown June 2017 China, Hebei ... More >> Hebei Tumor Hospital Shijiazhuang, Hebei, China, 050011 Less <<
NCT02072317 Advanced Gastric Cancer Phase 2 Unknown March 2016 China, Shanghai ... More >> Cancer hospital Fudan University Recruiting Shanghai, Shanghai, China, 200032 Contact: GUO WEI JIAN, doctor    13816066360    guoweijian1@hotmail.com Less <<
NCT00002893 Colorectal Cancer Phase 3 Unknown - United Kingdom ... More >> Velindre Hospital Cardiff, Wales, United Kingdom, CF4 7XL Less <<
NCT03585530 Esophagus Squamous Cell Carcin... More >>oma Less << Phase 2 Not yet recruiting July 15, 2022 -
NCT03083613 Gastric Cancer ... More >> Gastroesophageal Junction Adenocarcinoma Less << Phase 2 Unknown December 2018 China ... More >> Chinese Academy of Medical Sciences Recruiting Beijing, China, 10000 Contact: Ai ping Zhou    8610-87788145    zhouap1825@126.com Less <<
NCT03053167 ColoRectal Cancer Phase 2 Recruiting December 2020 China, Liaoning ... More >> The First Hospital of China Medical University Recruiting Shenyang, Liaoning, China, 110001 Contact: Yunpeng Liu, MD., PhD    86-24-83282312    cmuliuyunpeng@hotmail.com    Principal Investigator: Yunpeng Liu, MD., PhD. Less <<
NCT03398512 Peritoneal Metastases From Col... More >>orectal Cancer Less << Not Applicable Recruiting December 31, 2020 China, Hubei ... More >> Wuhan University Recruiting Wuhan, Hubei, China Contact: Bin Xiong    +86 27 67813152    jyn1983@163.com Less <<
NCT02562599 Nasopharyngeal Carcinoma Phase 2 Unknown August 2018 China, Hubei ... More >> Hubei Cancer hospital Recruiting Wu Han, Hubei, China, 430079 Contact: Han Guang, PH.D          Principal Investigator: Hu Desheng, M.D Less <<
NCT02618356 Metastatic Colon Cancer Phase 2 Recruiting November 2017 China, Shanghai ... More >> Fudan University Cancer Hospital Recruiting ShangHai, Shanghai, China, 200032 Contact: Wei Jian Guo    13816066360    mingzhuhuang0718@163.com Less <<
NCT03344614 Colorectal Cancer Phase 2 Recruiting July 1, 2019 China, Beijing ... More >> Chinese PLA General Hospital (301 Military Hospital) Recruiting Beijing, Beijing, China, 100853 Contact: Haiyan Si, M.D.    +8613911070673    sihaiyan2008@sina.com Less <<
NCT03196843 Head and Neck Squamous Cell Ca... More >>rcinoma Less << Phase 4 Recruiting August 2022 China, Liaoning ... More >> Lv Xiupeng Recruiting Dalian, Liaoning, China, 116000 Contact: Xiupeng Lv, M.D.    18098876707    lvxiupeng@foxmail.com Less <<
NCT01348412 Colorectal Cancer ... More >> Liver Metastases Less << Phase 2 Completed - France ... More >> Centre Georges François Leclerc Dijon, France, 21000 Less <<
NCT03392103 Gastric Cancer Phase 2 Recruiting December 2019 China, Hubei ... More >> Zhongnan Hopital of Wuhan University Recruiting Wuhan, Hubei, China, 430071 Contact: Fuxiang Zhou, M.D.    +86(0)2767813155    fuxiang.zhou@whu.edu.cn    Contact: Jing Dai, M.D.    +86(0)2767813155    daijing1116@163.com Less <<
NCT02557490 Colon Cancer Liver Metastasis Phase 4 Unknown December 2017 China, Beijing ... More >> Beijing Cancer Hospital Recruiting Beijing, Beijing, China, 100142 Contact: Zhu Xu, Master    0086-10-88195476    zhux387@263.net    Principal Investigator: Zhu Xu, Master Less <<
NCT04761185 Colorectal Cancer|Raltitrexed|... More >>HIPEC Less << PHASE1 UNKNOWN 2022-12-31 Fudan University Shanghai Canc... More >>er Center, Shanghai, 200032, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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