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Chemical Structure| 135558-11-1 Chemical Structure| 135558-11-1

Structure of Lobaplatin
CAS No.: 135558-11-1

Chemical Structure| 135558-11-1

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Lobaplatin is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links.

Synonyms: D-19466

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Product Details of Lobaplatin

CAS No. :135558-11-1
Formula : C9H18N2O3Pt
M.W : 397.33
SMILES Code : CC([O-]1)C([O-][Pt]21[NH2+]CC(CC3)C3C[NH2+]2)=O
Synonyms :
D-19466
MDL No. :MFCD00866545

Safety of Lobaplatin

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

Related Pathways of Lobaplatin

DNA
pyroptosis

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SMMC7721 cells 1.536 µg/mL 117.2 hours To investigate the radiosensitization effect of LBP on SMMC7721 cells, results showed that LBP significantly increased 125I-induced apoptosis. Cell Death Dis. 2019 Oct 3;10(10):744
HepG2 cells 5.972 µg/mL 117.2 hours To investigate the radiosensitization effect of LBP on HepG2 cells, results showed that LBP significantly increased 125I-induced apoptosis. Cell Death Dis. 2019 Oct 3;10(10):744
SOSP-9607 7.94 µg/mL (SOSP-9607-Vector) and 10.04 µg/mL (SOSP-9607-FUBP1) 24 hours To investigate the effect of FUBP1 overexpression on the sensitivity of SOSP-9607 cells to Lobaplatin. Results showed that FUBP1 overexpression increased the resistance of SOSP-9607 cells to Lobaplatin. MedComm (2020). 2023 May 9;4(3):e257
MG63 14.95 µg/mL (MG63-Vector) and 28.36 µg/mL (MG63-FUBP1) 24 hours To investigate the effect of FUBP1 overexpression on the sensitivity of MG63 cells to Lobaplatin. Results showed that FUBP1 overexpression increased the resistance of MG63 cells to Lobaplatin. MedComm (2020). 2023 May 9;4(3):e257
HCT116 cells 0, 8, 16, 32 μg/ml 8 hours To investigate the effect of Lobaplatin on the viability of HCT116 cells and its induction of pyroptosis. Results showed that Lobaplatin inhibited cell viability in a dose-dependent manner and induced cell swelling and large bubbles emerging from the plasma membrane, with TEM revealing multiple pores in the membrane. Cell Death Dis. 2019 Feb 25;10(3):193
HT-29 cells 0, 8, 16, 32 μg/ml 8 hours To investigate the effect of Lobaplatin on the viability of HT-29 and HCT116 cells and its induction of pyroptosis. Results showed that Lobaplatin inhibited cell viability in a dose-dependent manner and induced cell swelling and large bubbles emerging from the plasma membrane, with TEM revealing multiple pores in the membrane. Cell Death Dis. 2019 Feb 25;10(3):193
SaOS-2 osteosarcoma cells 10 μg/mL 24 hours To investigate the effect of rhIL-6 intervention on Lobaplatin resistance, results showed that rhIL-6 pretreatment reduced the sensitivity of osteosarcoma cells to Lobaplatin. Cancer Cell Int. 2021 Oct 30;21(1):581
MCF-7 cells 5, 10, 50 mg/L 24 hours To investigate the effect of lobaplatin on MCF-7 cell proliferation and apoptosis. Results showed that lobaplatin significantly reduced cell proliferation and increased cell apoptotic percentage. Drug Des Devel Ther. 2018 Oct 29;12:3563-3571
Y79 retinoblastoma cells 5, 10, 20, 40 µg/ml 24, 48, 72 hours To evaluate the inhibitory effect of lobaplatin on Y79 cell proliferation, results showed that lobaplatin significantly inhibited cell proliferation in a dose- and time-dependent manner and induced apoptosis. Int J Oncol. 2020 Sep;57(3):697-706

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Osteosarcoma xenograft model Subcutaneous injection 3 mg/kg Every 3 days for 6 weeks Evatanepag, as an EP2 receptor agonist, was used to stimulate the arachidonic acid metabolic pathway in FUBP1-silenced osteosarcoma cells to verify that FUBP1 promotes lobaplatin resistance in osteosarcoma cells through PTGES and the arachidonic acid metabolic pathway. MedComm (2020). 2023 May 9;4(3):e257
Nude mice Subcutaneous xenograft model Intraperitoneal injection 3 mg/kg Every 3 days for 6 weeks To investigate the effect of FUBP1 on Lobaplatin resistance in vivo. Results showed that FUBP1 overexpression increased tumor resistance to Lobaplatin, while FUBP1 knockdown increased tumor sensitivity to Lobaplatin. MedComm (2020). 2023 May 9;4(3):e257
BALB/c nude mice Subcutaneous xenograft tumor model Intraperitoneal injection 11 mg/kg Tumor volume was monitored every 3 days, and mice were sacrificed at the end of the experiment To investigate the inhibitory effect of Lobaplatin on colon cancer xenograft tumors. Results showed that Lobaplatin significantly inhibited tumor growth, and GSDME knockout did not affect the inhibitory effect of Lobaplatin on tumor formation. Cell Death Dis. 2019 Feb 25;10(3):193
BALB/c nude mice Y79 retinoblastoma xenograft model Tail vein injection 750 µg/kg Every 3 days for 1 or 2 weeks To evaluate the inhibitory effect of lobaplatin on Y79 xenograft tumors, results showed that lobaplatin significantly inhibited tumor growth and was more effective than carboplatin. Int J Oncol. 2020 Sep;57(3):697-706

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03731442 Esophageal Cancer Phase 3 Recruiting October 31, 2027 China, Beijing ... More >> Department of Radiation Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD Less <<
NCT03328234 IMRT With or Without Concurren... More >>t Chemotherapy for Esophageal Cancer Less << Phase 3 Recruiting December 31, 2022 China ... More >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, China, 100021 Contact: Xin Wang, MD    +861013311583220    beryl_wx2000@163.com Less <<
NCT03308552 Esophageal Neoplasms Phase 3 Recruiting August 30, 2021 China, Beijing ... More >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD Less <<
NCT02856126 Hepatocellular Carcinoma Phase 3 Recruiting August 2018 China, Guangdong ... More >> Dongguan People's Hospital Recruiting Dongguan, Guangdong, China, 523059 Contact: Wusheng Yu, MD    13827285010    yuwusheng1998@126.com    Cancer Center Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Ming Shi, MD    8620-87343115    shiming@mail.sysu.edu.cn    The First Affiliated Hospital, Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Guosheng Tan, MD    13725254145    tgs1976@163.com    Guangzhou Twelfth People 's Hospital Recruiting Guangzhou, Guangdong, China, 510620 Contact: Yuanmin Zhou, MD    15521278919    13430288977@139.com    Principal Investigator: Jinghua Chen, MD          Kaiping Central Hospital Recruiting Kaiping, Guangdong, China, 529300 Contact: Shijie Zhang, MD    13717287622    Shijie_9262511@163.com    China, Hunan The First Affiliated Hospital of University Of South China Recruiting Hengyang, Hunan, China, 421001 Contact: Xiaoping Wu, MD    13975486015    wxp19730806@sina.com    China, Shanxi The First Affiliated Hospital Of Xi'an Jiaotong University Recruiting Xi'an, Shanxi, China, 710061 Contact: Xin Zheng, MD    13649265446    183421344@qq.com Less <<
NCT01229839 Hepatocellular Carcinoma Phase 3 Unknown August 2018 China, Guangdong ... More >> Cancer Center Sun Yat-sen University Recruiting Guangzhou, Guangdong, China Contact: Ming Shi, MD    86-2087343582 ext 86-2087343582    shiming@mail.sysu.edu.cn    Contact: Rong Ping Guo, MD    86-2087343117 ext 86-2087343117    guorongp@mail.sysu.edu.cn    Principal Investigator: Ming Shi, MD Less <<
NCT01259414 Hepatocellular Carcinoma Phase 3 Unknown January 2017 China, Guangdong ... More >> Cancer Center Sun Yat-sen University Recruiting Guangzhou, Guangdong, China Contact: Ming Shi    86-2087343582 ext 86-2087343582    shiming@mail.sysu.edu.cn    Contact: Ping Rong Guo    86-2087343117 ext 86-2087343117    guorongp@mail.sysu.edu.cn    Principal Investigator: Ming Shi Less <<
NCT02435953 Hepatocellular Carcinoma ... More >> Chemoembolization, Therapeutic Ablation Techniques, RFA Less << Phase 4 Recruiting - China, Guangdong ... More >> Minimally Invasive Interventional Division, Medical Imaging Center, Sun Yat-sen University Cancer Center, Recruiting Guangzhou, Guangdong, China, 500060 Contact: Ming Zhao, doctor    +86 020 87343272    zhaoming@sysucc.org.cn    Contact: Tao Pan, doctor    +86 020 87343271    pantao0909@hotmail.com Less <<
NCT02973685 HepatoCellular Carcinoma Phase 3 Recruiting October 2019 China, Guangdong ... More >> Dongguan People's Hospital Recruiting Dongguan, Guangdong, China, 523059 Contact: Wusheng Yu, MD    13827285010    yuwusheng1998@126.com    Cancer Center Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Ming Shi, MD    8620-87343115    shiming@mail.sysu.edu.cn    The First Affiliated Hospital, Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Guosheng Tan, MD    13725254145    tgs1976@163.com    Guangzhou Twelfth People's Hospital Recruiting Guangzhou, Guangdong, China, 510620 Contact: Yuanmin Zhou, MD    15521278919    13430288977@139.com    Principal Investigator: Jinghua Chen, MD          Kaiping Central Hospital Recruiting Kaiping, Guangdong, China, 529300 Contact: Shijie Zhang, MD    13717287622    Shijie_9262511@163.com    China, Hunan The First Affiliated Hospital of University Of South China Recruiting Hengyang, Hunan, China, 421001 Contact: Xiaoping Wu, MD    13975486015    wxp19730806@sina.com    China, Shanxi The First Affiliated Hospital Of Xi'an Jiaotong University Recruiting Xi'an, Shanxi, China, 710061 Contact: Xin Zheng, MD    13649265446    183421344@qq.com Less <<
NCT03048123 Hepatocellular Carcinoma Phase 2 Completed - China, Guangdong ... More >> Cancer Center Sun Yat-sen University Guangzhou, Guangdong, China, 510060 Less <<
NCT02430974 Carcinoma, Non-Small-Cell Lung Phase 2 Unknown January 2018 -
NCT03196869 Locally Advanced Head and Neck... More >> Squamous Cell Carcinoma Less << Phase 2 Recruiting August 12, 2022 China, Guizhou ... More >> Cancer Hospital of Guizhou Medical University Recruiting Guiyang, Guizhou, China, 550000 Contact: Feng Jin, Bachelor    0851-86512802    jinf8865@yahoo.com.cn    Sub-Investigator: Weili Wu, master          Sub-Investigator: Jinhua Long, master          Sub-Investigator: Yuanyuan Li, master          Sub-Investigator: Xiuyun Gong, Bachelor          Sub-Investigator: Xiaoxiao Chen, Bachelor          Sub-Investigator: Juan Li, Bachelor Less <<
NCT03349827 Peritoneal Metastases From Gas... More >>tric Cancer Less << Not Applicable Recruiting November 30, 2020 China, Hubei ... More >> Wuhan University Recruiting Wuhan, Hubei, China Contact: Bin Xiong    +86 27 67813152    jyn1983@163.com Less <<
NCT02301091 Hepatocellular Carcinoma Phase 3 Recruiting October 2019 China, Guangdong ... More >> Minimally Invasive Interventional Division, Medical Imaging Center, Sun Yat-sen University Cancer Center, Recruiting Guangzhou, Guangdong, China, 500060 Contact: Ming Zhao, doctor    +86 020 87343272    zhaoming@sysucc.org.cn Less <<
NCT01869088 Hepatocellular Carcinoma Phase 3 Active, not recruiting January 2018 China, Guangdong ... More >> Cancer Center Sun Yat-sen University Guangzhou, Guangdong, China Less <<
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 <<
NCT02972320 Extensive Stage Small Cell Lun... More >>g Cancer Less << Phase 2 Unknown December 2018 China, Liaoning ... More >> The First Affiliated Hospital of China Medical University Recruiting Shenyang, Liaoning, China, 110001 Contact: mingfang zhao, professor    13644055129 Less <<
NCT03606239 Carcinoma, Non-Small-Cell Lung Not Applicable Not yet recruiting July 1, 2024 -
NCT00646100 Hepatocellular Carcinoma Phase 4 Completed - China, Guangdong ... More >> Cancer Canter Sun Yat-Sen University Guangzhou, Guangdong, China, 510060 Less <<
NCT03413436 Esophageal Cancer Phase 4 Not yet recruiting February 21, 2018 China, Henan ... More >> Henan Cancer Hospital/The affiliated Cancer Hospital of ZhengZhou university ZhengZhou, Henan, China, 450008 Less <<
NCT03221608 Colorectal Neoplasms Phase 3 Not yet recruiting August 1, 2024 -
NCT03371693 Ovarian Cancer ... More >> Ovary Neoplasm Ovarian Neoplasms Epithelial Ovarian Cancer Ovarian Cancer, Epithelial Hyperthermic Intraperitoneal Chemotherapy(HIPEC) Less << Phase 3 Active, not recruiting December 30, 2020 China, Hubei ... More >> Zhongnan Hospital of Wuhan University Wuhan, Hubei, China, 430072 Less <<
NCT01851746 - Unknown February 2015 China, Hubei ... More >> Zhongnan Hospital of Wuhan University Wuhan, Hubei, China, 430071 Less <<
NCT03117257 Locally Advanced Head and Neck... More >> Squamous Cell Carcinoma Less << Phase 2 Recruiting August 20, 2021 China, Guizhou ... More >> Cancer Hospital of Guizhou Medical University Recruiting Guiyang, Guizhou, China, 550000 Contact: Feng Jin, Bachelor    0851-86512802    jinf8865@yahoo.com.cn    Sub-Investigator: Weili Wu, master          Sub-Investigator: Jinhua Long, master          Sub-Investigator: Yuanyuan Li, master          Sub-Investigator: Xiuyun Gong, Bachelor          Sub-Investigator: Xiaoxiao Chen, Bachelor          Sub-Investigator: Mang Zhang, Bachelor Less <<
NCT01034683 Esophageal Carcinoma Phase 3 Unknown December 2010 China, Shandong ... More >> Taian Cancer Hospital Taian, Shandong, China, 271000 Less <<
NCT03188497 Acute Toxic Effects ... More >> Tumor Responses Less << Phase 1 Completed - China, Guangdong ... More >> the Fifth Hospital Affiliated to Sun Yat-Sen University Zhuhai, Guangdong, China, 519000 Less <<
NCT03613753 Small-cell Lung Cancer Phase 2 Recruiting June 1, 2021 China, Guizhou ... More >> The affiliated hospital of Guizhou medical university Recruiting Guiyang, Guizhou, China, 550004 Contact: Shengfa Su, PhD,MD    86-13608550432    sushengfa2005@163.com Less <<
NCT01483300 Breast Cancer Phase 2 Unknown November 2014 China, Heilongjiang ... More >> Cancer Hospital of Harbin Medical University Recruiting Harbin, Heilongjiang, China, 150081 Contact: Qingyuan Zhang, MD    86-451-86298276    zhma19650210@163.com    Contact: Xinmei Kang, MD    86-451-86298683    kxm791107@163.com    Principal Investigator: Qingyuan Zhang, MD          Sub-Investigator: Xinmei Kang, MD Less <<
NCT03613597 Small-cell Lung Cancer Phase 2 Recruiting January 1, 2022 China, Guizhou ... More >> The affiliated hospital of Guizhou medical university Recruiting Guiyang, Guizhou, China, 550004 Contact: Shengfa Su, PhD,MD    86-13608550432    sushengfa2005@163.com Less <<
NCT02099396 Lobaplatin and Gemcitabine in ... More >>Combination, Second-line Treatments on Advanced Osteosarcoma Less << Phase 2 Phase 3 Unknown - -
NCT03700359 Small Cell Lung Carcinoma Phase 2 Not yet recruiting November 29, 2021 -
NCT03210389 Recurrent Nasopharyngeal Carci... More >>noma Less << PHASE2 UNKNOWN 2025-12-21 Department of Radiation Oncolo... More >>gy, Sun Yat-Sen University Cancer Center, Guangzhou, Guangdong, 510000, China Less <<
NCT00493402 Hepatocellular Carcinoma Phase 3 Completed - China, Guangdong ... More >> Cancer Center Sun Yat-sen University Guangzhou, Guangdong, China, 510060 Less <<
NCT01350206 Hepatocellular Carcinoma With ... More >>PVTT Less << Phase 4 Unknown May 2013 China, Guangdong ... More >> Cancer Center Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Min-Shan Chen, M.D. Ph.D.    (8620) 8734 3117    Chminsh@mail.sysu.edu.cn    Principal Investigator: min-shan chen, M.D.,Ph.D. Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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

References

 

Historical Records

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