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Chloroquine phosphate

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Chemical Structure| 50-63-5 同义名 : 磷酸氯喹 ;Chloroquine (phosphate) (CRM);Chloroquine diphosphate;NSC 14050;DL-Chloroquine
CAS号 : 50-63-5
货号 : A233637
分子式 : C18H32ClN3O8P2
纯度 : 98%
分子量 : 515.862
MDL号 : MFCD00069852
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 30 mg/mL(58.16 mM)

动物实验配方:

PO 0.5% CMC-Na 45 mg/mL suspension

生物活性
描述 Chloroquine diphosphate (CQ), an autophagy inhibitor that may enhance the cytocidal effect of gefitinib against cSCC, was used in the present study. Suppression of autophagy by CQ, which was demonstrated by an alteration in microtubule associated protein 1 light chain 3-B in CQ pre-treated A431 cells, significantly enhanced cell apoptosis, which suggested that gefitinib-induced autophagy is cytoprotective. CQ was demonstrated to exhibit a synergistic apoptotic effect when used in combination with gefitinib during cSCC(cutaneous squamous cell carcinoma) therapy[2]. In vitro studies indicate that the antiviral effect of chloroquine diphosphate (CQ) requires a high concentration of the drug[3]. Chloroquine diphosphate (25mg/kg and 50mg/kg, respectively) significantly inhibited the growth of the implanted 4T1 tumor cells and induced apoptosis in the tumor microenvironment. Moreover, the metastasis of tumor cells to the lungs was inhibited significantly and the survival of the mice enhanced[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human HeLa cells Cytotoxic assay Cytotoxicity against human HeLa cells assessed as growth inhibition by MTT assay, IC50=30 μM 24354322
human HepG2 cells Cytotoxic assay 48 h Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=37.68 μM 23815186
human K562 cells Cytotoxic assay Cytotoxicity against human K562 cells by MTT assay, IC50=31.83 nM 18538567
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
NCT02563496 Malaria, Vivax Phase 2 Recruiting November 30, 2019 Colombia ... 展开 >> GSK Investigational Site Recruiting Monteria, Colombia Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    Thailand GSK Investigational Site Not yet recruiting Tak, Thailand, 63110 Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    Vietnam GSK Investigational Site Recruiting Hanoi, Vietnam, 100000 Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    GSK Investigational Site Recruiting Ho Chi Minh City, Vietnam, 700000 Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    GSK Investigational Site Recruiting Ho Chi Minh, Vietnam Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com 收起 <<
NCT01136850 Malaria in Pregnancy ... 展开 >> Sexually Transmitted Infections Anaemia 收起 << Phase 3 Completed - Papua New Guinea ... 展开 >> Papua New Guinea Institute of Medical Research Madang, Madang Province, Papua New Guinea 收起 <<
NCT00157859 Falciparum Malaria ... 展开 >> Vivax Malaria 收起 << Not Applicable Completed - Indonesia ... 展开 >> SP9 & SP12 Public Health- Malaria control clinics Timika, Papua, Indonesia 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.69mL

1.94mL

0.97mL

19.39mL

3.88mL

1.94mL

参考文献

[2]Wang J, Wang C, Hu X, Yu C, Zhou L, Ding Z, Zhou M. Gefitinib-mediated apoptosis is enhanced via inhibition of autophagy by chloroquine diphosphate in cutaneous squamous cell carcinoma cells. Oncol Lett. 2019 Jul;18(1):368-374

[3]Borba MGS, Val FFA, Sampaio VS, Alexandre MAA, Melo GC, Brito M, Mourão MPG, Brito-Sousa JD, Baía-da-Silva D, Guerra MVF, Hajjar LA, Pinto RC, Balieiro AAS, Pacheco AGF, Santos JDO Jr, Naveca FG, Xavier MS, Siqueira AM, Schwarzbold A, Croda J, Nogueira ML, Romero GAS, Bassat Q, Fontes CJ, Albuquerque BC, Daniel-Ribeiro CT, Monteiro WM, Lacerda MVG; CloroCovid-19 Team. Effect of High vs Low Doses of Chloroquine Diphosphate as Adjunctive Therapy for Patients Hospitalized With Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infection: A Randomized Clinical Trial. JAMA Netw Open. 2020 Apr 24;3(4):e208857

[4]Jiang PD, Zhao YL, Deng XQ, Mao YQ, Shi W, Tang QQ, Li ZG, Zheng YZ, Yang SY, Wei YQ. Antitumor and antimetastatic activities of chloroquine diphosphate in a murine model of breast cancer. Biomed Pharmacother. 2010 Nov;64(9):609-14