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/ Chloroquine phosphate

磷酸氯喹 /Chloroquine phosphate {[allProObj[0].p_purity_real_show]}

货号：A233637 同义名： 磷酸氯喹 / Chloroquine (phosphate) (CRM);Chloroquine diphosphate

Chloroquine phosphate是一种广泛用于治疗疟疾和类风湿性关节炎的抗疟药和抗炎剂。它是一种自噬和 Toll 样受体 (TLR) 抑制剂，在体外控制 SARS-CoV-2 (COVID-19) 感染的效果非常显著 (EC50 = 1.13 μM)。

Chloroquine phosphate 化学结构 CAS号：50-63-5
Chloroquine phosphate 化学结构
CAS号：50-63-5
Chloroquine phosphate 3D分子结构
CAS号：50-63-5
Chloroquine phosphate 化学结构 CAS号：50-63-5
Chloroquine phosphate 3D分子结构 CAS号：50-63-5
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Chloroquine phosphate 纯度/质量文件 产品仅供科研

货号：A233637 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ATM ↓ ATR ↓ 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

 		PI3K,DNA-PK,MLCK 99%+
CP-466722 +

ATM, IC50: 410 nM

 		99%+
Torin 2 ++

ATM, EC50: 28 nM

 		++

ATR, EC50: 35 nM

 		mTOR,DNA-PK 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

 		96%
ETP-46464 +

ATM, IC50: 545 nM

 		+++

ATR, IC50: 14 nM

 		mTOR,DNA-PK 98%
CGK733 ++

ATM, IC50: 200 nM

 		++

ATR, IC50: 200 nM

 		99%+
AZD0156 ✔ 99%+
Dactolisib +++

ATR, IC50: 21 nM

 		98+%
Ceralasertib ++++

ATR, IC50: 1 nM

 		99%+
Berzosertib +++

ATR, IC50: 19 nM

 		99%+
VE-821 +++

ATR, Ki: 13 nM

 		99%+
AZ20 ++++

ATR, IC50: 5 nM

 		mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

 		P-gp 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。
产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

 		97%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 hydrochloride ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		97%
Lys05 ✔ 99%+
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。

Chloroquine phosphate 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].

Chloroquine phosphate 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
human KB cells Cytotoxic assay Cytotoxicity against human KB cells by microplate method, IC50=0.6 μM 14640524

Chloroquine phosphate 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 <<

Chloroquine phosphate 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

Chloroquine phosphate 实验方案

计算器
存储液制备 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

Chloroquine phosphate 技术信息

CAS号50-63-5
分子式C18H32ClN3O8P2
分子量 515.862
别名 磷酸氯喹 ;Chloroquine (phosphate) (CRM);Chloroquine diphosphate;NSC 14050;DL-Chloroquine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
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

Tags: Chloroquine phosphate | Chloroquine (phosphate) (CRM);Chloroquine diphosphate;NSC 14050;DL-Chloroquine | 磷酸氯喹 | Pain and Pruritus Model | Drug Standard | Insect Repellent | ATM/ATR | Autophagy | AmBeed-信号通路专用抑制剂 | Chloroquine phosphate 纯度/质量文件 | Chloroquine phosphate 亚型比较 | Chloroquine phosphate 生物活性 | Chloroquine phosphate 细胞研究 | Chloroquine phosphate 临床数据 | Chloroquine phosphate 参考文献 | Chloroquine phosphate 实验方案 | Chloroquine phosphate 技术信息

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