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)。
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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 |
+++
ULK2, IC50: 711 nM ULK1, IC50: 108 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 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。 |
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 | ||
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 << |
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 |
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 |