Chloroquine Phosphate

Catalog No.S4157

Chloroquine Phosphate Chemical Structure

Molecular Weight(MW): 515.86

Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

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3 Customer Reviews

  • NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.

    Leukemia, 2017, 31(5):1123-1135. Chloroquine Phosphate purchased from Selleck.

    Cells were pre-treated with rapamycin (Rapa, 1 μM) for 12 h, or KRIBB3 (KR, 0.5 μM) or chloroquine (CQ, 10 μM) for 2 h, followed by treatment with of palmitate (PA, 150 μM) for 24 h. Then the lipid in L02 cells was observed with Oil Red O (ORO) staining and ORO absorbance detection. Values are means ± SD (n = 3), *p b 0.05, versus matched controls.

    Cell Signal, 2016, 28(8):1086-98. . Chloroquine Phosphate purchased from Selleck.

  • Rapamycin aggravates the autophagic reaction induced by CVB3 infection. HeLa cells were treated with 10 nM rapamycin and chloroquine phosphate (CQ group) for 2 h. The cells were washed thrice and infected with CVB3. In the CVB3 group, HeLa cells were incubated with DMEM containing 10% FBS for 2 h and infected with CVB3. The sham group was incubated with DMEM containing 10% FBS. Two hours later, the medium was refreshed with DMEM containing 2% FBS. At 24 h.p.i., cells were collected for western blot analysis. The LC3-II/LC3-I ratio was increased in the CVB3 and rapamycin group (p<0.01), and p-mTOR was decreased in the CVB3 group (p<0.05) and rapamycin group (p<0.01) compared with the sham group. The changes in the LC3-II/LC3-I ratio and p-mTOR were more obvious in the Rap group compared with the CVB3 group (p<0.05). The LC3-II/LC3-I ratio and p62 was increased in the CQ group compared with the CVB3 group (p<0.05). *p<0.05, compared with the sham group; **p<0.01, compared with the sham group; #p<0.05, compared with the CVB3 group. CVB3, coxsackievirus B3; DMEM, Dulbecco's modified Eagle's medium; FBS, fetal bovine serum; h.p.i., hours post-inoculation; LC3, light chain 3; mTOR, mammalian target of rapamycin.

    Int J Mol Med, 2017, 40(1):182-192. Chloroquine Phosphate purchased from Selleck.

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Biological Activity

Description Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
Targets
ATM [1]
(Cell-free assay)
In vitro

Chloroquine is a chemotherapeutic agent for the clinical treatment of malaria. Chloroquine is able to bind to DNA, and inhibit DNA replication and RNA synthesis which in turn results in cell death. The effect of Chloroquine may also be related to the formation of a toxic heme-Chloroquine complex. Chloroquine inhibits trophozoite hemoglobin degradation through increasing vacuolar pH and inhibiting the activity of vacuolar phospholipase, vacuolar proteases, and heme polymerase[1]. Chloroquine possesses definite antirheumatic properties. Chloroquine has immuno-modulatory effects, suppressing the production/release of tumour necrosis factor and interleukin 6. Moreover, Chloroquine exerts direct antiviral effects, inhibiting pH-dependent steps of the replication of several viruses including members of the flaviviruses, retroviruses, and coronaviruses. Its best-studied effects are those against HIV replication[2]. Chloroquine can accumulate inside the macrophage phagolysosome by ion trapping where it exerts potent antifungal activity against Histoplasma capsulatum and Cryptococcus neoformans by distinct mechanisms. Chloroquine inhibits growth of H. capsulatum by pH-dependent iron deprivation, whereas it is directly toxic to C. neoformans[3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human K562 cells Ml3WR5l1d3SxeHnjxsBie3OjeR?= Mln3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:OzFwOEOgcm0> MV2xPFU{QDV4Nx?=
human KB cells M3m1SWN6fG:2b4jpZ:Kh[XO|YYm= NH7wVmdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{BjgSCvaXPyc5Bt[XSnIH3leIhw\CxiSVO1NF0xNjZizszN MVqxOFY1ODV{NB?=
human MDA-MB-468 cells NYK4N5lmS3m2b4TvfIlkyqCjc4PhfS=> NIPiUYg1QCCq NX3sNmRpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIEOuOUB2VSB2LTiyMYNpdG:{bz2xNGgueGinbn;4ZZpqdi1zMD35cEkuViyQLXTp[ZRpgWykdYThck0yNWGvaX7lJIh6\HKxY3jsc5Jq\GVuIFfJOVA:Oi56MTFOwG0> MWCxPVk1PTF7Nx?=
human MCF7 cells M4rkRWN6fG:2b4jpZ:Kh[XO|YYm= MVW0PEBp NXyxfIR4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJFAvPCC3TTCxMUgyNSh2LTi3MZBp\W67bD2xTE1qdWmmYYrvX|QtPS2pXYH1bY5wgGGuaX6tOk16dCmkZX76fYwqeGmyZYLp[IlvNTRveXypMVFJNWKnborvX4RecW2rZHH6c4wuOih|SDmtc45mNCCJSUWwQVUvPTFizszN MYexPVk1PTF7Nx?=
human MDA-MB-231 cells MlL6R5l1d3SxeHnjxsBie3OjeR?= MlWxOFghcA>? M1PIS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTDpckBxemW|ZX7j[UBw\iB|LkWgeW0hPC1qMj3jbIxwem9vMUDIMZBp\W6xeHH6bY4uOTBveXypMW4tVi2maXX0bJlt[nW2YX6tNU1idWmwZTDofYRzd2OqbH;ybYRmNCCJSUWwQVYvODhizszN NYPlNpc3OTl7NEWxPVc>
human HeLa cells MXXDfZRwfG:6aXRCpIF{e2G7 MknkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCkeTDNWHQh[XO|YYmsJGlEPTB;M{Cg{txO MUGyOFM2PDN{Mh?=
human HepG2 cells NV36[o1iS3m2b4TvfIlkyqCjc4PhfS=> M1HJXFQ5KGh? NVHX[nYxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0{Py54ODFOwG0> NWjFeoV5OjN6MUWxPFY>

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Protocol

Solubility (25°C)

In vitro Water 100 mg/mL (193.85 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 515.86
Formula

C18H26ClN3.2H3O4P

CAS No. 50-63-5
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03610399 Recruiting P Vivax|Malaria Vivax Centers for Disease Control and Prevention|Ministry of Health Brazil|Evandro Chagas National Institute of Infectious Disease April 9 2018 Not Applicable
NCT02932007 Recruiting Atrial Fibrillation University of South Florida March 28 2017 Phase 2
NCT03400865 Not yet recruiting Resistance Disease|Prolactinoma Zhebao Wu|Xinqiao Hospital of Chongqing|First Hospital of China Medical University|Beijing Tiantan Hospital|First Affiliated Hospital of Wenzhou Medical Univeristy|First Affiliated Hospital of Fujian Medical University|Peking Union Medical College Hospital|Huashan Hospital|Chinese PLA General Hospital|Ruijin Hospital October 25 2018 Not Applicable
NCT00871156 Completed Malaria GlaxoSmithKline|Medicines for Malaria Venture March 24 2009 Phase 1
NCT02432417 Not yet recruiting Glioblastoma|Astrocytoma Grade IV Maastricht Radiation Oncology January 2020 Phase 2
NCT03208907 Not yet recruiting Malaria Vivax|Therapeutics Fundação de Medicina Tropical Dr. Heitor Vieira Dourado|Ministry of Health Brazil|Oswaldo Cruz Foundation May 2018 Phase 3

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ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID