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Chloroquine diphosphate

Catalog No.
A8628
Antimalarial drug, TLR7 and TLR9 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL H2O)
$61.00
In stock
100mg
$55.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

Chloroquine diphosphate (CAS 50-63-5) is an antimalarial agent and inhibitor of TLR7 and TLR9, commonly used in biomedical research to modulate autophagic processes. On the cellular level, chloroquine diphosphate promotes autophagy through cell cycle arrest at the G1 phase, involving increased expression of p27 and p53 and decreased levels of CDK2 and cyclin D1. Additionally, chloroquine diphosphate enhances sensitivity of cancer cells toward chemotherapy and radiotherapy treatments by elevating autophagy and apoptotic responses. In vitro studies demonstrated dose-dependent activity, with reported IC50 values typically ranging from approximately 15 to 40 µM depending on cell types. This compound is widely utilized as an autophagy modulator and therapeutic adjuvant in tumor cell models.

References:
[1].  Gewirtz, D.A., An autophagic switch in the response of tumor cells to radiation and chemotherapy. Biochem Pharmacol, 2014. 90(3): p. 208-11.
[2].  Jiang, P.D., et al., Antitumor and antimetastatic activities of chloroquine diphosphate in a murine model of breast cancer. Biomed Pharmacother, 2010. 64(9): p. 609-14.
[3].  Choi, J.H., et al., Chloroquine enhances the chemotherapeutic activity of 5-fluorouracil in a colon cancer cell line via cell cycle alteration. APMIS, 2012. 120(7): p. 597-604.
[4].  Zhou, Z.R., et al., Poly(ADP-ribose) polymerase-1 regulates the mechanism of irradiation-induced CNE-2 human nasopharyngeal carcinoma cell autophagy and inhibition of autophagy contributes to the radiation sensitization of CNE-2 cells. Oncol Rep, 2013. 29(6): p. 2498-506.
[5].  Sasaki, K., et al., Resistance of colon cancer to 5-fluorouracil may be overcome by combination with chloroquine, an in vivo study. Anticancer Drugs, 2012. 23(7): p. 675-82.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at RT
M.Wt515.86
Cas No.50-63-5
FormulaC18H26ClN3·2H3PO4
Solubilityinsoluble in DMSO; insoluble in EtOH; ≥106.06 mg/mL in H2O
Chemical Name4-N-(7-chloroquinolin-4-yl)-1-N,1-N-diethylpentane-1,4-diamine;phosphoric acid
SDFDownload SDF
Canonical SMILESCCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl.OP(=O)(O)O.OP(=O)(O)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Mouse breast cancer 4T1 cells

Preparation method

The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20°C for several months.

Reacting condition

3.125, 6.25, 12.5, 25, 50 and 100 μM; 24, 48 and 72 hrs

Applications

According to the results of the MTT assay, Chloroquine Diphosphate dose- and time-dependently inhibited proliferation of 4T1 cells.

Animal experiment [1]:

Animal models

4T1 tumor-bearing BALB/c mice

Dosage form

25 and 50 mg/kg; i.p.; q.d., for 28 days

Applications

Chloroquine Diphosphate treatment at the doses of 25 and 50 mg/kg significantly reduced the rates of primary tumor growth. In addition, 30% and 60% of mice in the 25 and 50 mg/kg Chloroquine Diphosphate-treated groups still survived on 61st day.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Jiang, P.D., et al., Antitumor and antimetastatic activities of chloroquine diphosphate in a murine model of breast cancer. Biomed Pharmacother, 2010. 64(9): p. 609-14.

Quality Control

Chemical structure

Chloroquine diphosphate

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Chloroquine diphosphate

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Chloroquine diphosphate

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Chloroquine diphosphate

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Chloroquine diphosphate

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Chloroquine diphosphate

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Chloroquine diphosphate