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  3. Quinacrine dihydrochloride

Quinacrine dihydrochloride (Synonyms: Mepacrine dihydrochloride; SN-390 dihydrochloride)

Cat. No.: HY-13735A Purity: 99.01%
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Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.

For research use only. We do not sell to patients.

Quinacrine dihydrochloride Chemical Structure

Quinacrine dihydrochloride Chemical Structure

CAS No. : 69-05-6

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Description

Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis[1].

In Vitro

Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells[1].
Quinacrine (7.5 and 15 μM; 24 hours) induces apoptosis in SGC-7901 cells, which is associated with mitochondria-dependent signal pathway and involves p53 upregulation and caspase-3 activation pathway[1].
Quinacrine (15 μM; 24 hours) treatment significantly increased the levels of proapoptotic proteins, including cytochrome c, Bax, and p53, and decreased the levels of antiapoptotic protein Bcl-2, thus shifting the ratio of Bax/Bcl-2 in favor of apoptosis [1].

Cell Viability Assay[1]

Cell Line: SGC-7901 cells
Concentration: 0, 5, 10, 15, and 20 μM
Incubation Time: 24 hours
Result: Cell viability was inhibited in a dose-dependent manner, and the mean IC50 value is 16.18 μM.

Apoptosis Analysis[1]

Cell Line: SGC-7901 cells
Concentration: 7.5 and 15 μM
Incubation Time: 24 hours
Result: The percentage of apoptotic cells, including the early phase and late phase apoptosis, increased to 26.30%, compared with control group of 3.37%.

Western Blot Analysis[1]

Cell Line: SGC-7901 cells
Concentration: 15 μM
Incubation Time: 24 hours
Result: The relative quantity of cytochrome c protein was upregulated, increased from 0.10 to 0.24.
The relative quantity of p53 protein was dramatically increased, from 0.06 to 0.19.
The Bax/Bcl-2 ratio was dramatically elevated from 1.21 to 2.59.
In Vivo

Quinacrine (100 mg/kg three times per week for two consecutive weeks) significantly suppresses circulating blast cells at days 30/31 and increases the median survival time (MST). Quinacrine does not decrease the body weight of treated animals at the tested dose[2].

Animal Model: Female SCID mice with acute myeloid leukemia (AML)-PS model[2]
Dosage: 100 mg/kg
Administration: Administered by oral gavage (po); three times a week for two consecutive weeks
Result: In the first AML mouse in vivo study, evaluation of circulating leukemic cells detected in blood samples (in percent of white blood cells (WBC)) at day 30/31 showed 72% human tumor cells in the control mice, whereas in mice treated with Quinacrine, this was only 2.2%.
The MST of control mice was 34 days whereas it was 46 days in Quinacrine-treated mice.
Clinical Trial
Molecular Weight

472.88

Formula

C₂₃H₃₂Cl₃N₃O

CAS No.

69-05-6

SMILES

CC(NC1=C(C=C(OC)C=C2)C2=NC3=CC(Cl)=CC=C31)CCCN(CC)CC.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (93.05 mM)

H2O : 33.33 mg/mL (70.48 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1147 mL 10.5735 mL 21.1470 mL
5 mM 0.4229 mL 2.1147 mL 4.2294 mL
10 mM 0.2115 mL 1.0574 mL 2.1147 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.01%

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Keywords:

QuinacrineMepacrineSN-390SN390SN 390ParasiteApoptosisAutophagyMitophagyMitochondrial AutophagyapoptosisBaxBcl-2p53SGC-7901AcutemyeloidleukemiaInhibitorinhibitorinhibit

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Quinacrine dihydrochloride
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