Quinacrine dihydrochloride

Research use only, not for human use.

An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years.

An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.(In Vitro):Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells.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.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 .(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.

Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells.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.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 . Cell Viability Assay 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 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 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.

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. Animal Model:Female SCID mice with acute myeloid leukemia (AML)-PS model 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.

——

Cell Cycle/DNA Damage

DNA Alkylator

DNA| Histamine N-methyltransferase| PLA2| PLCLP

Cancer

Prostate Cancer

69-05-6

472.88

C23H30CLN3O·2HCl

>98% (HPLC)

Ethanol: 28 mg/mL (59.21 mM); Water: 53 mg/mL (112.07 mM); DMSO: 14 mg/mL (29.6 mM)

[H+].[H+].[Cl-].[Cl-].CCN(CC)CCCC(C)NC1=C2C=C(OC)C=CC2=NC2=C1C=CC(Cl)=C2

——

(-20℃)

With Ice Pack

≥ 2 years