PAA5 is a methide carbon-centered polynuclear Au(I) cluster. PAA5 can release Au(I) causing Pro-oxidant response and accelerated ferroptosis. PAA5 increases the expression of pH2AX in a time-dependent manner. PAA5 has anticancer activity.
In Vitro Activity
PAA5 (0-4 µM; 24 h) induces ferroptosis and increase of the ferroptosis marker gene prostaglandin-endoperoxide synthase 2 (PTGS2). PAA5 decreases cell viability in EJ cells with IC50 values of 1.0 µM and 2.7 µM for EJ and HUVEC cells, respectively.
PAA5 (1.5 μM; 4 h; EJ and HUVEC cells) releases active Au(I) metabolites within cells and increases GSH and ROS level.
PAA5 (4 µM; 1, 3 and 6 h, EJ cells) causes significant DNA damage as indicated by the increase of histone H2AX phosphorylation (pH2AX).
In Vivo Activity
PAA5 (1.5 µM, 100 µL; intravesical delivered into the bladder; 5 times every other day for 8 days) shows anti-tumor activity in mouse.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
4-6 weeks, 18 g, female BALB/c nude mice
Dosage:
1.5 µM, 100 µL
Administration:
Intravesical delivered into the bladder; 5 times every other day for 8 days
Result:
Exhibited a good antitumor effect with the small average tumor volume of 564 ± 180 mm3 after 22 days and no significant body weight loss.
Storage & Handling
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping
Room temperature in continental US; may vary elsewhere.
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