QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC 50 of 35 nM
In Vitro
QC6352 is a potent KDM4C inhibitor with an IC 50 of 35±8 nM. In a concentration-dependent manner QC6352 dramatically reduces the anchorage-independent sphere-forming capacity of BCSC1 and BCSC2. QC6352 blocks proliferation and self-renewal of BCSCs. As shown by western blot analysis the protein levels of (Epidermal growth factor receptor) EGFR are reduced in both BCSC1 and BCSC2 upon treatment with QC6352. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
QC6352 strongly affects tumor growth and final tumor weight of both BCSC1 and BCSC2 xenografts. Treatment with QC6352 is well tolerated and does not affect body weight of the mice. Results demonstrate that treatment with the KDM4 inhibitor QC6352 blocks BCSC xenograft tumor growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
Cells are detached by Accutase and counted. 1×10 3 single BCSC1 and BCSC2 cells are seeded as triplicates in 50% Matrigel into individual wells of 24-well ultra-low attachment plates in serum-free MSC medium. After 7 days, spheres over 50 μm diameter are counted for QC6352- and QC6688-treated and control cells and spheres over 20 μm diameter are counted for paclitaxel-treated and control cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Mice: When tumors reach a palpable size of 3 mm 3 , mice are treated with vehicle (control) or QC6352. The inhibitor is administered daily to mice via oral gavage at 10 mg/kg. Control animals receive vehicle only. Animals are monitored twice weekly for weight and tumor growth . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
