AZD2014 is a novel dual mTORC1 and mTORC2 inhibitor with potential antineoplastic activity. AZD2014 inhibits biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy. AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen.
|Source||Cell Physiol Biochem (2018). Figure 4. AZD2014|
|Method||Flow cytometric analysis|
|Cell Lines||NSCLC cell|
|Incubation Time||24 h|
|Results||When mTOR was inhibited in anti-miR-99a-A549 cells by AZD2014, the cells became more sensitive to radiation than control cells and the levels of anti-apoptosis markers were reduced|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 18 mg/mL|
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