Lerociclib dihydrochloride

SupT1, Daudi, MCF7, ZR-75-1, A2058, WM2664, and H69 cells are seeded at 1000 cells per well; MV-4-11 and BV173 cells are plated at 4000 cells per well; Tom-1 cells are plated at 8,000 cells per well; NALM-1 cells are plated at 20,000 cells per well in Costar 3903 96 well plates. After 24 hours, plates are dosed with Lerociclib at a nine-point dose concentration from 10 μM to 1 nM. Cell viability is determined after four or six days. Plates are processed on BioTek Synergy2 multi-mode plate reader and data analyzed using GraphPad Prism 5 statistical software^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[1]
Female MMTV-NEU mice are used to test the efficacy of Lerociclib (100 mpk, medicated diet). At time of treatment, body composition is assessed and weight measurements (in grams) are recorded and used as a measure of gross toxicity. Female nude mice are implanted with NSCLC PDX CTG0159 tumor. Mice are then randomized into treatment groups and dosing initiated once tumors reached a volume that fell within the range of 150-300 mm³. 100 mg/kg Lerociclib or vehicle is orally administered for 28 consecutive days. Female NCI Ath/nu mice are implanted with H1975 NSC lung adenocarcinoma model. Once tumors reach an average size of 100-150 mm³, mice are randomized into treatment cohorts. Mice are orally administered daily Afatinib (20 mg/kg), Erlotinib (70 mg/kg), or Lerociclib (50 or 100 mg/kg), as single agents or in combination (Lerociclib+Erlotinib or Lerociclib+Afatinib) for the duration of the study. All tumors are measured twice weekly until mice reach tumor burden of 1500 mm³.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.