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Cat. No. M1720
AP26113 Structure


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Biological Activity

AP26113 is a highly potent ALK inhibitor with IC50 of 0.62 nM. As an ALK inhibitor, AP26113 overcomes mutation-based resistance in NSCLC models. Multiple mutations in ALK were identified that conferred resistance to crizotinib, but not AP26113, including the L1196M "gatekeeper" mutation which has now been observed clinically in patients who initially responded to crizotinib and then relapsed. AP26113 also inhibits activated EGFR in preclinical models, including the T790M "gatekeeper" mutant that confers resistance to current EGFR inhibitors. Constitutive EGFR activity due to activating mutation is a key feature of certain non-small cell lung cancers, and the T790M mutation causes resistance to inhibitor therapy in approximately 50 percent of these cases. In preclinical studies, AP26113 was shown to be specific for mutated EGFR and avoids inhibition of native (endogenous or unmutated) EGFR; such inhibition is thought to be associated with the toxicity of other EGFR inhibitors.

Customer Product Validations & Biological Datas
Source Mol Cancer Res (2015). Figure 1. AP26113
Method Western blot
Cell Lines KARPAS-299, SUP-M2 cell lines
Concentrations 0, 100, 300, and 1000 nmol/L
Incubation Time 20 nmol/L
Results In all AP26113-resistant KARPAS-derived cell lines, STAT-3 P-Tyr705 was present at higher drug doses than the one observed for parental cells and correlated with the persistent NPM-ALK phosphorylation
Cell Experiment
Cell lines H3122, H3122 CR, A549, H1299, SKBR3, H522, H460, and BT474 cells
Preparation method Survival assays
For 72-h drug treatments, 3000 cells were plated in replicates of six into 96-well plates. Following drug treatments, cells were incubated with CellTiter-Glo assay reagent (Promega) for 10 min and luminescence was measured using a Centro LB 960 microplate luminometer (Berthold Technologies).
Concentrations 0~1µ M
Incubation time 72 h
Animal Experiment
Animal models H3122 CR xenografts in athymic nude mice
Formulation saline
Dosages 50 mg/kg/day for 17 days
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 529.01
Formula C26H34ClN6O2P
CAS Number 1197958-53-4
Purity 99.29%
Solubility DMSO
Storage at -20°C

Abstract 1794: AP26113 is a dual ALK/EGFR inhibitor: Characterization against EGFR T790M in cell and mouse models of NSCLC.
Victor et al. Cancer Research. 2012 April 15;Volume 72, Issue 8, Supplement 1.

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Keywords: AP26113, Brigatinib supplier, ALK, inhibitors

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