Molecular Weight(MW): 529.01
AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.
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|Description||AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.|
|Features||At least 10-fold more potent and selective in ALK inhibition relative to crizotinib.|
AP26113 is highly active against both sensitive and resistant H3122 cells, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis in a dose dependent manner. AP26113 decreases p-ALK in the H3122 and H3122 CR cells, with IC50 values of 7.4 versus 16.8 nM, respectively. AP26113 decreases cell number in Ba/F3 cells expressing either native or mutant EML4-ALK with IC50 of 10 nM and 24 nM, respectively.  AP26113 inhibits cell growth of SU-DHL-1, H3122 and Ba/F3-EML4-ALK v1 cell lines with GI50 of 9 nM, 4 nM and 13 nM, respectively. AP26113 inhibits phosphorylation of ALK with IC50 of 3.2 nM, 1.5 nM and 2.1 nM in Karpas-299, SU-DHL-1 and L-82 cell lines. AP26113 dose-dependently inhibits phosphorylation of ALK and ERK in Karpas-299 and H3122 cells.  AP26113 inhibits cell growth with IC50 of 11 nM and 16 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK G1269S mutants). AP26113 inhibits ALK phosphorylationh with IC50 of 74 nM and 335 nM in Ba/F3 line (native EML4-ALK) and Ba/F3 line (EML4-ALK E1210K mutants). AP26113 (10 mg/kg-75 mg/kg) is efficacious in PF-02341066-resistant EML4-ALK mutant mouse xenograft models. AP26113 induces regression of tumors expressing native EML4-ALK and the G1269S and L1196M mutants at 25 mg/kg, 50 mg/kg and 50 mg/kg, respectively.  AP26113 inhibits EGFR phosphorylation and viability with IC50 of 75 nM and 114 nM, respectively, in Ba/F3 cells expressing EGFR-DEL. AP26113 inhibits EGFR phosphorylation and viability with IC50s of 15 and 281 nM, respectively, in Ba/F3 cells expressing EGFR-DEL/T790M. AP26113 inhibits EGFR phosphorylation with an IC50 of 62 nM and cell growth with a GI50 of 165 nM in a NSCLC line expressing EGFR-DEL (HCC827). AP26113 inhibits EGFR phosphorylation with an IC50 of 59 nM and cell growth with a GI50 of 245 nM in HCC827 cells expressing EGFR-DEL/T790M. AP26113 potently inhibits SLC34A2-ROS-driven signaling and proliferation in a dose dependent manner in HCC78 NSCLC cells. 
|In vivo||AP26113 (< 50 mg/kg) dose-dependently inhibits p-ALK in tumor of Karpas-299 xenograft mice model. AP26113 (< 50 mg/kg) dose-dependently inhibits tumor growth in Karpas-299 xenograft mice model and H3122 xenograft mice model. AP26113 demonstrates favorable properties including moderate in vitro plasma protein binding (47%, 70% and 76% in human, rat, mouse), negligible inhibition of major CYP isoforms. AP26113 (10 mg/kg) is well-tolerated with Cmax of 2587 ng/mL and AUC of 41120 hr.ng/mL in rats.  AP26113 (25 mg/kg) leads to tumor regression in HCC827(EGFR-DEL) or HCC827(EGFR-DEL/T790M) xenograft mice model. |
|In vitro||Ethanol||106 mg/mL (200.37 mM)|
|DMSO||45 mg/mL (85.06 mM)|
|In vivo||NMP+polyethylene glycol 300 (10+90, v+v)||30 mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02094573||Active, not recruiting||Non-small Cell Lung Cancer|Lung Cancer|Advanced Malignancies|Carcinoma||Ariad Pharmaceuticals||March 2014||Phase 2|
|NCT01449461||Active, not recruiting||Advanced Malignancies|Carcinoma, Non-Small-Cell Lung|Anaplastic Large Cell Lymphoma|Diffuse Large Cell Lymphoma|Inflammatory Myofibroblastic Tumors||Ariad Pharmaceuticals||September 2011||Phase 1|Phase 2|
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