Catalog No.S7358 Synonyms: NOV120101
Molecular Weight(MW): 491.34
Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.
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|Description||Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.|
Poziotinib specifically inhibits the cell growth in HER2 amplified gastric cancer cells, and inhibits the phosphorylation of EGFR and key components of downstream signaling cascades such as STAT3, AKT and ERK. Poziotinib also induces apoptosis and G1 cell cycle arrest by activating the mitochondrial pathway in HER2 amplified gastric cancer cells. Furthermore, Poziotinib also exerts synergistic effects with chemotherapeutic agents in both HER2 amplified and HER2 non-amplified gastric cancer cells. 
|In vivo||In nude mice bearing N87 human gastric cancer xenografts, Poziotinib (0.5 mg/kg p.o.) alone significantly inhibits the growth of tumors, and coadministraion of Poziotinib and 5-FU causes more effective tumor inhibition.  In addition, HM781-36B shows excellent antitumor activity in a variety of EGFR- and HER-2-dependent tumor xenograft models, including erlotinib-sensitive HCC827 NSCLC cells, erlotinib-resistant NCI-H1975 NSCLC cells, HER-2 overexpressing Calu-3 NSCLC cells, NCI-N87 gastric cancer cells, SK-Ov3 ovarian cancer cells and EGFR-overexpressing A431 epidermoid carcinoma cancer cells. |
Enzyme activity assay:To determine the IC50 values of HM781-36B for kinase inhibition, enzymes of EGFR, HER2, and HER4 are expressed as recombinant proteins in Sf9 insect cells. Enzyme selectivity screening is then performed using a tyrosine kinase assay kit. Briefly, the reactions are performed in 96 well polystyrene round-bottomed plates containing kinase buffer composed of 100 mM HEPES (pH 7.4), 25 mM MgCl2, 10 mM MnCl2 and 250 μM Na3VO4. The reactions are initiated by the addition of 100 ng/assay enzyme, 100 μM ATP, and 10 ng/mL poly(Glu, Tyr). After 1 h of incubation at room temperature, the reactions are terminated by adding 6 mM EDTA solution and then anti-phosphotyrosine antibody, PTK Green Tracer, and FP dilution buffer mixtures. The fluorescence polarization values are then measured after 30 min at room temperature using a Victor3 microplate reader. Finally, the IC50 values were calculated using the following equation: Y = bottom + (top–bottom)/(1 + 10(X-logIC50)).
|In vitro||DMSO||98 mg/mL (199.45 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02659514||Recruiting||Breast Cancer||Spectrum Pharmaceuticals, Inc||February 2016||Phase 2|
|NCT02979821||Recruiting||HER2 Gene Mutation|Adenocarcinoma Lung Stage IV||Korean Association for the Study of Targeted Therapy|Konkuk University Medical Center|Kyungpook National University|Kosin University Gospel Hospital|Chonnam National University Hospital|Chungnam National University Hospital||October 2015||Phase 2|
|NCT02544997||Recruiting||Metastatic Breast Cancer||Samsung Medical Center||September 2015||Phase 2|
|NCT02418689||Active, not recruiting||Metastatic Breast Cancer||National OncoVenture|Hanmi Pharmaceutical Company Limited||March 2015||Phase 2|
|NCT02216916||Unknown status||HNSCC||Yonsei University||August 2014||Phase 2|
|NCT01819428||Terminated||Adenocarcinoma of Lung Stage IIIB|Adenocarcinoma of Lung Stage IV||National OncoVenture|Hanmi Pharmaceutical Company Limited||March 2013||Phase 2|
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