Poziotinib (HM781-36B) - 97%, high purity , Epidermal growth factor receptor inhibitor, CAS No.1092364-38-9, Epidermal growth factor receptor inhibitor

Item Number

P413748

• Synonyms: 1-[4-[4-(3,4-dichloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]prop-2-en-1-one | CCG-264748 | DB12114 | EX-A528 | 1-(4-{[4-(3,4-dichloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxy}piperidin-1-yl)prop-2-en-1-one | DTXSID80148853 | CS-
• Specifications & Purity: Moligand™, ≥97%
• Biochemical and Physiological Mechanisms: Poziotinib (HM781-36B, NOV120101) 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. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Epidermal growth factor receptor inhibitor

Product Description

Information

Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HERinhibitor withIC50of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also inducesapoptosisand G1 cell cycle arrest. Phase 2.

Targets

HER1 (Cell-free assay); HER2 (Cell-free assay); HER4 (Cell-free assay) 3.2 nM; 5.3 nM; 23.5 nM

In vitro

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.

Cell Research(from reference)

Cell lines：Gastric cancer cell lines (SNU-1, 5, 16, 216, 484, 601, 620, 638, 668, 719, N87 and AGS) 

Concentrations：~10 μM 

Incubation Time：72 hours