Poziotinib

SKU: orb1305243

Description

Poziotinib (NOV120101; HM781-36B) is an irreversible pan-HER inhibitor targeting EGFR (HER1), HER2, and HER4 with IC50 values of 3, 5, and 23 nM, respectively. It is a research tool used in vitro and in vivo to study oncogenic signaling and has been investigated in preclinical models of various cancers, including non-small cell lung cancer.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1092364-38-9
• MW: 491.34
• Purity: 99.78% (May vary between batches)
• Formula: C₂₃H₂₁Cl₂FN₄O₃
• SMILES: COc1cc2ncnc(Nc3ccc(Cl)c(Cl)c3F)c2cc1OC1CCN(CC1)C(=O)C=C
• Target: Apoptosis,HER,EGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:91 mg/mL (185.21 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.72 mM)

Bioactivity

• Target IC50:
  HER4:23 nM|HER2:5 nM|HER1:3 nM
• In Vivo:
  Poziotinib inhibits the phosphorylation of EGFR and key components of downstream signaling cascades, such as STAT3, AKT, and ERK, and exhibits specific inhibitory effects on the growth of gastric cancer cells with HER2 amplification. It can induce G1 cell cycle arrest and apoptosis in gastric cancer cells with activated HER2 amplification through the mitochondrial pathway. Furthermore, Poziotinib demonstrates synergistic effects with chemotherapeutic agents in both HER2-amplified and non-amplified gastric cancer cells.
• In Vitro:
  In nude mice bearing N87 human gastric carcinoma xenografts, Poziotinib (0.5 mg/kg, orally administered) significantly inhibits tumor growth. The combined use of Poziotinib and 5-FU further enhances the efficacy in suppressing tumor growth.
• Cell Research:
  Viable cell growth is determined by an MTT reduction assay. Briefly, all cell lines are seeded at a density of 3 × 103 per well in 96-well culture plates and then incubated at 37 °C for 24 h. The cells are then treated with 0.001, 0.01, 0.1, or 10 μM of HM781-36B. Three days later, 50 μg of MTT are added to each well and the samples are then incubated for 4 h to reduce the dye. Next, the samples are treated with DMSO, after which the absorbance of the converted dye in the living cells is measured at a wavelength of 540 nm. Six replicate wells are used for each analysis, and at least three independent experiments are conducted. Data points shown represent the mean while bars represent the SE.(Only for Reference)

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NOV 120101, NOV120101, NOV-120101, EGFR, HM781-36B, HER1, HER2, HER4, Apoptosis, Poziotinib

Compound Identifiers

PubChem CID

25127713