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Poziotinib

Catalog No. T2630   CAS 1092364-38-9
Synonyms: HM781-36B, NOV120101

Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Poziotinib Chemical Structure
Poziotinib, CAS 1092364-38-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 90.00
10 mg In stock $ 117.00
25 mg In stock $ 270.00
50 mg In stock $ 413.00
100 mg In stock $ 615.00
1 mL * 10 mM (in DMSO) In stock $ 90.00
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Purity: 99.78%
Purity: 97.81%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
Targets&IC50 HER1:3 nM, HER2:5 nM, HER4:23 nM
Kinase Assay 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)).
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)
Synonyms HM781-36B, NOV120101
Molecular Weight 491.34
Formula C23H21Cl2FN4O3
CAS No. 1092364-38-9

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 91 mg/mL (185.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Nam HJ, et al. Cancer Lett. 2011, 302(2), 155-165. 2. Cha MY, et al. Int J Cancer. 2012, 130(10), 2445-2454.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Angiogenesis related Compound Library Anti-Ovarian Cancer Compound Library JAK-STAT Compound Library Immuno-Oncology Compound Library Anti-Prostate Cancer Compound Library

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HER2/neu (654-662) GP2 acetate Tucatinib Tuxobertinib BMS 599626 2HCl (873837-23-1(HCl)) Terfenadine Rilzabrutinib NS1643 BMS-690514

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Keywords

Poziotinib 1092364-38-9 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors HER EGFR NOV-120101 HM781-36B NOV120101 NOV 120101 inhibitor inhibit

 

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