-20℃ 3 years powder
-80℃ 2 years in solvent
Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | 56.00 | |
5 mg | In stock | 100.00 | |
10 mg | In stock | 130.00 | |
25 mg | In stock | 300.00 | |
50 mg | In stock | 460.00 | |
100 mg | In stock | 700.00 | |
1 mL * 10 mM (in DMSO) | In stock | 100.00 |
Description | Poziotinib(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM). |
Targets&IC50 | HER1 :ic50 3.2nM, HER2 :ic50 5.3nM, HER4 :ic50 23.5nM, |
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)
Cell lines: Gastric cancer cell lines (SNU-1, 5, 16, 216, 484, 601, 620, 638, 668, 719, N87 and AGS)
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Animal Research |
Animal Model: BALB/c athymic nude mice bearing N87 xenografts
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Synonyms | NOV120101 , HM781-36B |
Purity | 97.81% |
Molecular Weight | 491.34 |
Formula | C23H21Cl2FN4O3 |
CAS No. | 1092364-38-9 |
-20℃ 3 years powder
-80℃ 2 years in solvent
DMSO: 91 mg/mL (185.2 mM)
Ethanol: <1 mg/mL
Water: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
Safe and effective drug dosing is necessary, regardless of its purpose of administration. Learn More
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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.