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Angiogenesis HER Poziotinib

Poziotinib

Catalog No. T2630   CAS 1092364-38-9
Synonyms: NOV120101, HM781-36B
Purity 100.00% Datasheet

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

Poziotinib, CAS 1092364-38-9
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
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Purity 100.00%
Biological Description
Chemical Properties
Storage & Solubility Information
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)
Animal Research
Animal Model: BALB/c athymic nude mice bearing N87 xenografts
Synonyms NOV120101, HM781-36B
Purity 99.78%
Appearance solid
Molecular Weight 491.34
Formula C23H21Cl2FN4O3
CAS No. 1092364-38-9

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

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 )

Citations

References 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. 3. Kang MH, et al. Antitumor Activity of HM781-36B, alone or in Combination with Chemotherapeutic Agents, in Colorectal Cancer Cells. Cancer Res Treat. 2015 Mar 5.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Apoptosis Compound Library Tyrosine kinase inhibitor library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Fluorochemical Library Angiogenesis related Compound Library JAK STAT Compound Library

Related Products

Related compounds with same targets
Afatinib Dimaleate AG-1478 Afatinib Neratinib Neratinib Irbinitinib BMS 599626 Poziotinib

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