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Poziotinib

Catalog No. T2630 CAS 1092364-38-9

Synonyms: NOV120101, HM781-36B

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
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 97.81%

HNMR HPLC COA Datasheet MSDS

Purity 100.00%

HNMR HPLC COA Datasheet MSDS

Purity 99.78%

HNMR HPLC COA Datasheet MSDS

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	97.81%
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

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Related compounds with same targets

CP724714 Epertinib BGB-102 Epertinib hydrochloride TAS0728 Mollugin RG 14620 NS1643

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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.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.