Cat. No.: HY-15730

Poziotinib

(Synonyms: HM781-36B; NOV120101)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR^wt, HER-2 and HER-4 with IC₅₀s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR^T790M and EGFR^L858R/T790M, with IC₅₀s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.

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Pureté: 99.96%
CAS No.: 1092364-38-9
Formule: C₂₃H₂₁Cl₂FN₄O₃
Masse moléculaire:491.34

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Poziotinib Chemical Structure

CAS No.: 1092364-38-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (8)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 3.2 nM (EGFR^wt), 5.3 nM (HER-2), 23.5 nM (HER-4) 4.2 nM (EGFR^T790M), 2.2 nM (EGFR^L858R/T790M)^[2]

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	CC₅₀	31 nM Compound: Poziotinib	Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
A-431	EC₅₀	1.445 μM Compound: Poziotinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	GI₅₀	0.654 μM Compound: Poziotinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	IC₅₀	0.9 nM Compound: 38; HM781e36B	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 72 hrs by MTS assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 72 hrs by MTS assay	[PMID: 28754471]
BaF3	EC₅₀	0.012 μM Compound: Poziotinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	GI₅₀	0.002 μM Compound: Poziotinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	IC₅₀	0.21 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring HER2-P780-Y781 ins GSP mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2-P780-Y781 ins GSP mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	0.43 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	0.58 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR A763-Y764 ins FQEA mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR A763-Y764 ins FQEA mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	0.62 nM Compound: Poziotinib	Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR D770-N771 ins NPG mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR D770-N771 ins NPG mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	1 nM Compound: Poziotinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR exon 20 insertion mutant incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR exon 20 insertion mutant incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37669428]
Calu-3	GI₅₀	10.12 nM Compound: cpd p	Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
HS27	GI₅₀	3830 nM Compound: 38; HM781e36B	Antiproliferative activity against human HS27 cells expressing wild type HER2 incubated for 72 hrs by MTS assay Antiproliferative activity against human HS27 cells expressing wild type HER2 incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H1975	IC₅₀	5.7 nM Compound: 38; HM781e36B	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H358	GI₅₀	8.67 nM Compound: cpd p	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
PC-9	GI₅₀	0.9 nM Compound: cpd p	Antiproliferative activity against human PC-9 cells expressing EGFR E746/A750 deletion mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells expressing EGFR E746/A750 deletion mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
SK-BR-3	IC₅₀	1 nM Compound: 38; HM781e36B	Antiproliferative activity against human SKBR3 cells expressing wild type HER2 incubated for 72 hrs by MTS assay Antiproliferative activity against human SKBR3 cells expressing wild type HER2 incubated for 72 hrs by MTS assay	[PMID: 28754471]

In Vitro

The IC₅₀ levels of Poziotinib (HM781-36B) for N87 and SNU216 were 0.001 and 0.004 μM, respectively, which was 10-1000 fold lower than the IC₅₀ levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to ZD1839 or GW572016^[1].
Poziotinib (HM781-36B) also shows excellent selectivity with other kinases with greater than 100- to 1,000- fold IC₅₀ values compared with EGFR family members. Poziotinib (HM781-36B) possesses a functional α,β‐unsaturated carbonyl group as Michael acceptor moiety at the C6 position that allows covalent modifications of the EGFR kinase domain active site^[2].
The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC₅₀=0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1092364-38-9
Appearance Solid
Masse moléculaire 491.34
Formule C₂₃H₂₁Cl₂FN₄O₃
Color White to off-white
SMILES

C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O
Synonyms

HM781-36B; NOV120101
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (8)

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Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
J Med Chem

Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. [Abstract]

2022 May 12;65(9):6643-6655. PMID: 35486541
Mol Cancer Res

TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. [Abstract]

2019 Nov;17(11):2233-2243. PMID: 31467113
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Cancers (Basel)

Poziotinib Inhibits the Efflux Activity of the ABCB1 and ABCG2 Transporters and the Expression of the ABCG2 Transporter Protein in Multidrug Resistant Colon Cancer Cells. [Abstract]

2020 Nov 4;12(11):3249. PMID: 33158067

Poziotinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2020 Nov 4;12(11):3249. [Abstract]

Poziotinib, at 0.1, 0.3 and 0.6 μM, produces a significant decrease in the expression level of the ABCG2 transporter protein in S1-M1-80 cells after 72 h of incubation, compared to cells incubated with vehicle (0 μM). ABCG2 protein expression is significantly decreased in S1-M1-80 cells following incubation with 0.6 µM of Poziotinib for 48 or 72 h.
Biochem Biophys Res Commun

Poziotinib suppresses ovarian cancer stem cell growth via inhibition of HER4-mediated STAT5 pathway. [Abstract]

2020 May 21;526(1):158-164. PMID: 32201081
bioRxiv

2026 Jun 19.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (101.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0353 mL

10.1763 mL

20.3525 mL

5 mM

0.4071 mL

2.0353 mL

4.0705 mL

10 mM

0.2035 mL

1.0176 mL

2.0353 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.87 mg/mL (5.84 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.87 mg/mL (5.84 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.25 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.25 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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Références

[1]. Nam HJ, et al. Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett. 2011 Mar 28;302(2):155-65. [Content Brief]

[2]. Cha MY, et al. Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in CP-358774-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0353 mL	10.1763 mL	20.3525 mL	50.8813 mL
	5 mM	0.4071 mL	2.0353 mL	4.0705 mL	10.1763 mL
	10 mM	0.2035 mL	1.0176 mL	2.0353 mL	5.0881 mL
	15 mM	0.1357 mL	0.6784 mL	1.3568 mL	3.3921 mL
	20 mM	0.1018 mL	0.5088 mL	1.0176 mL	2.5441 mL
	25 mM	0.0814 mL	0.4071 mL	0.8141 mL	2.0353 mL
	30 mM	0.0678 mL	0.3392 mL	0.6784 mL	1.6960 mL
	40 mM	0.0509 mL	0.2544 mL	0.5088 mL	1.2720 mL
	50 mM	0.0407 mL	0.2035 mL	0.4071 mL	1.0176 mL
	60 mM	0.0339 mL	0.1696 mL	0.3392 mL	0.8480 mL
	80 mM	0.0254 mL	0.1272 mL	0.2544 mL	0.6360 mL
	100 mM	0.0204 mL	0.1018 mL	0.2035 mL	0.5088 mL

Keywords

Poziotinib

8 Cited Publications

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Poziotinib

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Publications Citing Use of MedChemExpress (MCE) Poziotinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (8)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Poziotinib Related Classifications

HY-15730 Related Classifications