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Pertuzumab (anti-HER2)

Synonyms: 2C4

Catalog No.A2008 Purity:99.17%

Pertuzumab (anti-HER2), a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.

Pertuzumab (anti-HER2) Chemical Structure

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Selleck's Pertuzumab (anti-HER2) has been cited by 9 publications

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Purity & Quality Control

Batch: Purity: 99.17% Protein concentration: 5.02mg/ml Endotoxin Level: ≤1 EU/mg

99.17

Choose Selective HER2 Inhibitors

Name	Citation	HER2	Others
Canertinib (CI-1033)	48	+++	EGFR
CP-724714	108	+++
Sapitinib (AZD8931)	46	++++	ErbB3,EGFR
CUDC-101	22	++	EGFR,HDAC,HDAC1
Mubritinib (TAK 165)	38	++++
AEE788 (NVP-AEE788)	13	++++	EGFR,c-Abl,FLT1
AC480 (BMS-599626)	10	++	HER1,HER4
TAK-285	4	++	EGFR/HER1,HER4,MEK1
Tyrphostin AG 879	3	+	Trk
Tuxobertinib (BDTX-189)	2	++++	EGFR,RIPK2,BLK
Epertinib hydrochloride	0	++++	EGFR,HER4
TAS0728	1	+++
Tyrphostin AG-528	0	+	EGFR
SU5204	1	+	VEGFR-2
Pyrotinib dimaleate	4	+	EGFR
Poziotinib	34	++++	HER1,HER4
HER2-Inhibitor-1	✔
Zongertinib	✔	EGFR-Ex20ins
Nordihydroguaiaretic acid (NDGA)	✔	p300,IGF-1R,lipoxygenase
EGCG ((-)-Epigallocatechin Gallate)	✔	FASN,EGFR,DNMT

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1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Biological Activity

Description

Features

Human IgG1

Targets

HER2 ^[1]

In Vitro
In vitro	The combination of pertuzumab with etoposide represents a promising strategy aimed at inhibition of viability and proliferation of gastric cancer cells. The mechanism of action includes induction of both extrinsic and intrinsic apoptotic pathway, where increased activity of caspase-8 and caspase-9 are demonstrated.^[1]
Cell Research:	The FAM-FLICA Caspase 8 Kit was used to determine caspase 8 activity after the treatment of AGS-CRL-1739 cells with etoposide (1 μM, 12.5 μM) as well as a combination of etoposide (1 μM, 12.5 μM) with trastuzumab or pertuzumab (10 μg/mL) for 24 h. After incubation, the cells were harvested and washed with cold buffer PBS. Then, 5 μl of diluted FLICA reagent and 2 μl of Hoechst 33342 were added to 93 μl of the cell suspension and mixed by pipetting. The gastric cancer cells were incubated for 60 min at 37°C. After that time, the cells were washed twice in 400 μl apoptosis wash buffer and centrifuged at 300 x g. After the last wash, the cells were resuspended in 100 μl apoptosis wash buffer and supplemented with 10 μg/ml PI.

In Vitro

In vitro

The combination of pertuzumab with etoposide represents a promising strategy aimed at inhibition of viability and proliferation of gastric cancer cells. The mechanism of action includes induction of both extrinsic and intrinsic apoptotic pathway, where increased activity of caspase-8 and caspase-9 are demonstrated.^[1]

Cell Research:

The FAM-FLICA Caspase 8 Kit was used to determine caspase 8 activity after the treatment of AGS-CRL-1739 cells with etoposide (1 μM, 12.5 μM) as well as a combination of etoposide (1 μM, 12.5 μM) with trastuzumab or pertuzumab (10 μg/mL) for 24 h. After incubation, the cells were harvested and washed with cold buffer PBS. Then, 5 μl of diluted FLICA reagent and 2 μl of Hoechst 33342 were added to 93 μl of the cell suspension and mixed by pipetting. The gastric cancer cells were incubated for 60 min at 37°C. After that time, the cells were washed twice in 400 μl apoptosis wash buffer and centrifuged at 300 x g. After the last wash, the cells were resuspended in 100 μl apoptosis wash buffer and supplemented with 10 μg/ml PI.

In Vivo
In vivo	Pertuzumab significantly inhibits tumor growth when combined with erlotinib. Pertuzumab treated DLD-1 xenograft tumors shows no enhanced necrosis, which is found in HCT116 derived xenografts.^[2]
Animal Research	AnimalModels:Nude mice bearing colon cancer xenograft tumors Formulation:10 mmol/L l-histidine, 240 mmol/L sucrose, 0.02% polysorbate 20 (pH 6) Dosages:12 mg/kg, followed by 6 mg/kg/week Administration:i.p.^[2]

In Vivo

In vivo

Pertuzumab significantly inhibits tumor growth when combined with erlotinib. Pertuzumab treated DLD-1 xenograft tumors shows no enhanced necrosis, which is found in HCT116 derived xenografts.^[2]

Animal Research

AnimalModels:Nude mice bearing colon cancer xenograft tumors
Formulation:10 mmol/L l-histidine, 240 mmol/L sucrose, 0.02% polysorbate 20 (pH 6)
Dosages:12 mg/kg, followed by 6 mg/kg/week
Administration:i.p.^[2]

References
[1] Gornowicz A, et al. PLoS One. 2021 Aug 26;16(8):e0255585. [2] Pohl M, et al. J Cancer Res Clin Oncol. 2009 Oct;135(10):1377-86.

References

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

Product Details

CAS No.	380610-27-5
Isotype	Human IgG1
Source	CHO cells
Formulation	100 mM Pro-Ac, 20mM Arg, pH5.0
Storage (From the date of receipt)	Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles

Comparison of Clones for

^*Literature analysis of various clone (for this target) products available on the market shows that Selleck's selected clones are more frequently applied. (data until September 2024)

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Frequently Asked Questions

Question 1:
How to store the antibody?

Answer:
Store the undiluted solution at 4 °C in the dark. Freezing antibodies can result in a loss of activity caused by the freezing/thawing process. Diluting antibodies to working concentrations and storing at 4°C for more than a day should be avoided. Additionally, make sure to keep the antibody sterile. Under these storage conditions, your antibodies should remain active for up to one year and oftentimes longer.