Pertuzumab (anti-HER2)

Catalog No.A2008 Batch: A200802

Technical Data

CAS No.	380610-27-5
Formulation	PBS buffer, pH 7.2
Isotype	Human IgG1
Source	CHO cells
Storage (From the date of receipt)	Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles
Purity	99.17%
Protein concentration	5.02mg/ml
Endotoxin Level	≤1 EU/mg

Biological Activity

Description

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.

Targets

HER2 ^[1]

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]

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]

Protocol (Only for Reference)

Cell Assay:	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.
Animal Study:	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]

Cell Assay:

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.

Animal Study:

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

Customer Product Validation

Selleck's Pertuzumab (anti-HER2) has been cited by 7 publications

Multi-Targeting Anticancer Activity of a New 4-Thiazolidinone Derivative with Anti-HER2 Antibodies in Human AGS Gastric Cancer Cells [ Int J Mol Sci, 2023, 24(7)6791]	PubMed: 37047765
The effect of the alpha-specific PI3K inhibitor alpelisib combined with anti-HER2 therapy in HER2+/PIK3CA mutant breast cancer [ Front Oncol, 2023, 13:1108242]	PubMed: 37469415
Establishment and large-scale validation of a three-dimensional tumor model on an array chip for anticancer drug evaluation [ Front Pharmacol, 2022, 13:1032975]	PubMed: 36313330
Optical biosensor based on weak value amplification for the high sensitivity detection of Pertuzumab in combination with Trastuzumab binding to the extracellular domain of HER2 [ Opt Express, 2022, 30(20):36839-36848]	PubMed: 36258605
Anti-HER2 monoclonal antibodies intensify the susceptibility of human gastric cancer cells to etoposide by promoting apoptosis, but not autophagy [ PLoS One, 2021, 16(8):e0255585]	PubMed: 34437575
A common MET polymorphism harnesses HER2 signaling to drive aggressive squamous cell carcinoma [ Nat Commun, 2020, 11(1):1556]	PubMed: 32214092
WEE1 inhibitor, AZD1775, overcomes trastuzumab resistance by targeting cancer stem-like properties in HER2-positive breast cancer. [ Cancer Lett, 2020, 472:119-131]	PubMed: 31866466

FOR RESEARCH USE ONLY. NOT FOR USE IN HUMANS.

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