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Your Position: Home > Antibody-Drug Conjugates (ADCs): the Magic Bullets for Treatment

Antibody-Drug Conjugates (ADCs): the Magic Bullets for Treatment

Targets for Antibody-Drug Conjugates
Hot Products
Product list
ADC targets
Proteases
PK analysis
service
Background

In recent years, Antibody-Drug Conjugates (ADCs) may serve as a novel therapeutic modality for many cancer patients. Indeed, three key elements define an ADC: the antibody directed against a specific tumor antigen, the cytotoxin/payload and the cleavable/uncleavable linker connecting the payload to the antibody [1]. Specific target recognition and effective toxin make ADCs veritable "magic bullet". These 'magic bullets' deliver treatment that is both highly targeted and highly potent, seeking out and attacking cancerous cells throughout the body, while avoiding harm to healthy cells. Reasonable selection of targets, antibody, linker, payload, and their rational combinations are crucial for an effective treatment. Among these elements, target selection, linker selection and evaluating preclinical /clinical efficacy are considered critical factors for ADCs development. >>> Download the ebook: Key point of ADCs design

To meet the needs of ADCs development, ACROBiosystems can provide:
A variety of high-quality target proteins;
SPR/BLI analytical service;
MMPs/Cathepsin/uPA for cleavable linker;
Anti-payload antibodies, anti-idiotypic antibodies(ADA) for immunogenicity and PK analysis.
All products and services can meet the entire process of ADCs from antibody preparation, initial screening, production to quality control, facilitating your ADCs development.
Hot Products
High-quality ADC target proteins

Features

  1. >> 50+ ADC targets, such as Trop-2, Nectin-4,LIV-1 and ROR1;

  2. >> Various species & tag;

  3. >> High purity verified by MALS;

  4. >> High bioactivity verified by ELISA / SPR / BLI / FACS, etc.

Applications

  • Suitable for immunization / antibody screening / cross-reactivity/cell-based assay/QC.

Featured products

  • Exclusive LIV-1 proteins:

  • ✔ Multiple species: Human, Mouse, Cynomolgus, Rat, etc.;

  • ✔ Expression sequences were designed based on the SGN-LIV1A binding epitope.

Proteases for peptide linker

Features

  1. >> Comprehensive products: Cathepsin, MMPs and uPA etc.;

  2. >> Natural conformation: HEK293 expressed protein to ensure the natural structure;

  3. >> High enzyme activity: enzyme activity > 2,500 pmol/min/µg.

Applications

  • ✔ Evaluate the effect of proteases cleavage of linker to ensure the efficient release of the intracellular payloads.

Tools for ADCs PK analysis

Features

  1. >> Comprehensive products: anti-MMAE antibodies and anti-idiotypic antibodies;

  2. >> High specificity & affinity;

  3. >> High sensitivity & stability.

Applications

  • ✔ Positive reference of ADCs preclinical / clinical immunogenicity;

  • ✔ PK analysis;

  • ✔ Anti-payload antibodies: Qualitative detection of DAR value.

Featured products

  • The activity of anti-MMAE monoclonal antibody (Cat.No.MME-M5252) is verified by binding to Disitamab Vedotin (RC-48) with a linear range of 0.1-2 ng/mL.

SPR/BLI analytical & ADA development service

SPR/BLI analytical service：

  1. >> Proteins offered for free;

  2. >> Experienced R&D technical team;

  3. >> Personalized solution design and report format.

ADA development service：

  • Service：

  • Monoclonal/polyclonal anti-idiotype antibody, pharmacokinetic and immunogenicity test kit.

  • Applications:

  • ✔ ADA assay: Perfect as Calibrator;

  • ✔ PK assay: Quantitative analysis of therapeutic antibody in matrix.

Product list

  • ADC target proteins

  • Proteases for peptide linker

  • Tools for ADCs PK analysis

Her2 HOTNectin-4 HOTTROP-2 HOTLIV-1  HOT NEWROR1 HOT NEWMesothelin HOTCEACAM-5 HOTEGF R HOTSiglec-2 HOTSiglec-3 HOTGUCY2C HOTErbB3FOLR1(FRα)NEWBCMA HOTCoagulation Factor III NEWPTK7 NEWLY75 NEWENPP3 NEWClaudin-18.2 NEWTIM-1 NEWALCAMAxlB7-H3CA125CD27 LigandCD19CD30CD37CD46CD48CD74CD79BDLL3EGFRvIIIEpCAMFlt-3HGF RIGF-I RIL-2 R alphaIL-3 R alphaLRRC15 NCAM-1PSMAROR2SLC1A5Syndecan-1TNF-alphaTPBGTRAIL R2Transferrin R
TypeMoleculeCat.No.Product descriptionPreorder/Order
CathepsinCathepsin BCTB-H5222Human Cathepsin B / CTSB Protein, His Tag (active enzyme)

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Cathepsin LCT1-H5222Human Cathepsin L / CTSL1 Protein, His Tag

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Cathepsin SCTS-H5224Human Cathepsin S / CTSS Protein, His Tag

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PLAUPLAUPLU-H5229Human PLAU / uPA Protein, His Tag

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PLAUPLU-H5228Human PLAU / uPA Protein, His Tag (activated by trypsin) (active enzyme)

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MMPsMMP-1MM1-H5222Human MMP-1 Protein, His Tag

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MMP-2MM2-H5225Human MMP-2 Protein, His Tag

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MMP-2MM2-H82E3Biotinylated Human MMP-2 Protein, His,Avitag™

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MMP-2MM2-M52H3Mouse MMP-2 Protein, His Tag

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MMP-9MM9-H5221Human MMP-9 Protein, His Tag (active enzyme)

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Cat.No.Product descriptionNeutralizing activityAffinity KD, nMApplication
MME-M5252NEWAnti-MMAE Antibodies//PK assay; ELISA
ADB-Y19Anti-Adalimumab AntibodiesNeutralizing Antibody0.0013ADA assay; Neutralizing assay; Indirect ELISA
ADB-Y23bAnti-Adalimumab AntibodiesNon-Neutralizing Antibody/PK bridging ELISA with ADB-BY17; Indirect ELISA
ADB-BY17Biotinylated Anti-Adalimumab AntibodiesNeutralizing Antibody/PK bridging ELISA with ADB-Y23b
BEB-Y9Anti-Bevacizumab AntibodiesNeutralizing Antibody1.92ADA assay; Indirect ELISA
BEB-Y10Anti-Bevacizumab AntibodiesNeutralizing Antibody/PK bridging ELISA with BEB-BY13; Neutralizing assay; Indirect ELISA
BEB-BY13Biotinylated Anti-Bevacizumab AntibodiesNeutralizing Antibody/PK bridging ELISA with BEB-Y10
CEB-Y27Anti-Cetuximab AntibodiesNeutralizing Antibody0.007ADA assay; Neutralizing assay; Indirect ELISA
CEB-Y29Anti-Cetuximab AntibodiesNeutralizing Antibody/PK bridging ELISA with CEB-BY31; Neutralizing assay; Indirect ELISA
CEB-BY31Biotinylated Anti-Cetuximab AntibodiesNon-Neutralizing Antibody/PK bridging ELISA with CEB-Y29
RIB-Y35cAnti-Rituximab AntibodiesNeutralizing Antibody/ADA assay; Neutralizing assay; Indirect ELISA
TRB-Y1bAnti-Trastuzumab AntibodiesNeutralizing Antibody/PK bridging ELISA with TRB-Y5b; Neutralizing assay; Indirect ELISA
TRB-Y5bAnti-Trastuzumab AntibodiesNon-Neutralizing Antibody/PK bridging ELISA with TRB-Y1b
High-quality ADC target proteins
TROP-2
                    
Nectin-4
                    
EGFR
                    
Her2
                    
CEACAM-5
                    
CD79B
                    
PSMA
                    
Claudin18.2
                    
FOLR1
                    
Siglec-3
                    
BCMA
                    
Siglec-2
                    
CD19
                    
CD30
                    
DLL3
                    
PTK7
                    
TF
                    
TF
                    
ROR1
                    
ENPP3
                    
LIV-1
                    
HGFR
                    
NCAM-1
                    
EGFRvIII
                    
CD133
                    
LY75

Case study

High purity verified by MALS

The purity of Human Her2, His Tag (Cat. No. HE2-H5225) was more than 90% and the molecular weight of this protein is around 80-95 kDa verified by SEC-MALS.

High affinity validated by ELISA

Immobilized Human TROP-2, His Tag (Cat. No. HE2-H5225) at 1 μg/mL (100 μL/well) can bind Mouse Monoclonal Antibody Against Human TROP-2, Mouse IgG1 with a linear range of 0.1-2 ng/mL (QC tested).

Immobilized Human PSMA, His Tag (Cat. No. PSA-H52H3) at 2 μg/mL (100 μL/well) can bind Monoclonal Anti-Human PSMA Antibody, Human IgG1 with a linear range of 0.3-39 ng/mL (Routinely tested).

High affinity validated by SPR

Anti-LIV-1 mAb captured on CM5 chip via anti-human IgG Fc antibody can bind Human LIV-1, His Tag (Cat. No. LV1-H5223) with an affinity constant of 5.24 nM as determined in a SPR assay (Biacore T200) (Routinely tested).

Herceptin (Trastuzumab) captured on CM5 chip via anti-human IgG Fc antibodies surface, can bind Human Her2, His Tag (Cat. No. HE2-H5225) with an affinity constant of 1.07 nM as determined in a SPR assay.

High affinity validated by BLI

Loaded Mouse Nectin-4, His Tag (Cat. No. NE4-M52H3) on HIS1K Biosensor, can bind Human Nectin-1, Fc Tag (Cat. No. PV1-H5253) with an affinity constant of 0.12 μM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

High affinity validated by FACS

2e5 of anti-ROR1 CAR-293 cells were stained with 100 μL of 10 μg/mL of Human / Cynomolgus / Rhesus macaque ROR1 (39-151, Ig-like domain), His Tag (Cat. No. RO1-H5221) and negative control protein respectively, washed and then followed by PE-anti-His Tag and analyzed with FACS (Routinely tested).

Proteases for peptide linker
In the design and development of ADC, linker affects the stability of ADCs in systematic circulation, the speed of lysosomal processing, etc. There are two main categories of ADC linkers in current ADC drugs, cleavable linkers, and non-cleavable linkers.
Peptide linker as a protease-sensitive cleavable linker, is used in most ADCs that are undergoing clinical testing.  In the design of peptide linker, it is necessary to consider the selection of a suitable protease for linker cleavage, such as: MMPs/Cathepsin/ PLAU [2].
Thus, ACROBiosystems has developed a series of MMPs, Cathepsin and uPA protein products for cleavage of Linker.
More anti-payload antibodies (Anti-Dxd antibody/Anti-SN-38 antibody/Anti-SN-38 antibody) are coming soon！

Case study

ProductsCat.No：CTB-H5222 Human Cathepsin B / CTSB Protein, His Tag (active enzyme)Cat.No：MM9-H5221 Human MMP-9 Protein, His Tag (active enzyme)
Hydrolyzed substrateFluorogenic peptide substrate Z-LR-AMCFluorogenic peptide substrate Mca-PLGL-Dpa-AR-NH2
Enzymatic activity
（pmol/min/μg）		> 2500> 2500
PK analysis
Supporting Immunogenicity and PK analysis, ACRO provides series of anti-MMAE antibodies and anti-idiotypic antibodies with high affinity, high specificity and high sensitivity.
Used for the positive reference of ADCs preclinical/clinical immunogenicity and PK analysis;
Save customer's time to prepare antibodies;
Complete methodology protocols are available freely.

Case study

PK assay: Anti-MMAE antibody binding MMAE with high specificity

The EC50 value of anti-MMAE antibody to MMAE-conjugated hRS7 (MMAE-ADC) was 0.12 μg/ml. The unconjugated hRS7 antibody was used as negative control

Immobilized Disitamab Vedotin (RC48) at 0.2 μg/mL (100 μL/well) can bind Mouse Anti-MMAE Antibody, Mouse IgG1 (Cat. No. MME-M5252) with a linear range of 0.1-2 ng/mL (QC tested).

PK assay: Specific detection of antibody drug levels in the body
Detection of rituximab by antigen-capture ELISA (0.1% serum).
Detection of rituximab by anti-idiotypic capture ELISA (0.1% serum).
Detection of rituximab by anti-idiotypic bridging ELISA (10% serum).
MethodCoatedSampleLinear range
(µg/mL)		Sensitivity
(µg/mL)		Advantage
Antigen capture ELISACD20Goat anti-human IgG——Simple and universal method
Anti-idiotypic capture ELISAAnti-Rituximab AntibodiesGoat anti-human IgG0.156-100.156It is a simple method for extracting CD20
Bridging ELISA by anti-idiotypic antibodiesAnti-Rituximab AntibodiesBiotinylated Anti-Rituximab Antibodies0.012-0.780.012CD20 can be obtained with good sensitivity and low background noise
Comparison between anti-idiotypic capture ELISA and anti-idiotypic bridging elisa for rituximab detection in patient samples
SPR/BLI analytical service & Anti-idiotypic antibody development service
In addition, relying on a very capable and highly professional team, ACROBiosystems also provides customers with high-quality integrated SPR&BLI analytical service and one-stop services about monoclonal/polyclonal anti-idiotype antibody, facilitating your ADCs development.
SPR/BLI analytical service
Cooperated with hundreds of industrial and scientific research users;
Proteins offered for free;
High standard quality management control system;
Next day reports at the earliest;
Support more than 300 drugs until clinical applications.
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Anti-idiotypic antibody development service
ACRO proteins supplied for free;
Quick response, one-to-one service from the project team, real-time follow-up;
Provide one-stop service from antigen preparation to detection kit development;
Guaranteed delivery of PK/ADA detection reagents whose sensitivity meets regulatory requirements.
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References

[1]Criscitiello C, et al. Antibody-drug conjugates in solid tumors: a look into novel targets. J Hematol Oncol. 2021 Jan 28;14(1):20.

[2]Poreba M. Protease-activated prodrugs: strategies, challenges, and future directions. FEBS J. 2020 May;287(10):1936-1969.

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