ADC Linkers, PEG Linkers Supply

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ADC Linkers

Antibody-drug conjugates (ADCs) are a rapidly evolving class of biopharmaceuticals that are revolutionizing clinical cancer therapy. Often described as guided missiles, ADCs are designed to deliver potent cytotoxic payloads directly to tumor cells while sparing healthy tissue. Currently, dozens of ADCs have been approved and over hundreds are in various stages of clinical trials. An ADC consists of three critical components:

● Monoclonal Antibody (mAb): Targets specific proteins on tumor surfaces.
● Cytotoxic Payload: The warhead that kills the cancer cell.
● ADC Linker: The chemical bridge connecting the antibody to the payload.

The linker plays a critical role in determining stability, release behavior, and overall therapeutic performance. ADC linkers are generally classified into two main types: cleavable linkers and non-cleavable linkers.

● Cleavable Linkers: Cleavable linkers (including pH-sensitive hydrazone bonds, reduction-sensitive disulfide bonds, and enzyme-sensitive peptides) utilize the unique environment of the tumor cell to trigger the release of the payload. They are used in over 80% of clinically approved ADCs.
● Non-Cleavable Linkers: Non-cleavable linkers offer exceptional plasma stability and rely on the complete degradation of the antibody for payload release.

The Strategic Advantage of PEG Linkers in ADCs

PEG linkers are especially valuable in ADC development, particularly monodispersed PEG chains. Unlike polydispersed mixtures, monodispersed PEGs consist of a single, precise molecular weight, ensuring high purity and batch-to-batch consistency.

PEGs create a protective shield that wraps the ADC payload from its microenvironment, improving solubility and stability. Other benefits include reduced aggregation and thus lower immunogenicity, improved pharmacokinetics, increased circulation time and reduced toxicity.

Two of the most recent landmark ADC approvals— Trodelvy and Zynlonta —were developed using PEG moieties as a core part of their linker technology. These components are vital for improving solubility and maintaining stability in vivo.

Biopharma PEG offers a variety of PEG linkers to facilitate ADC development projects. All PEG linkers are of >95% purity and they are the basic building blocks for a successful ADC.

Technique support: GMP standard production support, impurity control < 0.5%. Contact for Technical Files.

References:
1. Zheng Su, Dian Xiao, Fei Xie, Lianqi Liu, Yanming Wang, Shiyong Fan, Xinbo Zhou, Song Li, Antibody–drug conjugates: Recent advances in linker chemistry, Acta Pharmaceutica Sinica B, Volume 11, Issue 12, 2021,Pages 3889-3907, ISSN 2211-3835, https://doi.org/10.1016/j.apsb.2021.03.042.
2. Joubert, N.; Beck, A.; Dumontet, C.; Denevault-Sabourin, C. Antibody–Drug Conjugates: The Last Decade. Pharmaceuticals 2020, 13, 245. https://doi.org/10.3390/ph13090245

Catalog No.	Name	Structure	M.W.	Purity	Buy
MD006005	N3-PEG2-NH2		174.2	≥95%

MD006005	N3-PEG4-NH2		262.31	≥95%

MD006016	N3-PEG2-COOH		203.19	≥95%

MD006016	N3-PEG3-COOH		247.3	≥95%

MD006016	N3-PEG4-COOH		291.301	≥95%

MD006016	N3-PEG5-COOH		335.35	≥95%

MD006016	N3-PEG6-COOH		379.41	≥95%

MD006016	N3-PEG8-COOH		467.51	≥95%

MD006016	N3-PEG9-COOH		511.56	≥95%

MD006025	N3-PEG3-SPA		344.3	≥95%

MD006025	N3-PEG4-SPA		388.37	≥95%

MD002002	OH-PEG8-OH		370.436	≥95%

MD002002	OH-PEG9-OH		414.488	≥95%

MD002002	OH-PEG24-OH		1075.28	≥95%

MD002038	OH-PEG4-Tos		348.412	≥95%

MD001025	mPEG7-SPA		509.5	≥95%

MD001025	mPEG10-SPA		645	≥95%

MD001025	mPEG11-SPA		685.75	≥95%

MD001025	mPEG25-SPA		1301	≥95%

MD005002	NH2-PEG4-OH		193.2	≥95%

MD005002	NH2-PEG12-OH		545.667	≥95%

MD005016	NH2-PEG4-COOH		265.3	≥95%

MD005016	NH2-PEG6-COOH		353.4	≥95%

MD005016	NH2-PEG24-COOH		1146.37	≥95%

MD005016	NH2-PEG36-COOH		1674.99	≥95%

MD005067	NH2-PEG2-CH2CH2COOtBu		233.3	≥95%

MD005067	NH2-PEG4-CH2CH2COOtBu		321.4	≥95%

MD005067	NH2-PEG6-CH2CH2COOtBu		409.5	≥95%

MD005067	NH2-PEG8-CH2CH2COOtBu		497.6	≥95%

MD006300	2-((Azido-PEG8-carbamoyl)methoxy)acetic acid		554.6	≥95%

MD136016	CBZ-NH-PEG3-COOH		355.383	≥95%

MD069016	Fmoc-NH-PEG2-COOH		399.44	≥95%

MD069016	Fmoc-NH-PEG3-COOH		443.5	≥95%

MD069016	Fmoc-NH-PEG4-COOH		487.5	≥95%

MD069016	Fmoc-NH-PEG8-COOH		663.8	≥95%

MD069016	Fmoc-NH-PEG12-COOH		839.963	≥95%

MD141016	Mal-PEG4-COOH		345.3	≥95%

MD141025	Mal-PEG1-SPA		310.26	≥95%

MD141025	Mal-PEG2-NHS		354.3	≥95%

MD141025	Mal-PEG4-NHS		442.4	≥95%

MD000019	N-(acid-PEG3)-N-bis(PEG3-azide)		623.7	≥95%

MD000017	N-(ACID-PEG3)-N-BIS(PEG3-AMINE)		571.704	≥95%

MD000019	N-(Hydroxy-peg3)-n-boc-peg4-t-butyl ester		597.74	≥95%

MD001212	mPEG8-CH2CH2CHO		396.5	≥95%

MD002067	OH-PEG3-CH2CH2COOtBu		278.3	≥95%

MD002067	OH-PEG4-CH2CH2COOtBu		322.39	≥95%

MD005121	NH2-PEG4-CH2COOH		251.3	≥95%

MD016050	COOH-PEG24-NH2.HCl		1182	≥95%

MD022005	Mal-NH-PEG2-NH2			≥95%

MD022016	Mal-NH-PEG8-COOH		592.6	≥95%

MD023023	NHS-PEG3-NHS		444.4	≥95%

MD007005	Alkyne-PEG2-NH2		143.2	≥95%

MD007005	Alkyne-PEG8-NH2		407.5	≥95%

MD007016	Alkyne-PEG3-COOH		216.2	≥95%

MD056006	Br-PEG2-N3		238.08	≥95%

MD056006	Br-PEG3-N3		282.1	≥95%

MD056067	Br-PEG4-CH2CH2COOtBu		385.29	≥95%

MD056068	Br-PEG4-NH-Boc		400.31	≥95%

MD068002	Boc-NH-PEG6-OH		381.5	≥95%

MD068005	BOC-NH-PEG4-NH2		336.4	≥95%

MD068121	Boc-NH-PEG2-CH2COOH		263.3	≥95%

MD115006	Aminooxy-PEG3-N3		234.3	≥95%