PEG Linkers for ADCs Development

Today we offer you:

A fully certified high-quality PEG linkers, which can be used in many different fields, such as ADC linker. This is an excellent choice for your PEG linkers supply if you seek to translate your R&D efforts into faster commercialization:

• Providing high-purity PEG linkers with a wide variety of functional groups from R&D to commercial scale, in both non-GMP and GMP grades.
• Providing custom PEG linkers synthesis services to meet the unique needs of clients’ projects.
• Whenever you encounter any technical problems, we look forward to providing you with scientific guidance at any time!

Introduction to ADC Drugs

Antibody-drug conjugates (ADCs) are a class of targeted therapeutics for the treatment of cancer, consisting of monoclonal antibodies (Antibody) targeting tumor-specific or tumor-associated antigens coupled with different numbers of small molecule cytotoxic drug (Payloads) via linkers.

A superior ADC linker can help antibodies to selectively deliver and accurately release cytotoxic drugs at the tumor site. In addition, it plays critical roles in ADCs stability during preparation, storage and circulation. A stable ADC drug ensures that less cytotoxic payload is reduced before it reaches the tumor cell, thereby improving safety and limiting dose.

Fig. 1. Schematic diagram of ADC represents the key components and their significant role.

PEG Linkers for ADC Drugs

The PEG linker has become an attractive tool for bio-coupling, drug delivery and ADC development due to its water solubility and non-immunogenicity. PEG linkers are chemically functionalized polyethylene glycol (PEG) linkers. The use of various difunctionalized PEG linkers enables the formation of different types of ADC linkers by simple and rapid combinations with different structures. At the same time, it enables targeted coupling. In addition, the use of multibranched PEG derivatives not only increases the drug loading capacity, but also allows the construction of ADC molecules bearing multiple different toxins, which supports the development of a new generation of ADC drugs.

Fig. 2. Application of PEG Linkers in ADC Drugs.

PEG linkers are particularly attractive as linkers for antibody-drug couplers (ADCs):

1) Increase drug solubility and stability

2) Reduces toxicity

3) Reduces immunogenicity, improves pharmacokinetics and increases circulation time

Featured Monofunctional PEG Linkers
Catalog	Product Name	Structural Formula	MW	Reactive Group
CDPB-04221	mPEG3-NH2		163.2	Carboxy、Hydroxyl、Isocyanato
CDPB-04233	mPEG36-NH2		1616.95	Carboxy、Hydroxyl、Isocyanato
CDPB-041021	mPEG7-SPA		509.6	Amine
CDP23-0318	mPEG10-SPA		645	Amine
CDPB-041025	mPEG11-SPA		685.75	Amine
CDPB-041029	mPEG25-SPA		1301	Amine
CDPB-041063	mPEG8-Aldehyde		396.5	Amine、Aldehyde、Hydroxyl
CDBCP221	mPEG-SCM		-	Amine
CDPB-04836	Fmoc-NH-PEG3-COOH		443.5	Amine、Hydroxyl
CDPB-04837	Fmoc-NH-PEG4-COOH		487.6	Amine、Hydroxyl
CDN-04013	Fmoc-NH-PEG6-COOH		575.6	Amine、Hydroxyl
CDPB-04841	Fmoc-NH-PEG8-COOH		663.8	Amine、Hydroxyl
CDP23-0979	Fmoc-NH-PEG12-COOH		839.963	Amine、Hydroxyl
CDPB-04635	N-(Hydroxy-peg3)-n-boc-PEG4-t-butyl ester		597.74	Amine、Carboxy
CDPB-04167	Amino-PEG4-t-butyl ester		321.4	Hydroxy、Isocyanato
Featured Bifunctional PEG Linkers
Catalog	Product Name	Structural Formula	MW	Reactive Group
CDPB-041311	Mal-NH-PEG8-COOH*1		592.6	Thiol、Amine、Dienophile
CDP23-1143	2-((Azide-PEG8-carbamoyl) methoxy)acetic acid*2		554.6	DBCO、BCN、Alkyne、Amine、Hydroxyl
CDPB-041285	Mal-PEG12-NHS*3		794	Thiol、Amine、Dienophile
CDPB-041278	MAL-PEG1-NHS ester*3		310.3	Thiol、Amine、Dienophile
CDPB-041272	Mal-PEG3-COOH*4		301.3	Amine、Hydroxyl、Dienophile
CDPB-04141	NH2-PEG4-COOH*5		265.3	Amine、Hydroxyl、Isocyanato、Carboxy
CDPB-04143	NH2-PEG6-COOH*5		353.4	Amine、Hydroxyl、Isocyanato、Carboxy
CDPB-04152	NH2-PEG24-COOH*5		1146	Amine、Hydroxyl、Isocyanato、Carboxy
CDPB-04156	NH2-PEG36-COOH*5		1675	Amine、Hydroxyl、Isocyanato、Carboxy
CDP23-0952	COOH-PEG4-NH2.HCl		301.81	Amine、Hydroxyl
CDP23-0983	COOH-PEG24-NH2.HCl		1182	Amine、Hydroxyl
CDPB-04050	Alkyne-PEG2-NH2		143.2	Azide、Isocyanato、Carboxy、Hydroxyl
CDPB-04052	Alkyne-PEG4-NH2		231.3	Azide、Isocyanato、Carboxy、Hydroxyl

Featured Bifunctional PEG Linkers
Catalog	Product Name	Structural Formula	MW	Reactive Group
CDPB-04055	Alkyne-PEG8-NH2		407.5	Azide、Carboxy、Hydroxyl、Isocyanato
CDP23-0541	N3-PEG3-SPA		344.3	DBCO、BCN、Alkyne、Amine
CDP23-0319	OH-PEG6-OH		282.331	Amine、Carboxy
CDP23-0380	OH-PEG8-OH		370.436	Amine、Carboxy
CDP23-0379	OH-PEG9-OH		414.488	Amine、Carboxy
CDPB-04179	NH2-PEG4-OH		193.2	Amine、Hydroxyl、Carboxy、Isocyanato
CDPB-04182	NH2-PEG7-OH		325.4	Amine、Hydroxyl、Carboxy、Isocyanato
CDPB-04187	NH2-PEG12-OH		545.667	Amine、Carboxy、Hydroxyl、Isocyanato
CDN-04015	N3-PEG2-NH2		174.2	DBCO、BCN、Alkyne、Hydroxyl、Isocyanato、Carboxy
CDPB-041117	N3-PEG2-COOH		203.2	Amine、Hydroxyl、DBCO、BCN、Alkyne
CDPB-041119	N3-PEG4-COOH		291.3	Amine、Hydroxyl、DBCO、BCN、Alkyne
CDPB-041122	N3-PEG8-COOH		467.5	Amine、Hydroxyl、DBCO、BCN、Alkyne
CDPB-041123	N3-PEG9-COOH		511.6	Amine、Hydroxyl、DBCO、BCN、Alkyne
CDPB-041124	N3-PEG10-COOH		555.62	Amine、Hydroxyl、DBCO、BCN、Alkyne

Featured Bifunctional PEG Linkers
Catalog	Product Name	Structural Formula	MW	Reactive Group
CDPB-04557	N-(acid-PEG3)-N-Bis(PEG3-Azide)		623.7	Amine、Hydroxyl、DBCO、BCN、Alkyne
CDN1801	OH-PEG-NH2		-	Amine、Carboxy、Isocyanato
CDP23-0233	OH-PEG-AA		-	Amine、Hydroxyl、Carboxy
CDPB-04910	OH-PEG4-Tos		348.4	Amine、Carboxy
CDP23-0677	COOH-PEG-COOH		-	Amine、Hydroxyl

Note: Products marked with "*" are ADC linkers used in marketed drugs or research papers.

1. ADC Therapeutics, Inc. Zynlonta, first FDA-approved ADC targeting CD19.

2. Gilead Trodelvy^®, FDA-approved ADC for the treatment of mTNBC.

3. Trastuzumab-PEG24-DM1 (DOI: 10.1016/j.jconrel.2021.07.041)

4. Ab-PEG4-Mal-DM1 (DOI: 10.1158/0008-5472.CAN-09-3546)

5. Trastuzumab-conjugated ADCs (DIO: 10.1016/j.bmc.2021.116497)