PEG-derivatives for Drug Development


PEG-derivatives for Drug Development Download PDF

CD Bioparticles is a high-tech company that integrates professional R&D, production and sales to provide customized solutions for the development and production of drug delivery systems (DDS) and new medical materials.

CD Bioparticles is a leading global supplier of PEG derivatives with a dedicated research team and strong technical capabilities. These derivatives are manufactured under ISO9001 and ISO13485 compliance, and operate according to ICH Q7A guidelines to produce PEG derivatives. CD Bioparticles is committed to providing PEG raw material, high purity PEG derivatives, custom PEG synthesis and PEGylation services to customers worldwide. These PEG derivatives are used in a wide range of pharmaceuticals, sustained release, drug delivery, medical diagnostics, etc.

PEG derivatives for Drug Development

Today we offer you:

Fully certified high-quality PEG derivatives. They are an excellent choice for your PEG derivative supply if you seek to translate your R&D efforts into faster commercialization:

  • High-purity PEG derivatives with a wide variety of functional groups from R&D to commercial scale, in both non-GMP and GMP grades.
  • Large format, high purity PEG raw materials for chemical, biological, medical and commercial applications.
  • Custom PEG synthesis services to meet the unique needs of clients' projects.
  • Whenever you encounter any technical problems, we are always happy to provide you with scientific advice!

Table of Contents

  • PEGylation
  • LNPs Delivery System Excipients
  • PEG Linkers for ADC Drugs
  • PROTAC Linkers
  • PEG Hydrogels for Medical Devices
  • Dye Labeling
  • 3D Printing
  • PEG Raw Materials
  • Featured Monodispersed Linear PEGs
  • Featured Heterobifunctional Linear PEGs

PEGylation

PEGylation is the covalent addition of PEG to another molecule, which is mainly coupled to peptides, proteins and antibody fragments in the biomedical field.

Significant pharmacological advantages of PEGylation peptides, proteins and antibody fragments include:

1) Improvement of drug solubility

2) Reduction of potential drug toxicity

3) Reduction of dosage frequency

4) Enhancement of drug stability, especially protection against protein drug degradation

PEGylation Reagents

Product Name Structural Formula PEG MW CAS NO.
mPEG-SC
550, 750, 1k, 2K, 3.4K, 4K, 5K, 10K, 12K, 20K, 30K, 40K Da -
mPEG-Mal
1k, 2K, 3.4K, 5K, 10K, 20K, 30K, 40K Da -
t-Boc-N-amido-PEG3-CH2CO2H
- 462100-06-7
Fmoc-NH-PEG4-COOH
- 557756-85-1
mPEG-ALD
350, 550, 750, 1k, 2K, 3.4K, 5K, 10K, 12K, 20K, 30K, 40K Da -
mPEG-SPA
350, 550, 750, 1k, 2K, 3.4K, 5K, 6K, 8K, 10K, 20K, 30K, 40K Da -
Amino-PEG2-t-butyl ester
- 756525-95-8
t-Boc-N-amide-PEG2-CH2CO2H
- 108466-89-3

LNPs Delivery System Excipients

Lipid nanoparticles (LNPs) are commonly used drug delivery systems in the field of nucleic acid drugs. The LNP technology is mainly developed for vaccine development.

Among them, PEG is commonly used to improve the stability of LNPs.

Product Name Structural Formula PEG MW CAS NO.
mPEG-DTA
2K, 3.4K, 5K, 10K Da 1849616-42-7
mPEG-DMG
550, 1K, 2K, 3.4K, 5K, 10K Da 160743-62-4
mPEG-CH2CH2CH2-NH2
2K, 3.4K, 5K, 10K Da -
DSPE-PEG-Mannose
1K, 2K, 3.4K, 5K, 10K, 20K Da -
mPEG-DPPE
2K, 5K Da 205494-72-0
mPEG-DSPE
350, 550, 750, 1K, 2K, 3.4K, 4K, 5K, 10K, 20K, 30K, 40K Da 147867-65-0
mPEG-AA
350, 550, 750, 1K, 2K, 3.4K, 4K, 5K, 10K, 20K, 30K, 40K Da -
mPEG-OH
350, 550, 750, 1K, 2K, 3.4K, 4K, 5K, 10K, 20K, 30K, 40K Da 9004-74-4
DSPE-PEG-NH2
200, 400, 500, 600, 800, 1K, 2K, 3.4K, 5K, 6K, 8K, 10K, 20K Da 474922-26-4
DOPE-PEG-NH2
2K, 3.4K, 5K, 10K Da -
DOPE-PEG-FA
2K Da -
CLS-PEG-OH
1K, 2K, 5K Da -
Palmitic acid-PEG-NH2
2K, 5K Da -

PEG Linkers for 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 toxins (Payloads) via linkers. The chemistry of the linker affects various properties of ADCs, including toxicity, specificity, stability and potency.

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

1) Increase drug solubility and stability

2) Reduce toxicity

3) Reduce immunogenicity, improve pharmacokinetics and increase circulation time

Product Name Structural Formula Molecular weight Purity
COOH-PEG4-NH2.HCl
301.81 ≥95%
2-((Azido-PEG8-carbamoyl)methoxy)acetic acid
554.6 ≥95%
mPEG25-SPA
1301 ≥95%
Mal-PEG12-NHS
794 ≥95%
Mal-NH-PEG8-COOH
592.6 ≥95%
Alkyne-PEG4-NH2 231.3 ≥95%
mPEG-SCM
- ≥95%
N3-PEG3-SPA
344.3 ≥95%
Mal-PEG3-COOH
301.3 ≥95%
N-(Hydroxy-peg3)-n-boc-peg4-t-butyl ester
597.74 ≥95%
NH2-PEG12-OH
545.667 ≥95%
mPEG36-NH2
1616.95 ≥95%

PROTAC Linkers

PROTAC is a bifunctional molecule that efficiently and specifically catalyzes the degradation of disease-causing proteins. It consists of three parts: a target protein binding ligand at one end, an E3 ubiquitin ligand at the other end, and a linker chain in the middle.

PEG linkers are the most common motifs in the PROTAC linker structure.

Product Name Structural Formula Molecular weight Purity
Tos-PEG3-O-C1-CH3COO
376.42 ≥95%
Boc-NH-PEG2-Tos
403.49 ≥95%
Tos-PEG2-NH2
259.32 ≥95%
Thalidomide-O-PEG5-Tosyl
578.61 ≥95%
Dox-Ph-PEG1-Cl
228.67 ≥95%
NH2-Ph-C4-acid-NH2-Me
222.28 ≥95%
Boc-NH-PEG2-C2-amido-C4-acid
376.45 ≥95%
Boc-C1-PEG2-C4-Cl
294.81 ≥95%
Thalidomide-O-amido-PEG3-NH2
506.509 ≥95%
Tos-PEG4-Tos
502.6 ≥95%
Boc-NH-PEG3-OH
249.3 ≥95%
Pomalidomide-PEG4-Ph-NH2
540.57 ≥95%

PEG Hydrogels for Medical Devices

Multi-arm PEG derivatives are mostly employed in the formation of hydrogels. PEG hydrogels can be used to prepare drug slow-release systems, tissue engineering, cell culture, wound sealing, wound healing and so on. In drug slow-release systems, PEG-PLA hydrogels can be used as carriers to control the release rate of drugs. In tissue engineering, PEG-DA hydrogel can be used as the scaffold material for cell culture and tissue repair.

Product Name Structural Formula PEG MW Purity
8-Arm-PEG-SS
5K, 10K, 20K, 40K Da ≥95%
8-Arm-PEG-SG
5K, 10K, 20K, 40K Da ≥95%
4-Arm-PEG-SS
2K, 5K, 10K, 20K, 40K Da ≥95%
4-Arm-PEG-SG
2K, 5K, 10K, 20K, 40K Da ≥95%
8-Arm-PEG-SH
10K, 20K, 40K Da ≥95%

Dye Labeling

PEGylated fluorescent dyes enhance specific tumor labeling. The PEG chains alter tissue biodistribution, allowing brighter liver metastases labeling and decreased accumulation in normal organs, particularly the liver.

PEG derivatives for Drug Development

PEG derivatives for Drug Development

3D Printing

3D printing has become a promising frontier in the field of complex tissue engineering due to its porosity, biodegradability and good biocompatibility. PEG derivatives are particularly attractive in three-dimensional printing due to their good biocompatibility under both in vitro and in vivo conditions.

Product Name Structural Formula PEG MW
AC-PEG-RGD
2K, 3.4K, 5K Da
8-Arm-PEG-Acrylate
5K, 10K, 20K, 40K Da
ACRL-PEG-ACRL
400, 600, 800, 1k, 2K, 3.4K, 5K, 10K, 20K Da

PEG Raw Materials

CD Bioparticles provides high purity PEG raw materials (linear and multi-arm PEG) for chemical, biological, medical and industrial applications in batch sizes of 5kg, 15kg, 20kg and 100kg. These PEG raw materials are suitable for further derivatization into PEG derivatives.

Product Name Structural Formula PEG MW
4-Arm-PEG-OH
5K, 10K, 20K, 40K Da
mPEG-OH
1K, 2K, 3.5K, 5K, 10K, 20K, 40K Da
NH2-PEG-NH2
1K, 2K, 3.4K, 5K, 10K, 20K, 40K Da
Trt-PEG-OH
1K, 1.2K, 2K, 3.4K, 5K, 6K, 8K, 10K, 20K Da
HO-PEG-OH
200, 400, 500, 800, 1K, 1.2K, 2K, 3.4K, 5K, 10K, 20K, 40K Da

Featured Monodispersed Linear PEGs

Product Name Structural Formula Molecular weight Purity
(2-pyridyldithio)-PEG2-t-butyl ester
359.5 ≥95%
2-((Azide-PEG8-carbamoyl)methoxy)acetic acid
554.6 ≥95%
N3-PEG3-OH
175.186 ≥95%
SH-PEG3-SH
226.4 ≥95%
Mal-NH-PEG4-NHS
513.5 ≥95%
NH2-PEG3-OH
149.18 ≥95%
Boc-NH-PEG3-Tos
447.54 ≥95%
Trityl-PEG7-N3
637.8 ≥95%
OH-PEG4-Tos
348.412 ≥95%
OH-PEG9-OH
414.488 ≥95%
N3-PEG3-COOH
247.3 ≥95%
Fmoc-NH-PEG8-CH2COOH
649.7 ≥95%
NH2-PEG5-CH2CH2COOtBu
365.5 ≥95%
CLS-PEG4-NH-Mal
856.14 ≥95%
N3-PEG3-SPA
344.3 ≥95%

Featured Heterobifunctional Linear PEGs

Product Name Structural Formula PEG MW Purity
SH-PEG-Biotin
200, 400, 500, 600, 800, 1K, 2K, 3.4K, 5K, 6K, 8K, 10K, 20K Da ≥95%
SH-PEG-NH2
200, 400, 500, 600, 800, 1K, 2K, 3.4K, 5K, 6K, 8K, 10K, 20K Da ≥95%
Mal-PEG-SCM
1K, 2K, 3.4K, 5K, 7.5K, 10K, 20K Da ≥95%
HO-PEG-Propylamine-Boc
3.4K Da ≥95%
Br-CH2CO-NH-PEG-OH
1K, 2K, 5K Da ≥95%
Boc-NH-PEG-SH
2K, 3K, 3.4K, 5K, 10K Da ≥95%
PLGA(15K)-PEG-Mal
2K, 3.5K, 5K, 10K Da ≥95%
Phosphoric acid-PEG-COOH
2K Da ≥95%
I-PEG-COOH
2K, 5K Da ≥95%
N3-PEG-Br
2K, 5K, 10K, 20K Da ≥95%
Bn2-PEG-OH
1K, 1.5K, 2k, 3.4K, 5K, 10K, 20K Da ≥95%
DF-PEG-NH2
2K, 3.4K, 5K Da ≥95%
DBCO-PEG-AC
1K, 2K, 5K, 10K Da ≥95%
HZ-PEG-N3
2K, 3.4K, 5K, 10K Da ≥95%
ACA-PEG-SVA
3.4K Da ≥95%
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