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PROTAC BRD4 Degrader-5-CO-PEG3-N3

  CAS No.:   Cat No.: BADC-01355   Purity: 98% 4.5  

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker, which includes the BRD4 degrader GNE-987 and PEG-based linker.

PROTAC BRD4 Degrader-5-CO-PEG3-N3

Structure of

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Category
ADC Linker
Molecular Formula
C58H75ClN12O12S2
Molecular Weight
1231.87
Storage
Store at 0-4°C for short term (days to weeks) or -20°C for long term (months to years)

* For research and manufacturing use only. We do not sell to patients.

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Popular Publications Citing BOC Sciences Products
IUPAC Name
[(3R,5S)-1-[(2S)-2-[[2-[2-[2-[2-[[2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetyl]amino]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-5-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-3-yl] 2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]acetate
Canonical SMILES
CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NC(C)C5=CC=C(C=C5)C6=C(N=CS6)C)OC(=O)COCCOCCOCCN=[N+]=[N-])C(C)(C)C)C7=CC=C(C=C7)Cl)C
InChI
InChI=1S/C58H75ClN12O12S2/c1-35-38(4)85-57-50(35)51(41-13-15-43(59)16-14-41)65-45(54-68-67-39(5)71(54)57)30-47(72)61-17-19-77-21-23-79-25-27-81-32-48(73)66-53(58(6,7)8)56(76)70-31-44(83-49(74)33-82-28-26-80-24-22-78-20-18-63-69-60)29-46(70)55(75)64-36(2)40-9-11-42(12-10-40)52-37(3)62-34-84-52/h9-16,34,36,44-46,53H,17-33H2,1-8H3,(H,61,72)(H,64,75)(H,66,73)/t36-,44+,45-,46-,53+/m0/s1
InChIKey
WMOYJXQCSDGERS-WVLZNWKQSA-N
Appearance
Solid
Storage
Store at 0-4°C for short term (days to weeks) or -20°C for long term (months to years)

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a targeted degrader molecule for BRD4, applied in ADC payload and linker research. The structure integrates a PROTAC moiety with a PEG3 spacer and an azide functional group (N3), enabling conjugation to antibodies via click chemistry. In ADC linker design, the PEG3 spacer provides flexibility and solubility, allowing precise attachment of the payload while maintaining antibody functionality.

In ADC payload applications, the PEG3 segment reduces steric hindrance between the antibody and the PROTAC payload, preserving antigen-binding capability and supporting predictable pharmacokinetics. The azide functional group facilitates bioorthogonal, site-specific conjugation, enabling consistent drug-to-antibody ratios (DAR) and controlled delivery of the BRD4 degrader to target cells.

The chemical stability of PROTAC BRD4 Degrader-5-CO-PEG3-N3 under physiological conditions ensures that the payload remains attached during circulation until reaching the tumor microenvironment, where it can induce BRD4 degradation. Its design is compatible with various ADC linker chemistries and antibody formats, making it suitable for research on targeted protein degradation within ADC frameworks.

This PROTAC-based linker-payload conjugate is applied in ADC studies that require precise payload attachment, controlled drug release, and evaluation of linker-payload interactions. The combination of PEG3 flexibility and azide reactivity allows effective integration into antibody-drug conjugates for research in targeted oncology therapeutics.

What is PROTAC BRD4 Degrader-5-CO-PEG3-N3 and its role in ADCs?

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a bifunctional molecule designed for targeted protein degradation of BRD4. The PEG3-N3 moiety enables conjugation to antibodies via click chemistry for ADC applications.

9/8/2021

We would like to know how PROTAC BRD4 Degrader-5-CO-PEG3-N3 achieves targeted degradation.

The PROTAC recruits E3 ligases to BRD4, promoting ubiquitination and proteasomal degradation. Conjugation to antibodies allows selective delivery to target cells, enhancing degradation efficiency while minimizing systemic exposure.

2/2/2019

Could you kindly advise what conjugation strategies are used with PROTAC BRD4 Degrader-5-CO-PEG3-N3?

The azide group in PROTAC BRD4 Degrader-5-CO-PEG3-N3 enables SPAAC click chemistry with cyclooctyne-functionalized antibodies, providing a copper-free, efficient, and site-specific conjugation method.

12/2/2016

Good morning! What precautions should be taken when using PROTAC BRD4 Degrader-5-CO-PEG3-N3 in ADC synthesis?

Due to its chemical sensitivity, the PROTAC should be stored under inert conditions at low temperature and protected from moisture. Reaction conditions should avoid strong acids or bases to maintain structural integrity.

4/8/2022

Good afternoon! What quality and analytical documentation is available for PROTAC BRD4 Degrader-5-CO-PEG3-N3?

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is accompanied by supporting documents including CoA, NMR, and MS verification to confirm structure and composition. Storage is recommended at low temperatures, typically -20°C, in a moisture-free environment to maintain chemical integrity. Detailed handling protocols are provided to ensure safe and stable use in experimental procedures.

7/11/2018

— Dr. James Carter, Senior Scientist (USA)

PROTAC BRD4 Degrader-5-CO-PEG3-N3 enabled precise degradation studies with consistent lot-to-lot quality. Highly reliable product.

12/2/2016

— Prof. Anna Müller, Biochemistry Researcher (Germany)

The delivery of PROTAC BRD4 Degrader-5-CO-PEG3-N3 was prompt, and batch purity was excellent, facilitating our preclinical studies.

7/11/2018

— Dr. Michael Thompson, ADC Scientist (UK)

Using PROTAC BRD4 Degrader-5-CO-PEG3-N3, we achieved reproducible cellular degradation assays without unexpected variability.

4/8/2022

— Dr. Michael Evans, Medicinal Chemist (USA)

The PROTAC BRD4 Degrader-5-CO-PEG3-N3 performed flawlessly in our degradation assays. BOC Sciences ensured consistent purity and timely delivery.

9/8/2021

— Dr. Laurent Dupont, Medicinal Chemist (France)

PROTAC BRD4 Degrader-5-CO-PEG3-N3 outperformed our previous linkers in efficiency and purity.

— Prof. Emily Thompson, Medicinal Chemist (UK)

The PROTAC BRD4 Degrader-5-CO-PEG3-N3 arrived ahead of schedule and performed flawlessly in our degradation assays. The detailed datasheet made planning experiments much easier.

2/2/2019

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Historical Records: SS-bis-amino-PEG4-NHS ester | PTAD-PEG4-amine | PTAD-PEG4-alkyne | Aminooxy-amido-PEG4-propargyl | Tetrazine-PEG4-oxyamine hydrochloride | NH2-PEG4-hydrazone-DBCO | Tetrazine-PEG6-amine hydrochloride | APN-PEG36-tetrazine | NH2-C5-PEG4-N3-L-Lysine-PEG3-N3 | Tetrazine-PEG4-SS-Py | PROTAC BRD4 Degrader-5-CO-PEG3-N3
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