1350456-56-2

Basic information

• Product Name: FMoc-Val-Cit-PAB-MMAE
• Synonyms: FMoc-Val-Cit-PAB-MMAE
• CAS NO: 1350456-56-2
• Molecular Formula: C73H104N10O14
• Molecular Weight: 1345.66546
• Mol File: 1350456-56-2.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: FMoc-Val-Cit-PAB-MMAE(CAS DataBase Reference)
• NIST Chemistry Reference: FMoc-Val-Cit-PAB-MMAE(1350456-56-2)
• EPA Substance Registry System: FMoc-Val-Cit-PAB-MMAE(1350456-56-2)

Safety Data

• Hazardous Substances Data: 1350456-56-2(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
FMoc-Val-Cit-PAB-MMAE is used as a precursor for antibody drug conjugates (ADCs) for the targeted treatment of cancer. The molecule is engineered to be attached to a monoclonal antibody (MAb), which directs the ADC towards cancer cells. Upon internalization, the cleavable Val-Cit peptide and PABC linker ensure the release of the cytotoxic MMAE payload within the cancer cell, leading to cell death and potentially reducing damage to healthy cells.
Additionally, FMoc-Val-Cit-PAB-MMAE may be used in the development of novel drug delivery systems to improve the efficacy and bioavailability of ADCs, potentially enhancing their therapeutic outcomes in cancer treatment.

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Relevant articles and documents

PHOSPHOLIPID ETHER CONJUGATES AS CANCER-TARGETING DRUG VEHICLES

Disclosed herein are therapeutic compounds capable of targeting a broad range of tumor cells. The present disclosure is further directed to compositions comprising the therapeutic compounds, methods of manufacturing the therapeutic compounds, and methods of treating cancer comprising administering the therapeutic compounds.

ANTIBODY-DRUG CONJUGATE

Provided herein is an antibody-drug conjugate (ADC) especially a PEGylated mono or bispecific antibody-drug conjugate (BsADC) prepared with site-specific conjugation to provide homogeneous conjugate with high potency and low toxicity. It also relates to a

SELF-STABILIZING LINKER CONJUGATES

The present invention provides Ligand-Drug Conjugates, Drug-Linkers, Linkers, and Ligand-Linker Conjugates comprising a self-stabilizing linker assembly component.

LINKERS AND CONJUGATES

A conjugate comprising a protein or a peptide, a linker and an active agent, wherein the linker comprises the moiety of formula (III): (III) wherein two of A1, A2 and A3 are N and the other of A1, A2

PROCESS FOR PREPARING INTERMEDIATE OF ANTIBODY DRUG CONJUGATE

The present disclosure relates to a process for preparing an intermediate of antibody-drug conjugate. Compared with the conventional art, the process for preparing an intermediate of the antibody-drug conjugate provided by the present disclosure significantly reduces the feed loss for drug moiety, such as MMAD/MMAE or MMAF, etc., as drug moiety is involved in the last step of the reaction, thereby effectively reducing production costs, as well as increasing production efficiency. In addition, the process provided by the present disclosure is simple, environmentally friendly and suitable for large-scale industrialization.

ACYL HYDRAZONE LINKERS, METHODS AND USES THEREOF

The present application is directed to compounds of Formula (I)-(VI): (I), (II), (III), (IV), (V) (VI), (VII) and (VIII), compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics.

HETEROCYCLIC ACYL HYDRAZONE LINKERS, METHODS AND USES THEREOF

The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and /or diagnostics.

Covalent Linkers in Antibody-Drug Conjugates and Methods of Making and Using the Same

The present invention provides novel and advantageous compositions having a linker capable of covalently coupling one or more free thiols of an antibody. Specifically, provided herein are the molecular structures, synthetic pathways, coupling mechanisms, and applications thereof as used in an antibody-drug conjugate (ADC).

CYCLODEXTRIN PROTEIN DRUG CONJUGATES

Provided herein are compounds, compositions, conjugates and methods for the treatment of diseases, and/or conditions such as, but not limited to, proliferative diseases. In certain embodiments, compounds, compositions, and conjugates are provided, which include cyclodextrin-based linker-payloads and protein conjugates thereof, and/or in combination with other agents. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced.

One-pot: N -glycosylation remodeling of IgG with non-natural sialylglycopeptides enables glycosite-specific and dual-payload antibody-drug conjugates

Chemoenzymatic transglycosylation catalyzed by endo-S mutants is a powerful tool for in vitro glycoengineering of therapeutic antibodies. In this paper, we report a one-pot chemoenzymatic synthesis of glycoengineered Herceptin using an egg-yolk sialylglycopeptide (SGP) substrate. Combining this one-pot strategy with novel non-natural SGP derivatives carrying azido or alkyne tags, glycosite-specific conjugation was enabled for the development of new antibody-drug conjugates (ADCs). The site-specific ADCs and semi-site-specific dual-drug ADCs were successfully achieved and characterized with SDS-PAGE, intact antibody or ADC mass spectrometry analysis, and PNGase-F digestion analysis. Cancer cell cytotoxicity assay revealed that small-molecule drug release of these ADCs relied on the cleavable Val-Cit linker fragment embedded in the structure. These results represent a new approach for glycosite-specific and dual-drug ADC design and rapid synthesis, and also provide the structural requirement for their biologic activities.