863971-53-3

Usage

Uses

Used in Pharmaceutical Industry:
FMoc-Val-Cit-PAB-PNP is used as a cleavable linker in the development of antibody drug conjugates (ADCs) for targeted cancer therapy. The Val-Cit linker is specifically designed to be cleaved by cathepsin B, an enzyme overexpressed in cancer cells, allowing for the selective release of the cytotoxic payload within the tumor microenvironment. This targeted approach aims to minimize systemic toxicity and improve the therapeutic index of the treatment.
Additionally, the PNP group in FMoc-Val-Cit-PAB-PNP serves as a versatile and efficient leaving group for the conjugation of amine-bearing payloads, enabling the development of a wide range of ADCs with different cytotoxic drugs. This flexibility allows researchers to optimize the potency and selectivity of ADCs, potentially leading to more effective cancer treatments with fewer side effects.

Biological Activity

Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker that can be used to synthesize antibody drug conjugates (ADCs).

Upstream product

• 5070-13-3 bis-(p-nitrophenyl) carbonate 
• 159858-22-7 (9H-fluorenyl)methyl ((S)-1-(((S)-1-(((4-(hydroxymethyl)phenyl)amino)-1-oxo-5-ureidovalerylamido-2-yl)amino))-3-methylbutyramido-2-yl)-carbamate 
• 67-56-1 methanol 
• 372-75-8 Citrulline 
• 623-04-1 4-aminobenzenemethanol 
• 159858-21-6 (S)-2-((S)-2-((((9H-fluoren-9-yl)-methoxy)carbonyl)amino)-3-methylbutanamido)-5-ureidopentanoic acid 
• 130878-68-1 2,5-dioxopyrrolidin-1-yl-N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-valinate 
• 7693-46-1 4-Nitrophenyl chloroformate 
• 68858-20-8 Fmoc-Val-OH 

Downstream Products

• 1610769-13-5 4-((S)-2-((S)-2-amino-3-methylbutanamido)-5-ureidopentanamido)benzyl (2-(pyridin-2-yldisulfanyl)ethyl)carbamate 
• 1613321-11-1 (2S,3S,4R)-2-(N-((9H-fluoren-9-yl)methoxycarbonyl)-L-valinyl-L-citrullinyl-4-am inobenzyloxycarbonylamino)-1-(δ-D-galactopyranosyloxy)-3-hydroxyoctadecan-4-yl hexacosanoate 
• 1350456-56-2 C₇₃H₁₀₄N₁₀O₁₄ 

Relevant academic research and scientific papers

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

CANCER VACCINE

The invention relates to a combination of a TLR-9 agonist and a conjugate of Formula (I) or pharmaceutically acceptable salt thereof. (Formula (I))

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

GLYCOPEPTIDE VACCINE

The present invention generally relates to a glycopeptide conjugate compound of Formula (I):, as described herein, compositions comprising the conjugate compound and to the use of such a compound to as a vaccine.

SULFOMALEIMIDE-BASED LINKERS AND CORRESPONDING CONJUGATES

The present invention relates to a linker of the following formula (I) or a salt thereof: (I). The present invention relates to a linker-drug conjugate of the following formula (II) or a salt thereof: (II). The present invention relates also to a binding unit-drug conjugate, such as an antibody- drug conjugate, of the following formula (III) or (IV) or a salt thereof: (III), (IV), as well as a pharmaceutical composition comprising such a binding unit-drug conjugate and its use in the treatment of cancer.

Amatoxins antibody conjugate

The invention discloses an amatoxins antibody conjugate. The compound of the type is conjugated with a corresponding binding group with a special chemical structure, and the structure is stable in plasma and can be cracked into an active component in a special biological environment, and thus the target cell destruction is maximized, and the toxic, harmful and side effects of non-target cell can be minimized; and the amatoxins antibody conjugate is applicable to treatment of various malignant tumors.

Bifunctional cytotoxic agents

Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

BENZOSELNOPHENE-BASED COMPOUND AND ANTIBODY-DRUG CONJUGATE CONTAINING THE SAME

The present invention relates to a benzoselnophene-based compound, and a preparation method thereof, and antibody-drug conjugate (ADC) containing the benzoselnophene-based compound. The present invention provides the benzoselnophene-based compound or a sa

A water-soluble nucleolin aptamer-paclitaxel conjugate for tumor-specific targeting in ovarian cancer

Paclitaxel (PTX) is among the most commonly used first-line drugs for cancer chemotherapy. However, its poor water solubility and indiscriminate distribution in normal tissues remain clinical challenges. Here we design and synthesize a highly water-solubl

BIFUNCTIONAL CYTOTOXIC AGENTS CONTAINING THE CTI PHARMACOPHORE

The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: [in-line-formulae]F1-L1-T-L2-F2 [/in-line-formulae] where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.