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 
• 67-56-1 methanol 
• 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 
• 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 
• 1415329-11-1 4-((S)-2-((S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3-methylbutanamido)-5-ureidopentanamido)benzyl ((S)-1-(((S)-1-(((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)(methyl)amino)-3-methyl-1-oxobutan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)(methyl)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

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))

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

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.

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

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

FUNCTIONALIZED MORPHOLINYL ANTHRACYCLINE DERIVATIVES

The present invention relates to new functionalized morpholinyl anthracycline derivatives which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds, or the pharmaceutical compositions containing them. The invention also relates to the use of these derivatives in the preparation of conjugates. The morpholinyl anthracycline derivatives are of the formula Ant-L-W-Z-RM (I) wherein RM is null or a reactive moiety; Z is null or a peptidic, non peptidic or hybrid - peptidic and non peptidic - linker; W is null or a self-immolative system, comprising one or more self-immolative groups; L is null or a conditionally-cleavable moiety; Ant is an anthracycline moiety selected from the formulas (II), (III), (IV) and (V), wherein the wavy line indicates the attachment to the conditionally-cleavable moiety L, or to the self-immolative system W, or to the linker Z, or to the reactive moiety RM; provided that at least one of L, W, Z and RM is not null; R1 is halogen or NR4R5; R2 is OR6, NR7R8 or an optionally substituted group selected from straight or branched C1C4alkyl-, NR7R8-C1C4alkyl- and R60-C1C4alkyl-; R4 and R5 are independently hydrogen, a monosubstituted-benzyl, a disubstituted-benzyl, or an optionally substituted group selected from straight or branched C1-C6alkyl, NR7R8-C1-C6alkyl-, R60-C1-C6alkyl-, R7R8N-C1-C6alkylcarbonyl-, R60-C1-C6alkylcarbonyl-, R7R8N-C1-C6alkoxycarbonyl- and R60-C1-C6alkoxycarbonyl-; or R4 and R5, taken together with the nitrogen atom to which they are bound, form a heterocyclyl substituted with R4', wherein R4' is hydrogen or a group selected from straight or branched C1-C6alkyl and NR7R8-C1-C6alkyl-; R15 is null or an optionally substituted bivalent group selected from -NR7-C1-C6alkyl*, -O-C1-C6alkyl*, -NR7-C1-C6alkylcarbonyl*, -O-C1-C6alkylcarbonyl*, -NR7-C1-C6alkoxycarbonyl* and -O-C1-C6alkoxycarbonyl*, wherein * indicates the point of attachment to -NH-Ant; R6, R7 and R8 are independently hydrogen or an optionally substituted straight or branched C1-C6alkyl; or a pharmaceutically acceptable salt thereof.