Boc-Val-Cit-PAB-PNP Chemical Properties

Boiling point:

896.0±65.0 °C(Predicted)

Density 

1.291±0.06 g/cm3(Predicted)

storage temp. 

-20°C, stored under nitrogen, away from moisture

solubility 

DMSO : 250 mg/mL (387.80 mM; Need ultrasonic)

pka

11.25±0.46(Predicted)

form 

Solid

color 

White to off-white

InChIKey

PJCUTAUEMJZDQD-ZEQRLZLVSA-N

SMILES

C(N)(=O)[C@H](CCCNC(N)=O)N(C(=O)[C@H](C(C)C)NC(OC(C)(C)C)=O)C1=CC=C(COC(OC2=CC=C([N+]([O-])=O)C=C2)=O)C=C1

Boc-Val-Cit-PAB-PNP Usage And Synthesis

Description

Boc-Val-Cit-PAB-PNB is a cleavable peptide ADC linker. The Val-Cit will specifically be cleaved by Cathepsin B. As this enzyme is only present in the lysosome, the ADC payload will be released only in the cell.PNP can be substituted by amine bearing molecules.

Uses

Boc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

IC 50

Protease Cleavable Linker; Cleavable Linker

References

[1] Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337. DOI:10.1038/nrd.2016.268