Mc-Val-Ala-PAB-PNP Chemical Properties

Boiling point:

946.4±65.0 °C(Predicted)

Density 

1.323±0.06 g/cm3(Predicted)

pka

13.31±0.70(Predicted)

form 

Solid

color 

White to off-white

InChIKey

VMOQJVBAOUFRSX-LGGPFLRQSA-N

SMILES

C(N)(=O)[C@H](C)N(C(=O)[C@H](C(C)C)NC(=O)CCCCCN1C(=O)C=CC1=O)C1=CC=C(COC(OC2=CC=C([N+]([O-])=O)C=C2)=O)C=C1

Mc-Val-Ala-PAB-PNP Usage And Synthesis

Uses

Mc-Val-Ala-PAB-PNP is a cleavable ADC linker for the synthesis of antibody-drug conjugates (ADCs). Cryptophycin-55 (CR55) can be conjugated to the model antibody trastuzumab (an anti-HER2 antibody drug approved by the FDA for the treatment of breast cancer) through the linker of Mc-NHS and Mc-Val-Cit-PAB-PNP to prepare trastuzumab-CR55 conjugates. These conjugates exhibit potent cytotoxicity in HER2-positive tumor cell lines, with IC50 values at low nanomolar levels (0.58-1.19 nM)^[1].

Biological Activity

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

in vitro

target

References

[1] QINHUAI LAI . Cryptophycin-55/52 based antibody-drug conjugates: Synthesis, efficacy, and mode of action studies[J]. European Journal of Medicinal Chemistry, 2020. DOI:10.1016/j.ejmech.2020.112364.