Auristatin S TFA is a potent Auristatin payload. Auristatin S TFA binds to the vinca-binding site on tubulin, thereby inhibiting microtubule assembly and inducing cell cycle arrest and apoptosis. Auristatin S TFA acts as a cytotoxic component of antibody-drug conjugates (ADCs) and exerts target-specific cytotoxicity against cancer cells. Auristatin S TFA can be used in the research of lymphoma, anaplastic large cell lymphoma and Hodgkin lymphoma [1].
In Vitro, Auristatin S (1.4 μM; 1 h) TFA competes with FITC-MMAE for binding to tubulin in a cell-free system[1]. Auristatin S TFA has a LogD value of 1.6, exhibiting lower hydrophobicity and cell permeability compared with MMAE[1]. Auristatin S (96 h) TFA exerts in vitro cytotoxic effects in lymphoma cell lines (DEL, Karpas299, KarpasBVR, L540cy, etc.), with a mean IC50 value of 20 nM[1]. Auristatin S (100 nM; 18-72 h) TFA induces markers of immunogenic cell death (HMGB1 release and ATP release) in MiaPaCa and L540cy cells[1].
References:
[1]. Moquist PN, et al. Auristatin S: An Auristatin Payload with Improved Tolerability and Modified Bystander Activity. ACS medicinal chemistry letters. 2025 Jul 10;16(7):1354-1358.
In Vitro, Auristatin S (1.4 μM; 1 h) TFA competes with FITC-MMAE for binding to tubulin in a cell-free system[1]. Auristatin S TFA has a LogD value of 1.6, exhibiting lower hydrophobicity and cell permeability compared with MMAE[1]. Auristatin S (96 h) TFA exerts in vitro cytotoxic effects in lymphoma cell lines (DEL, Karpas299, KarpasBVR, L540cy, etc.), with a mean IC50 value of 20 nM[1]. Auristatin S (100 nM; 18-72 h) TFA induces markers of immunogenic cell death (HMGB1 release and ATP release) in MiaPaCa and L540cy cells[1].
References:
[1]. Moquist PN, et al. Auristatin S: An Auristatin Payload with Improved Tolerability and Modified Bystander Activity. ACS medicinal chemistry letters. 2025 Jul 10;16(7):1354-1358.