Payload · Auristatin

Aur0101 (auristatin 0101; PF-06380101)

Microtubule / tubulin-polymerization inhibitor (antimitotic)

CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@@H](CC2=CC=CC=C2)C3=NC=CS3)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)C(C)(C)N

Physicochemistry

Properties

743 Da

XLogP3

4.1

logD₇.₄

TPSA

184 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

PubChem CID

71569947

Bioactivity

Free payload Aur0101 (PF-06380101) is a Dolastatin 10 analogue / auristatin microtubule (tubulin polymerization) inhibitor; ADCdb reports payload IC50 0.8 nM in HT-29 colon adenocarcinoma cells. Membrane-permeable, giving bystander killing of NOTCH3-negative neighboring cells. PF

3 agents