Payload · Auristatin

Auristatin F-hydroxypropylamide (AF-HPA; ledadotin; DolaLock/Dolasynthen payload)

Microtubule polymerization inhibitor; AF-HPA is membrane-permeable and is intracellularly converted to the membrane-impermeable active catabolite auristatin F (controlled bystander effect)

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)C(=O)NCCCO)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)N(C)C

Physicochemistry

Properties

803.1 Da

XLogP3

4.3

logD₇.₄

TPSA

170 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Partial

PubChem CID

71135741

1 agent

ADCs built on this payload

Agent · target

Ocular

Hepatic

Neutrop.

Thrombo.

Anemia

ILD

Neuro.

XMT-1660 (Emiltatug ledadotin)VTCN1

0%severity100%

Assessed · clear

true 0%

No data

never assessed