Payload · Tubulysin

Tubulysin (proprietary tubulysin analog)

Microtubule destabilizer; inhibits tubulin polymerization (binds vinca domain of beta-tubulin)

CC[C@H](C)[C@@H](C(=O)N(COC(=O)CC(C)C)[C@H](C[C@H](C1=NC(=CS1)C(=O)N[C@@H](CC2=CC=C(C=C2)C)C[C@H](C)C(=O)O)OC(=O)C)C(C)C)NC(=O)[C@H]3CCCCN3C

Physicochemistry

Properties

842.1 Da

XLogP3

5.4

logD₇.₄

TPSA

213 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Yes

PubChem CID

52945681

Bioactivity

ADCdb payload page (PAY0PCTOE / PubChem CID 52945681, tubulysin) reports cytotoxicity IC50 2.2 nM (A2780 ovarian) and 2.5 nM (LNCaP prostate); mechanism is inhibition of tubulin polymerization into microtubules. Clinically, BMS-986148 MTD was 1.2 mg/kg IV q3w with ORR ~2-23% acro

1 agent

ADCs built on this payload

Agent · target

Ocular

Hepatic

Neutrop.

Thrombo.

Anemia

ILD

Neuro.

BMS-986148MSLN

0%severity100%

Assessed · clear

true 0%

No data

never assessed