Payload · Maytansinoid

Maytansinoid (DM4-class maytansine derivative; warhead SC236)

Tubulin polymerization inhibition / microtubule disruption -> mitotic arrest -> apoptosis

CNC(=O)CCCC(=O)N(C)C(C)C(=O)OC1CC(=O)N(C)c2cc(cc(OC)c2Cl)C/C(C)=C\C=C/C(OC)C2(O)CC(OC(=O)N2)C(C)C2OC12C

Physicochemistry

Properties

794.4 Da

XLogP3

3.6

logD₇.₄

TPSA

157 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Partial

PubChem CID

Bioactivity

STRO-001 in vitro cytotoxicity (EC50) on CD74+ multiple myeloma lines: MC/CAR 0.84 nM (90% kill), U266B1 8.8 nM (83%), MM.1S 12 nM (85%), ARP-1 23 nM (88%); ARD and OPM-2 not killed. Unconjugated SP7219 antibody non-cytotoxic. Released catabolites SC246 (major) and SC401 (minor)

1 agent

ADCs built on this payload

Agent · target

Ocular

Hepatic

Neutrop.

Thrombo.

Anemia

ILD

Neuro.

STRO-001CD74

0%severity100%

Assessed · clear

true 0%

No data

never assessed