Payload · Calicheamicin

Calicheamicin gamma1

DNA strand break

CCN[C@H]1CO[C@H](C[C@@H]1OC)O[C@@H]2[C@H]([C@@H]([C@H](O[C@H]2O[C@H]3C#C/C=C\\C#C[C@@]\\4(CC(=O)C(=C3/C4=C\\CSSSC)NC(=O)OC)O)C)NO[C@H]5C[C@@H]([C@@H]([C@H](O5)C)SC(=O)C6=C(C(=C(C(=C6OC)OC)O[C@H]7[C@@H]([C@@H]([C@H]([C@@H](O7)C)O)OC)O)I)C)O)O

Physicochemistry

Properties

1368.4 Da

XLogP3

logD₇.₄

TPSA

410 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Partial

PubChem CID

10953353

Bioactivity

ADCdb (DRG0JOHND) reports payload/ADC potency against CD33+ cells with most potent IC50 ~20 pM (ML-2) and ~30 pM (MOLM-13, EoL-1); clinical objective response rate ~85% in CD33+ AML. Calicheamicin warhead induces sequence-selective double-strand DNA breaks (ADCdb lists the mechan

3 agents

ADCs built on this payload

Agent · target

Ocular

Hepatic

Neutrop.

Thrombo.

Anemia

ILD

Neuro.

PF-06647263EFNA4

Gemtuzumab ozogamicinCD33

Inotuzumab ozogamicinCD22

0%severity100%

Assessed · clear

true 0%

No data

never assessed