Tesirine

Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity[1][2].

Product Specifications

CAS Number

[1595275-62-9]

Product Name Alternative

SG3249

UNSPSC

12352203

Target

DNA Alkylator/Crosslinker; Drug-Linker Conjugates for ADC

Type

ADC Related

Related Pathways

Antibody-drug Conjugate/ADC Related; Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mp-peg8-va-pabc.html

Purity

98.31

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=C(COC(N2[C@@H](O)[C@@](CC(C)=C3)([H])N3C(C4=CC(OC)=C(OCCCCCOC5=C(OC)C=C6C(N7[C@](CC(C)=C7)([H])C=NC6=C5)=O)C=C42)=O)=O)C=C1)[C@H](C)NC([C@H](C(C)C)NC(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCN8C(C=CC8=O)=O)=O)=O)=O

Molecular Formula

C75H101N9O23

Molecular Weight

1496.65

References & Citations

[1]Tiberghien AC, et al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016;7 (11) :983-987. Published 2016 May 24. |[2]Hartley JA, et al. Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine. Sci Rep. 2018;8 (1) :10479. Published 2018 Jul 11.