Tesirine

• Product Name Alternative:

  SG3249

• UNSPSC Description:

  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].

• Target Antigen:

  DNA Alkylator/Crosslinker; Drug-Linker Conjugates for ADC

• Type:

  ADC Related

• Related Pathways:

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

• Field of Research:

  Cancer

• Assay Protocol:

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

• Purity:

  98.10

• 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 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, protect from light, stored under nitrogen)

• Clinical Information:

  Phase 3

• CAS Number:

  1595275-62-9