Tesirine

SKU: orb2655870

Description

Tesirine ( SG3249) is a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine (PBD) dimer as antibody-drug conjugate (ADC) payload; Tesirine (SG3249) was designed to combine potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics; Rovalpituzumab tesirine is a first-in-class antibody-drug conjugate directed against delta-like protein 3 (DLL3), a novel target identified in tumour-initiating cells and expressed in small-cell lung cancer.

Key Properties

• CAS Number: 1595275-62-9
• MW: 1496.673
• Purity: >98% (HPLC)
• Formula: C₇₅H₁₀₁N₉O₂₃
• SMILES: CC1=CN2C(C1)C=NC3=CC(=C(C=C3C2=O)OC)OCCCCCOC4=C(C=C5C(=C4)N(C(C6CC(=CN6C5=O)C)O)C(=O)OCC7=CC=C(C=C7)NC(=O)C(C)NC(=O)C(C(C)C)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCN8C(=O)C=CC8=O)OC
• Target: Drug-Linker Conjugates
• Solubility: In Vitro: DMSO : 200 mg/mL (133.63 mM)

Bioactivity

• In Vitro:
  Tesirine (SG3199) is the released warhead component of the ADC payload Tesirine. Tesirine inhibits K562, NCIN87, BT474, and SKBR3 cancer cells with IC50s of 150 pM, 20 pM, 1 nM and 320 pM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SG3249 | SG-3249

Quick Database Links

Gene Symbol

Drug-Linker Conjugates