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Tesirine

CAS No. 1595275-62-9

Tesirine( SG3249 | SG-3249 )

Catalog No. M12277 CAS No. 1595275-62-9

Tesirine ( SG3249) is a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine (PBD) dimer as antibody-drug conjugate (ADC) payload.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Tesirine
  • Note
    Research use only, not for human use.
  • Brief Description
    Tesirine ( SG3249) is a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine (PBD) dimer as antibody-drug conjugate (ADC) payload.
  • 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.
  • 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.
  • In Vivo
    ——
  • Synonyms
    SG3249 | SG-3249
  • Pathway
    Antibody Drug Conjugates (ADC)
  • Target
    Drug-Linker Conjugates
  • Recptor
    Drug-Linker Conjugates
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1595275-62-9
  • Formula Weight
    1496.673
  • Molecular Formula
    C75H101N9O23
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 200 mg/mL (133.63 mM)
  • 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
  • Chemical Name
    4-((S)-N-((S)-1-amino-1-oxopropan-2-yl)-34-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-2-isopropyl-4,32-dioxo-7,10,13,16,19,22,25,28-octaoxa-3,31-diazatetratriacontanamido)benzyl (11S,11aS)-11-hydroxy-7-methoxy-8-((5-(((S)-7-methoxy-2-methyl-5-oxo-5,11a-dihydr

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Tiberghien AC, et al. ACS Med Chem Lett. 2016 May 24;7(11):983-987. 2. Cancer Discov. 2015 Dec;5(12):OF4. doi: 10.1158/2159-8290.CD-NB2015-144. 3. Rudin CM, et al. Lancet Oncol. 2017 Jan;18(1):42-51.
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