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Tesirine

Chemical Structure : Tesirine

CAS No.: 1595275-62-9

Tesirine ( SG3249;SG-3249)

Catalog No.: PC-35368Not For Human Use, Lab Use Only.

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

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Biological Activity

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.

Physicochemical Properties

M.Wt 1496.673
Formula C75H101N9O23
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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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