Tesirine

Modify Date: 2024-01-01 19:50:56

Tesirine Structure
Tesirine structure
Common Name Tesirine
CAS Number 1595275-62-9 Molecular Weight 1496.651
Density 1.3±0.1 g/cm3 Boiling Point 1428.0±65.0 °C at 760 mmHg
Molecular Formula C75H101N9O23 Melting Point N/A
MSDS N/A Flash Point 817.4±34.3 °C

 Use of Tesirine


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.

 Names

Name N-[31-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-29-oxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacontan-1-oyl]-L-valyl-N-{4-[({[(11S,11aS)-11-hydroxy-7-methoxy-8-[(5-{[(11aS)-7-methoxy-2-methyl-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy}pentyl)oxy]-2-methyl-5-oxo-11,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl}oxy)methyl]phenyl}-L-alaninamide
Synonym More Synonyms

 Tesirine Biological Activity

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.
References 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. View Related Products by Target Drug-Linker Conjugates

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 1428.0±65.0 °C at 760 mmHg
Molecular Formula C75H101N9O23
Molecular Weight 1496.651
Flash Point 817.4±34.3 °C
Exact Mass 1495.701050
LogP -0.60
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.601

 Synonyms

N-[31-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)-29-oxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacontan-1-oyl]-L-valyl-N-{4-[({[(11S,11aS)-11-hydroxy-7-methoxy-8-[(5-{[(11aS)-7-methoxy-2-methyl-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy}pentyl)oxy]-2-methyl-5-oxo-11,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl}oxy)methyl]phenyl}-L-alaninamide
L-Alaninamide, N-[31-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1,29-dioxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacont-1-yl]-L-valyl-N-[4-[[[[(11S,11aS)-8-[[5-[[(11aS)-5,11a-dihydro-7-methoxy-2-methyl-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy]pentyl]oxy]-11,11a-dihydro-11-hydroxy-7-methoxy-2-methyl-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-10(5H)-yl]carbonyl]oxy]methyl]phenyl]-