| Identification | Back Directory | [Name]
SG3199 | [CAS]
1595275-71-0 | [Synonyms]
SG3199
SG3199 SG-3199
5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one, 8,8'-[1,5-pentanediylbis(oxy)]bis[1,11a-dihydro-7-methoxy-2-methyl-, (11aS,11'aS)- | [Molecular Formula]
C33H36N4O6 | [MDL Number]
MFCD34469130 | [MOL File]
1595275-71-0.mol | [Molecular Weight]
584.66 |
| Chemical Properties | Back Directory | [Boiling point ]
816.2±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [form ]
Solid | [pka]
3.89±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249)[1][2]. | [in vivo]
The in vitro binding of [3H]-SG3199 to the plasma proteins of rat (Sprague Dawley), cynomolgus monkey and human at concentrations of 0.8, 5 and 50 ng/mL is determined. Plasma protein binding is high in all species; rat ～97%, cynomolgus monkey ～90% and human ～95%[1].
Following i.v. administration at 0.1 μg/kg, 0.5 μg/kg and 1 μg/kg, SG3199 shows a very rapid clearance in rats. In the 0.5 μg/kg and 1 μg/kg dose groups, the rapid clearance was between 1000 and 1500 mL/h/kg, with a T1/2 between 8 and 42 minutes[1]. | [IC 50]
Pyrrolobenzodiazepines | [storage]
Store at -20°C, protect from light, stored under nitrogen | [References]
[1] John A Hartley, 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 Jul 11;8(1):10479. DOI:10.1038/s41598-018-28533-4
[2] Francesca Zammarchi, et al. ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood. 2018 Mar 8;131(10):1094-1105. DOI:10.1182/blood-2017-10-813493 |
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