SG3199
- Product Name
- SG3199
- CAS No.
- 1595275-71-0
- Chemical Name
- SG3199
- Synonyms
- SG3199;PBD (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)-;(7S)-13-methoxy-12-[(5-{[(7S)-13-methoxy-5-methyl-2-oxo-3,9-diazatricyclo[8.4.0.03,?]tetradeca-1(10),4,8,11,13-pentaen-12-yl]oxy}pentyl)oxy]-5-methyl-3,9-diazatricyclo[8.4.0.03,?]tetradeca-1(14),4,8,10,12-pentaen-2-one
- CBNumber
- CB34668504
- Molecular Formula
- C33H36N4O6
- Formula Weight
- 584.66
- MOL File
- 1595275-71-0.mol
SG3199 Property
- 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
- pka
- 3.89±0.40(Predicted)
- form
- Solid
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
SG3199 Chemical Properties,Usage,Production
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
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
SG3199 Preparation Products And Raw materials
Raw materials
Preparation Products
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