[CAS NO. 1595275-71-0] SG3199
PRODUCTS SPECIFICATIONS [1595275-71-0]
DESCRIPTION [1595275-71-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 584.66 |
| Molecular Formula | C33H36N4O6 |
| SMILES | O=C1N2[C@](CC(C)=C2)([H])C=NC3=CC(OCCCCCOC4=C(OC)C=C5C(N6[C@](CC(C)=C6)([H])C=NC5=C4)=O)=C(OC)C=C13 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
Pyrrolobenzodiazepines |
In Vitro
SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines with a mean GI
50
of 151.5 pM. Cells defective in DNA repair protein ERCC1 or homologous recombination repair show increased sensitivity to SG3199 and the drug is only moderately susceptible to multidrug resistance mechanisms
[1]
.
SG3199 is highly efficient at producing DNA interstrand cross-links in naked linear plasmid DNA and dose-dependent cross-linking is observed in cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The in vitro binding of [
3
H]-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 T
1/2
between 8 and 42 minutes
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 130 mg/mL ( 222.35 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7104 mL | 8.5520 mL | 17.1040 mL |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4208 mL |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7104 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 3.25 mg/mL (5.56 mM); Clear solution
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.
- [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.
