Description
SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PDB) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).
Product information
CAS Number: 1595275-71-0
Molecular Weight: 584.66
Formula: C33H36N4O6
Chemical Name: (7S)-13-methoxy-12-[(5-{[(7S)-13-methoxy-5-methyl-2-oxo-3,9-diazatricyclo[8.4.0.0³,⁷]tetradeca-1(14),4,8,10,12-pentaen-12-yl]oxy}pentyl)oxy]-5-methyl-3,9-diazatricyclo[8.4.0.0³,⁷]tetradeca-1(10),4,8,11,13-pentaen-2-one
Smiles: CC1C[C@H]2C=NC3C=C(OCCCCCOC4C=C5N=C[C@@H]6CC(C)=CN6C(=O)C5=CC=4OC)C(=CC=3C(=O)N2C=1)OC
InChiKey: YMTZZJOPSATRTO-GOTSBHOMSA-N
InChi: InChI=1S/C33H36N4O6/c1-20-10-22-16-34-26-14-30(28(40-3)12-24(26)32(38)36(22)18-20)42-8-6-5-7-9-43-31-15-27-25(13-29(31)41-4)33(39)37-19-21(2)11-23(37)17-35-27/h12-19,22-23H,5-11H2,1-4H3/t22-,23-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SG3199 was potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines with a mean GI50 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. SG3199 is highly efficient at producing DNA interstrand cross-links in naked linear plasmid DNA and dose-dependent cross-linking is observed in cells.
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%. 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.
Products are for research use only. Not for human use.
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