1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. DNA Alkylator/Crosslinker
    ADC Cytotoxin
  3. SG3199

SG3199 

Cat. No.: HY-101161
Handling Instructions

SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PDB) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).

For research use only. We do not sell to patients.

SG3199 Chemical Structure

SG3199 Chemical Structure

CAS No. : 1595275-71-0

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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)[1][2].

IC50 & Target[1]

Pyrrolobenzodiazepines

 

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[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 [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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

584.66

Formula

C₃₃H₃₆N₄O₆

CAS No.
SMILES

O=C1N2[[email protected]](CC(C)=C2)([H])C=NC3=CC(OCCCCCOC4=C(OC)C=C5C(N6[[email protected]](CC(C)=C6)([H])C=NC5=C4)=O)=C(OC)C=C13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SG3199SG 3199SG-3199DNA Alkylator/CrosslinkerADC CytotoxincytotoxicitypyrrolobenzodiazepinePBDdimerDNAcross-linkingADCInhibitorinhibitorinhibit

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SG3199
Cat. No.:
HY-101161
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