SG3199 - ≥98% , CAS No.1595275-71-0

CAS: 1595275-71-0 Cat. No.: S648315 Formule: C₃₃H₃₆N₄O₆ Poids moléculaire: 584.66 PubChem CID: 129203820

QUALITÉ & PURETÉ ≥98%

Storage

Protected from light,Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

Vue d’ensemble

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

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. ?\nSG3199 is highly efficient at producing DNA interstrand cross-links in naked linear plasmid DNA and dose-dependent cross-linking is observed in cells. 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% . ?\nFollowing 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:Pyrrolobenzodiazepines

Spécifications

Spécifications et pureté

≥98%

Mécanismes biochimiques et physiologiques

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

Conditions de stockage de stockage

Protected from light,Store at -20°C,Argon charged

Expédié en

Ice chest + Ice pads

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Pureté

≥98%

Noms et identifiants

Sourires canoniques

CC1=CN2C(C1)C=NC3=CC(=C(C=C3C2=O)OC)OCCCCCOC4=C(C=C5C(=C4)N=CC6CC(=CN6C5=O)C)OC

IUPAC Name

3-[5-[[(6aR)-2-methoxy-8-methyl-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]pentoxy]-2-methoxy-8-methyl-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one

InChIKey

YMTZZJOPSATRTO-WTQRLHSKSA-N

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?/m1/s1

PubChem CID

129203820

Poids moléculaire

584.66

Propriétés chimiques et physiques

• Solubilité: DMSO : 130 mg/mL (222.35 mM; Need ultrasonic)