SG3199 - ≥98% , CAS No.1595275-71-0

CAS: 1595275-71-0 Cat. No.: S648315 분자식: C₃₃H₃₆N₄O₆ 분자량: 584.66 PubChem CID: 129203820

GRADE & PURITY ≥98%

Storage

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

Shipped In

Ice chest + Ice pads

개요

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

Specifications

사양 및 순도

≥98%

생화학 및 생리적 메커니즘

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

보관 조건

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

배송

Ice chest + Ice pads

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순수함

≥98%

이름과 식별자

• 정식 스마일: 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
• 분자량: 584.66

화학 및 물리적 특성

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