SML3081

AG14361

≥98% (HPLC)

• 동의어(들): 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, AG 14361, AG-14361
• 실험식(Hill 표기법): C₁₉H₂₀N₄O
• CAS Number: 328543-09-5
• Molecular Weight: 320.39
• MDL number: MFCD18385009
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: powder
• 색상: white to beige
• solubility: DMSO: 2 mg/mL, clear (warmed)
• 저장 온도: 2-8°C
• SMILES string: O=C1C2=C3C(N=C(N3CCN1)C4=CC=C(C=C4)CN(C)C)=CC=C2
• InChI: 1S/C19H20N4O/c1-22(2)12-13-6-8-14(9-7-13)18-21-16-5-3-4-15-17(16)23(18)11-10-20-19(15)24/h3-9H,10-12H2,1-2H3,(H,20,24)
• InChI key: SEKJSSBJKFLZIT-UHFFFAOYSA-N

설명

생화학적/생리학적 작용

AG14361 is a potent oly(ADP-ribose) polymerase-1 inhibitor (human PARP-1 Ki = 5.8 nM) that suppresses 25 μM MNNG-induced PARP-1 activity (NAD+ depletion = 70% without vs.12% with 0.4 μM AG14361; 87% reduced ADP-ribose polymer induction with 0.4 μM AG14361) and greatly amplifies temozolomide and topotecan cytotoxicity (2.2- and 2.0-fold lower IG50, respectively, with 0.4 μM AG14361) in A549 cultures. AG14361 is shown to selectively kill BRCA2-deficient cells over BRCA2-expressing cells both in cultures (1-10 μM) and in mice in vivo (25 mg/10 mL/kg/d ip).

Potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor in vitro and in vivo.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable