SML3807

BAY 1816032

≥98% (HPLC)

• Sinonimo/i: 2-(3,5-Difluoro-4-((9-(5-methoxy-4-(3-methoxy-pyridin-4-ylamino)-pyrimidin-2-yl)-7,8-diaza-bicyclo[4.3.0]nona-1,3,5,8-tetraen-7-yl)-methyl)-phenoxy)-ethanol, 2-[3,5-Difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]ethanol, 2-{3,5-Difluoro-4-[(3-{5-methoxy-4-[(3-methoxypyridin-4-yl)amino]pyrimidin-2-yl}-1H-indazol-1-yl)methyl]phenoxy}ethanol, BAY-1816032, BAY1816032
• Formula empirica (notazione di Hill): C₂₇H₂₄F₂N₆O₄
• Numero CAS: 1891087-61-8
• Peso molecolare: 534.51
• Numero MDL: MFCD31657337
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear (Warmed)
• Temperatura di conservazione: -10 to -25°C

Descrizione

Azioni biochim/fisiol

BAY 1816032 is an orally active, ATP-competitive (Ki = 1.2 μM), highly potent and selective BUB1 inhibitor (IC50 = 6.1 nM with 10 μM ATP; affinity Kd = 3.3 nM/BUB1 vs 57 nM/STK10, 850 nM/DMPK2, 2.3 μM/DDR1 and >2.3 μM toward more than 390 other kinases) that effectively targets BUB1-dependent cellular signaling (H2A-pThr120 IC50 = 29 nM post 1h treatment of nocodazole-arrested HeLa cells) and tumor cell proliferation in vitro (IC50 range from 0.5 to 5.8 μM in 43 human and mouse cancer cultures) and in human triple-negative breast xenograft models in vivo (25-50 mg/kg twice daily p.o.; SUM-149 and MDA-MB-436).

Orally active, ATP-competitive, highly potent and selective BUB1 inhibitor with anti-proliferation efficacy against cancer cells in cultures and in vivo.

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable