SML3807

BAY 1816032

≥98% (HPLC)

• 别名: 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
• 经验公式（希尔记法）: C₂₇H₂₄F₂N₆O₄
• CAS号: 1891087-61-8
• 分子量: 534.51
• MDL编号: MFCD31657337
• UNSPSC代码: 12352200
• NACRES: NA.77

属性

• 质量水平: 100
• 方案: ≥98% (HPLC)
• 表单: powder
• 颜色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear (Warmed)
• 储存温度: -10 to -25°C

说明

生化/生理作用

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.

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable