BAY-1816032 - 98%, high purity , CAS No.1891087-61-8

Item Number

B414286

• Synonyms: 2-[3,5-bis(fluoranyl)-4-[[3-[5-methoxy-4-[(3-methoxypyridin-4-yl)amino]pyrimidin-2-yl]indazol-1-yl]methyl]phenoxy]ethanol
• Specifications & Purity: ≥98%
• Biochemical and Physiological Mechanisms: BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads

Product Description

Information

BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity.

Targets

BUB1 (Cell-free assay) 6.1 nM

In vitro

BAY 1816032 is a novel, bioavailable inhibitor of the catalytical activity of the mitotic checkpoint protein BUB1, which is involved in centromere cohesion and attachment error correction. Inhibition of BUB1 sensitizes tumor cells towards paclitaxel and docetaxel, and towards ATR inhibitors and PARP inhibitiors.

In vivo

In xenograft models of triple-negative breast cancer BAY 1816032 in combination with paclitaxel or olaparib strongly delays outgrowth of tumors under treatment as compared to paclitaxel or olaparib single agents.

Cell Research(from reference)

Cell lines：HeLa, SUM-149, MDA-MB-436, NCI-H1299, 22RV1, H4 cells. 

Concentrations：0.1 μM to 10 μM 

Incubation Time：4 h, 24 h, 48 h, 72 h, 96 h