BAY-1816032

SKU: orb1309944

Description

BAY-1816032 is a potent, orally active BUB1 kinase inhibitor with an IC50 of 0.7 nM. It effectively blocks BUB1-mediated histone H2A phosphorylation in cellular assays and is a valuable chemical probe for investigating mitosis, chromosomal instability, and cancer biology in both in vitro and in vivo research models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 1891087-61-8
• MW: 534.51
• Purity: 99.81% (May vary between batches)
• Formula: C₂₇H₂₄F₂N₆O₄
• SMILES: COc1cnccc1Nc1nc(ncc1OC)-c1nn(Cc2c(F)cc(OCCO)cc2F)c2ccccc12
• Target: Serine/threonin kinase,Others
• Solubility: H2O:< 0.1 mg/mL (insoluble);DMSO:15 mg/mL (28.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.74 mM)

Bioactivity

• Target IC50:
  BUB1 kinase:7 nM
• In Vivo:
  METHODS: BAY-1816032 (100 mg/kg, oral, 24 days) was used to treat 8505C xenograft model mice to evaluate the anti-ATC activity and safety of BAY-1816032 in mice. RESULTS There was no significant difference in the body weight of each group of mice; the tumor weight of mice treated with BAY-1816032 was significantly reduced.
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• In Vitro:
  METHODS: BAY-1816032 (0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM, 48 hours) treated ATC cells (TPC-1, 8505C), and CCK-8 assay was used to study cell viability. RESULTS BAY-1816032 treatment resulted in a decrease in ATC cell viability, with IC50 values ​​of 4.230 μM in TPC-1 cells and 6.216 μM in 8505C cells. METHODS: Colony formation assay, cell cycle, invasion, migration and wound healing assay were performed after ATC cells were treated with BAY-1816032 (0, 2.5, 5 μM). RESULTS BAY-1816032 can significantly reduce colony formation ability; BAY-1816032 can cause cell cycle arrest similar to siRNA; BAY-1816032 treatment can significantly hinder the invasion and migration of ATC cells in a dose-dependent manner.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BUB1, BUB1 kinase, BAY 1816032, BAY1816032, BAY-1816032, inhibit, Inhibitor

Compound Identifiers

PubChem CID

118958833