Home Metabolism Serine/threonin kinase inhibitor BAY-1816032 For research use only.

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.

BAY-1816032 Chemical Structure

BAY-1816032 Chemical Structure

CAS: 1891087-61-8

Purity & Quality Control

Batch: S894501 DMSO] 50 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.43%
99.43

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Choose Selective Serine/threonin kinase Inhibitors

Biological Activity

Description 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 [1]
(Cell-free assay)
6.1 nM
In vitro
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 towards ATR inhibitors and PARP inhibitiors.[1]
Cell Research 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
Method

Cells are plated into 384-well plates at densities between 600 and 800 cells per well. After 24 h, cells are treated with BAY 1816032 and the second compound either as single compound treatments, or in nine fixed compound ratios. Cell viability is assessed after 96 hour exposure, using the CellTiter-Glo Luminescent Cell Viability Assay.
In Vivo
In vivo

In xenograft models of triple-negative breast cancer BAY 1816032 in combination with olaparib strongly delays outgrowth of tumors under treatment as compared to olaparib single agents.[1]
Animal Research Animal Models male Wistar rats, female CD1 mice, female Beagle dog
Dosages 1.0 mg/kg, 0.5 mg/kg, 5 mg/kg, 10 mg/kg, 25 mg/kg, 40 mg/kg, 50 mg/kg, 100 mg/kg
Administration Oral gavage, IV

Chemical Information & Solubility

Molecular Weight 534.51 Formula

C27H24F2N6O4
CAS No. 1891087-61-8 SDF --
Smiles COC1=CN=C(N=C1NC2=C(C=NC=C2)OC)C3=NN(C4=CC=CC=C43)CC5=C(C=C(C=C5F)OCCO)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 50 mg/mL ( (93.54 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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