BAY-1816032

Catalog No.S8945 Batch:S894501

Technical Data

Formula

C₂₇H₂₄F₂N₆O₄

Molecular Weight

534.51

CAS No.

1891087-61-8

Solubility (25°C)*

In vitro

DMSO

50 mg/mL (93.54 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.25mg/ml
	5% DMSO 1 95% Corn oil	0.625mg/ml

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

In vivo

In xenograft models of triple-negative breast cancer BAY 1816032 in combination strongly delays outgrowth of tumors under treatment.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	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

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

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

References

[1] Gerhard Siemeister, et al. Clin Cancer Res. 2019 Feb 15;25(4):1404-1414.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.