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Merck
CN

SML3807

BAY 1816032

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C27H24F2N6O4
CAS Number:
1891087-61-8
Molecular Weight:
534.51
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD31657337

Key Documents

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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Quality Level

100

Related Categories

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000277522
0000277521
0000268297
0000268297
0000277521

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Inhibition of BUB1 suppresses tumorigenesis of osteosarcoma via blocking of PI3K/Akt and ERK pathways
Journal of Cellular and Molecular Medicine, 25(17), 8442-8453 (2021)
Biallelic BUB1 mutations cause microcephaly, developmental delay, and variable effects on cohesion and chromosome segregation.
Science Advances, 8(3), eabk0114-eabk0114 (2022)
Mapping Proximity Associations of Core Spindle Assembly Checkpoint Proteins.
Journal of Proteome Research, 20(7), 3414-3427 (2021)
Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo
Clinical Cancer Research, 25(4), 1404-1414 (2019)
Miao Zhang et al.
The EMBO journal, 39(3), e101863-e101863 (2019-11-27)
Chromosome segregation in mitosis requires the removal of catenation between sister chromatids. Timely decatenation of sister DNAs at mitotic centromeres by topoisomerase IIα (TOP2A) is crucial to maintain genomic stability. The chromatin factors that recruit TOP2A to centromeres during mitosis

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