BAY-1816032
Axon 3832
CAS:
1891087-61-8
Purity:
99%
- Soluble in DMSO
- MF: C27H24F2N6O4
- MW: 534.51
Description
BAY-1816032 is an orally available, highly potent and selective BUB1 (Mitotic checkpoint serine/threonine-protein kinase) inhibitor, with an enzymatic IC50 of 7 nM, and highly selective against other 395 kinases. Mechanistically BAY 1816032 abrogated nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with an IC50 of 29 nM, induced lagging chromosomes and mitotic delay. Demonstrated in vitro and in vivo antitumor efficacy when applied in combination with taxanes.
More Information
| Parent CAS No. | 1891087-61-8 |
|---|---|
| Chemical Name | 2-(3,5-Difluoro-4-((3-(5-methoxy-4-(3-methoxypyridin-4-ylamino)pyrimidin-2-yl)-1H-indazol-1-yl)methyl)phenoxy)ethanol |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=C2N(CC3C(F)=CC(OCCO)=CC=3F)N=C(C3N=C(NC4C=CN=CC=4OC)C(OC)=CN=3)C2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C27H24F2N6O4/c1-37-23-13-30-8-7-21(23)32-26-24(38-2)14-31-27(33-26)25-17-5-3-4-6-22(17)35(34-25)15-18-19(28)11-16(12-20(18)29)39-10-9-36/h3-8,11-14,36H,9-10,15H2,1-2H3,(H,30,31,32,33) |
| InChiKey | QVOGVAVHOLLLAZ-UHFFFAOYSA-N |
| CID | 118958833 |
| Short Description | BUB1 inhibitor |
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