BAY-1816032
BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM. BAY 1816032 showed long target residence time and induced chromosome mis-segregation upon combination with low concentrations of paclitaxel. It was synergistic or additive in combination with paclitaxel or docetaxel, as well as with ATR or PARP inhibitors in cellular assays. Tumor xenograft studies demonstrated a strong and statistically significant reduction of tumor size and excellent tolerability upon combination of BAY 1816032 with paclitaxel or olaparib as compared with the respective monotherapies.
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Chemical Information
| Name | BAY-1816032 |
|---|---|
| Iupac Chemical Name | 2-(3,5-difluoro-4-((3-(5-methoxy-4-((3-methoxypyridin-4-yl)amino)pyrimidin-2-yl)-1H-indazol-1-yl)methyl)phenoxy)ethan-1-ol |
| Synonyms | BAY-1816032; BAY 1816032; BAY1816032 |
| Molecular Formula | C27H24F2N6O4 |
| Molecular Weight | 534.5238 |
| Smile | COC1=C(NC2=NC(C3=NN(CC4=C(F)C=C(OCCO)C=C4F)C5=C3C=CC=C5)=NC=C2OC)C=CN=C1 |
| InChiKey | QVOGVAVHOLLLAZ-UHFFFAOYSA-N |
| 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) |
| CAS Number | 1891087-61-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | 固体粉末 |
|---|---|
| Purity | 98% Min. |
| Storage | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| Solubility | 可溶于DMSO |
| Handling | |
| Shipping Condition | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Siemeister G, Mengel A, Fernández-Montalván AE, et al. Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo. Clin Cancer Res. 2019;25(4):1404–1414. doi:10.1158/1078-0432.CCR-18-0628
Chemical Structure
