BAY-1816032
- Product Name
- BAY-1816032
- CAS No.
- 1891087-61-8
- Chemical Name
- BAY-1816032
- Synonyms
- BAY-1816032;BAY-1816032 (BAY1816032);BAY-1816032, 10 mM in DMSO;inhibit,BAY1816032,Inhibitor,BAY 1816032,BAY-1816032;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)ethan-1-ol;Ethanol, 2-[3,5-difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]-
- CBNumber
- CB23364608
- Molecular Formula
- C27H24F2N6O4
- Formula Weight
- 534.51
- MOL File
- 1891087-61-8.mol
BAY-1816032 Property
- Boiling point:
- 640.8±55.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:37.5(Max Conc. mg/mL);70.16(Max Conc. mM)
- form
- A solid
- pka
- 14.05±0.10(Predicted)
- color
- Off-white to yellow
N-Bromosuccinimide Price
- Product number
- DC20751
- Product name
- BAY-1816032
- Purity
- >98%
- Packaging
- 100mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- DC20751
- Product name
- BAY-1816032
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- DC20751
- Product name
- BAY-1816032
- Purity
- >98%
- Packaging
- 1g
- Price
- $2700
- Updated
- 2021/12/16
BAY-1816032 Chemical Properties,Usage,Production
Uses
BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM.
Biological Activity
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) th at 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).
in vivo
In tumor xenograft studies BAY 1816032 only marginally inhibits tumor growth as single agent upon oral administration, however, upon combination with paclitaxel or docetaxel a strong and statistically significant reduction of tumor size as compared to the respective monotherapy is observed[1].
storage
Store at -20°C
References
[1] Siemeister G, et al. BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Ishington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 287. doi:10.1158/1538-7445.AM2017-287
BAY-1816032 Preparation Products And Raw materials
Raw materials
Preparation Products
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