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BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $32 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $128 | In Stock | In Stock | |
| 25 mg | $255 | In Stock | In Stock | |
| 50 mg | $377 | In Stock | In Stock | |
| 100 mg | $538 | In Stock | In Stock | |
| 200 mg | $738 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $92 | In Stock | In Stock |
| Description | BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM. |
| Targets&IC50 | BUB1 kinase:7 nM |
| In vitro | METHODS: BAY-1816032 (0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM, 48 hours) treated ATC cells (TPC-1, 8505C), and CCK-8 assay was used to study cell viability. RESULTS BAY-1816032 treatment resulted in a decrease in ATC cell viability, with IC50 values of 4.230 μM in TPC-1 cells and 6.216 μM in 8505C cells. [2] METHODS: Colony formation assay, cell cycle, invasion, migration and wound healing assay were performed after ATC cells were treated with BAY-1816032 (0, 2.5, 5 μM). RESULTS BAY-1816032 can significantly reduce colony formation ability; BAY-1816032 can cause cell cycle arrest similar to siRNA; BAY-1816032 treatment can significantly hinder the invasion and migration of ATC cells in a dose-dependent manner. [2] |
| In vivo | METHODS: BAY-1816032 (100 mg/kg, oral, 24 days) was used to treat 8505C xenograft model mice to evaluate the anti-ATC activity and safety of BAY-1816032 in mice. RESULTS There was no significant difference in the body weight of each group of mice; the tumor weight of mice treated with BAY-1816032 was significantly reduced. [2] |
| Molecular Weight | 534.51 |
| Formula | C27H24F2N6O4 |
| Cas No. | 1891087-61-8 |
| Smiles | COc1cnccc1Nc1nc(ncc1OC)-c1nn(Cc2c(F)cc(OCCO)cc2F)c2ccccc12 |
| Relative Density. | 1.40 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 15 mg/mL (28.06 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.74 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
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