BAY-1816032
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 100mg | $920 | Check With Us |
| 250mg | $1600 | Check With Us |
| 500mg | $2400 | Check With Us |
: Cat #: V4173 CAS #: 1891087-61-8 Purity ≥ 98%
Description: BAY-1816032 (BAY1816032) is a novel, potent and oral bioavailable inhibitor of BUB1 (budding uninhibited by benzimidazoles 1) kinase with anticancer effects.
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- Related Biological Data
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| Molecular Weight (MW) | 534.51 |
|---|---|
| Molecular Formula | C27H24F2N6O4 |
| CAS No. | 1891087-61-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | COC1=C(NC2=NC(C3=NN(CC4=C(F)C=C(OCCO)C=C4F)C5=C3C=CC=C5)=NC=C2OC)C=CN=C1 |
| Synonyms | BAY-1816032; BAY 1816032; BAY1816032 |
| Protocol | In Vitro | BAY-1816032 inhibits BUB1 enzymatic activity with an IC50 of 7 nM, shows slow dissociation kinetics resulting in a long target residence time of 87 min, and an excellent selectivity on a panel of 395 kinases. Mechanistically BAY-1816032 abrogates 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. Persistent lagging chromosomes and missegregation are observed upon combination with low concentrations of paclitaxel. Single agent BAY-1816032 inhibits proliferation of various tumor cell lines with a median IC50 of 1.4 μM and demonstrates synergy or additivity with paclitaxel or docetaxel in almost all cell lines evaluated (minimal combination index 0.3). |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8709 mL | 9.3544 mL | 18.7087 mL | 37.4174 mL |
| 5mM | 0.3742 mL | 1.8709 mL | 3.7417 mL | 7.4835 mL |
| 10mM | 0.1871 mL | 0.9354 mL | 1.8709 mL | 3.7417 mL |
| 20mM | 0.0935 mL | 0.4677 mL | 0.9354 mL | 1.8709 mL |
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