上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
BAY-1816032 纯度: 99.19%
BAY-1816032是有效,有口服活性的苯并咪唑出芽抑制解除同源物蛋白1激酶 (BUB1 (budding uninhibited by benzimidazoles 1) kinase) 抑制剂,IC50 值小于 7 nM。
BAY-1816032 Chemical Structure
CAS No. : 1891087-61-8
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥2293 | In-stock | |
5 mg | ¥1950 | In-stock | |
10 mg | ¥2950 | In-stock | |
25 mg | ¥5900 | In-stock | |
50 mg | ¥9900 | In-stock | |
100 mg | ¥17000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
BAY-1816032 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Chemical Probe Library
- Targeted Diversity Library
生物活性 |
BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM. |
IC50 & Target |
IC50: 7 nM (BUB1)[1] |
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体外研究 (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)[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
534.51 |
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Formula |
C27H24F2N6O4 |
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CAS 号 |
1891087-61-8 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 25 mg/mL (46.77 mM; Need ultrasonic and warming) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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参考文献 |
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