现货，Barasertib (AZD1152-HQPA) ，CAS号:722544-51-6，目录号 S1147 ，Aurora Kinase YZ剂，美国Selleck_详细资料

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保存条件：零下二十摄氏度低温保存供应商：美国Selleck南京办事处英文名： Barasertib (AZD1152-HQPA) CAS号： 722544-51-6 保质期：两年数量：大量规格： 5mg

信号转导通路: HDAC-HSP-Aurora >> Aurora Kinase >> Aurora Kinase YZ剂 >> Barasertib (AZD1152-HQPA)
http://selleck.cn/azd1152-hqpa-S1147.html
技术数据:

分子量(MW): 507.56

化学式:
C₂₆H₃₀FN₇O₃

溶解度: DMSO ≥102mg/mL Water ≥102mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 722544-51-6

生物活性

Barasertib (AZD1152-HQPA) is a highly potent and selective Aurora B inhibitor with a Ki of 0.36 nM. Barasertib (AZD1152-HQPA) inhibits Aurora A with a Ki of 1.37 nM. AZD1152 is converted rapidly to the active Barasertib (AZD1152-HQPA) in plasma. Barasertib (AZD1152-HQPA) has a high specificity versus a panel of 50 other kinases. Consistent with inhibition of Aurora B kinase, addition of Barasertib (AZD1152-HQPA) to tumor cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis. ^[1][2][3]

参考文献

The selective Aurora B kinase inhibitor AZD1152 as a novel treatment for hepatocellular carcinoma Arihiro Aihara, Shinji Tanaka,et al. Journal of Hepatology 2010;52：63–71

Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts Elisabeth Walsby, Val Walsh,et al. haematologica 2008;93(5) ：662－669

Enhancement of radiation response in p53-deﬁcient cancer cells by the Aurora-B kinase inhibitor AZD1152 Y Tao1,P Zhang,et al. Oncogene 2008;27：3244–3255

客户反馈数据

The alamarBlue assay revealed that AURKB inhibition with AZD1152 was effective in NB TICs at EC50 of 1.5 to 4.6 μmol/L, whereas AURKB inhibition was effective in SKPs at 12.4 μmol/L.

1205Lu cells were treated for 48hours with the indicated concentrations of AZD1152-HQPA.

p53 phosphorylation by Aurora B. A, p53 reporter construct was co-transfected with the indicated plasmids into H1299 cells and reporter activation was determined as described under “Experimental Procedures.” B, U2OS cells and H1299 cells were treated with AZD1152 (AZD) for 12 h at the indicated doses. Cell lysates were harvested and immunoblotted with Bax and actin antibodies. C, U2OS cells were treated with 100 ng/ml nocodazole (noc) overnight, and then shake off cells were harvested, washed with PBS, and reseeded. Approximately 2 h later, cells were either lysated or treated with dimethyl sulfoxide (DMSO) or AZD1152 for another 16 h before harvesting. Cell lysates were immunoblotted with Bax, phospho-H3, and actin antibodies. D, GST-p53 or GST control proteins were incubated with Aurora B protein and analyzed for phosphate incorporation (left panel). Coomassie staining of GSTp53 and GST protein is also shown (right panel). E, In vitro phosphorylation sites of GST-p53 identified by mass spectrometry analysis. F, GST-p53 wild-type and 3A mutant proteins were analyzed in a kinase assay as in B. G, plasmids encoding wild-type or 3A mutant (CMV)-FLAG-p53 were transiently transfected into H1299 cells, with or without Myc-Aurora B (AurB) expression vector. 20 h post-transfection, cells were lysed and subjected to immunoprecipitation (IP) with p53 antibody (fl-393). Precipitates were immunoblotted with antibodies to p53 (DO-1), Thr(P) and Ser(P), as indicated. Vec, vector.

如果需要长期保存，请于零下二十度低温保存。

禁止用于人体及ZL！

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20 ° C ，抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

温馨提示：不可用于临床ZL。

分子量(MW):	507.56
化学式:	C₂₆H₃₀FN₇O₃
溶解度:	DMSO ≥102mg/mL Water ≥102mg/mL Ethanol ≥3mg/mL
纯度:	>99%
稳定性:	at -20℃ 2 years
CAS号:	722544-51-6

	The alamarBlue assay revealed that AURKB inhibition with AZD1152 was effective in NB TICs at EC50 of 1.5 to 4.6 μmol/L, whereas AURKB inhibition was effective in SKPs at 12.4 μmol/L.
	1205Lu cells were treated for 48hours with the indicated concentrations of AZD1152-HQPA.
	p53 phosphorylation by Aurora B. A, p53 reporter construct was co-transfected with the indicated plasmids into H1299 cells and reporter activation was determined as described under “Experimental Procedures.” B, U2OS cells and H1299 cells were treated with AZD1152 (AZD) for 12 h at the indicated doses. Cell lysates were harvested and immunoblotted with Bax and actin antibodies. C, U2OS cells were treated with 100 ng/ml nocodazole (noc) overnight, and then shake off cells were harvested, washed with PBS, and reseeded. Approximately 2 h later, cells were either lysated or treated with dimethyl sulfoxide (DMSO) or AZD1152 for another 16 h before harvesting. Cell lysates were immunoblotted with Bax, phospho-H3, and actin antibodies. D, GST-p53 or GST control proteins were incubated with Aurora B protein and analyzed for phosphate incorporation (left panel). Coomassie staining of GSTp53 and GST protein is also shown (right panel). E, In vitro phosphorylation sites of GST-p53 identified by mass spectrometry analysis. F, GST-p53 wild-type and 3A mutant proteins were analyzed in a kinase assay as in B. G, plasmids encoding wild-type or 3A mutant (CMV)-FLAG-p53 were transiently transfected into H1299 cells, with or without Myc-Aurora B (AurB) expression vector. 20 h post-transfection, cells were lysed and subjected to immunoprecipitation (IP) with p53 antibody (fl-393). Precipitates were immunoblotted with antibodies to p53 (DO-1), Thr(P) and Ser(P), as indicated. Vec, vector.

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现货，Barasertib (AZD1152-HQPA) ，CAS号:722544-51-6，目录号 S1147 ，Aurora Kinase YZ剂，美国Selleck

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