Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Barasertib (AZD1152) 是 Barasertib-hQPA 的前体药物,在癌细胞中诱导生长停滞和凋亡。它是高度选择性的Aurora B 抑制剂,IC50值为 0.37 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 298 | 现货 | ||
2 mg | ¥ 428 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,270 | 现货 | ||
50 mg | ¥ 3,890 | 现货 | ||
100 mg | ¥ 5,570 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay. |
靶点活性 | Aurora B:0.37 nM |
体外活性 | AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM and it also inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 causes significant accumulation of cells with 4N/8N DNA content in KMS12 and U266 and induces apoptosis in KMS18 and U266. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[1]. AZD1152 in combination with DEX, has negative effects on cell viability in comparison with single agent in PMI8226, KMS11 and U266[3]. |
体内活性 | Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells[1]. AZD1152 (25 mg/kg/day) treatment reduces xenograft levels such that they are slightly lower levels than after the first round of treatment, but this is not statistically significant indicating that residual cells might be more resistant to a second cycle of AZD1152[4]. In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner[2]. |
别名 | 巴拉塞替, AZD1152 |
分子量 | 587.54 |
分子式 | C26H31FN7O6P |
CAS No. | 722543-31-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33 mg/mL (56.17 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.702 mL | 8.5101 mL | 17.0201 mL | 42.5503 mL |
5 mM | 0.3404 mL | 1.702 mL | 3.404 mL | 8.5101 mL | |
10 mM | 0.1702 mL | 0.851 mL | 1.702 mL | 4.255 mL | |
20 mM | 0.0851 mL | 0.4255 mL | 0.851 mL | 2.1275 mL | |
50 mM | 0.034 mL | 0.1702 mL | 0.3404 mL | 0.851 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Barasertib 722543-31-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase breast cancer colon Inhibitor 巴拉塞替 AZD 1152 leukemia lung inhibit AZD-1152 AZD1152 inhibitor