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Barasertib

Barasertib

产品编号 T14371   CAS 722543-31-9
别名: 巴拉塞替, AZD1152

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。

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Barasertib Chemical Structure
Barasertib, CAS 722543-31-9
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
其他形式的 Barasertib:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
产品目录号及名称: Barasertib (T14371)
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纯度: 99.63%
纯度: 98.1%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 33 mg/mL (56.17 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Yang J, et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 2. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. 3. Evans RP, et al. The selective Aurora B kinase inhibitor AZD1152 is a potential new treatment for multiple myeloma. Br J Haematol. 2008 Feb;140(3):295-302. 4. Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8.
Sanguinarine chloride TJ191 Gemcitabine elaidate Protosappanin B NU 7026 MKC-1 Sesamol Lycorine

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 药物功能重定位化合物库 抗癌药物库 抑制剂库 抗癌活性化合物库 人代谢物化合物库 经典已知活性库 表观遗传库 已知活性化合物库 抗癌化合物库

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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。

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Keywords

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

 

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