Barasertib (AZD1152) 是 Barasertib-hQPA 的前药,是一种高选择性的 Aurora B 抑制剂,IC50 为 0.37 nM。Barasertib (AZD1152) 可诱导癌细胞生长停滞和凋亡。
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产品名称 | Aurora A ↓ ↑ | Aurora B ↓ ↑ | Aurora C ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BI-847325 |
++
Aurora A (Human), IC50: 25 nM |
++++
Aurora B (Xenopus laevis), IC50: 3 nM |
++
Aurora C (Human), IC50: 15 nM |
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CCT 137690 |
++
Aurora A, IC50: 15 nM |
++
Aurora B, IC50: 25 nM |
++
Aurora C, IC50: 19 nM |
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MK-5108 |
++++
Aurora A, IC50: 0.064 nM |
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KW-2449 |
+
Aurora A, IC50: 48 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Tozasertib |
++++
Aurora A, Ki app: 0.6 nM |
++
Aurora B, Ki app: 18 nM |
+++
Aurora C, Ki app: 4.6 nM |
FLT3,Bcr-Abl | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
AT9283 |
++++
Aurora A, IC50: ~3.0 nM |
++++
Aurora B, IC50: ~3.0 nM |
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MLN8054 |
+++
Aurora A, IC50: 4 nM |
+
Aurora B, IC50: 172 nM |
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ZM-447439 |
+
Aurora A, IC50: 110 nM |
+
Aurora B, IC50: 130 nM |
Src | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
TCS7010 |
++++
Aurora A, IC50: 3.4 nM |
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TAK-901 |
++
Aurora A-TPX2, IC50: 21 nM |
++
Aurora B-INCENP, IC50: 15 nM |
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Danusertib |
+++
Aurora A, IC50: 13 nM |
+
Aurora B, IC50: 79 nM |
+
Aurora C, IC50: 61 nM |
RET | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
MK-8745 |
++++
Aurora A, IC50: 0.6 nM |
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PHA-680632 |
++
Aurora A, IC50: 27 nM |
+
Aurora B, IC50: 135 nM |
+
Aurora C, IC50: 120 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
AMG 900 |
+++
Aurora A, IC50: 5 nM |
+++
Aurora B, IC50: 4 nM |
++++
Aurora C, IC50: 1 nM |
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Alisertib |
++++
Aurora A, IC50: 1.2 nM |
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ENMD-2076 |
+++
Aurora A, IC50: 14 nM |
+
Aurora B, IC50: 350 nM |
FLT3,RET | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
JNJ-7706621 |
+++
Aurora A, IC50: 11 nM |
++
Aurora B, IC50: 15 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
CYC-116 |
+++
Aurora A, Ki: 8 nM |
+++
Aurora B, Ki: 9 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
Reversine |
+++
Aurora A, IC50: 12 nM |
+++
Aurora B, IC50: 13 nM |
++
Aurora C, IC50: 20 nM |
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CCT129202 |
++
Aurora A, IC50: 42 nM |
+
Aurora B, IC50: 198 nM |
+
Aurora C, IC50: 227 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
SNS-314 mesylate |
+++
Aurora A, IC50: 9 nM |
++
Aurora B, IC50: 31 nM |
++++
Aurora C, IC50: 3 nM |
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Barasertib-HQPA |
++++
Aurora B, IC50: 0.37 nM |
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Hesperadin |
+
Aurora B (human), IC50: 250 nM |
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GSK-1070916 |
++++
Aurora B-INCENP, IC50: 3.5 nM |
+++
Aurora C-INCENP, IC50: 6.5 nM |
SIK,Tie-2 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Barasertib, also known as AZD1152, is the precursor to Barasertib-hQPA and is a potent inhibitor of Aurora B kinase, demonstrating an IC50 value of 0.37 nM in cell-free assays. It is known to halt cell proliferation and promote apoptosis in various cancer cells. When applied to freshly isolated leukemia cells at a concentration of 3 μM for 3 hours, Barasertib-HQPA markedly reduces the levels of phosphorylated histone H3[1]. Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is swiftly transformed into the active form, Barasertib-HQPA, within the plasma[2]. Barasertib-HQPA elicits a significant anti-proliferative response, resulting in the emergence of a polyploid cell population, often culminating in apoptosis[3]. |
Animal study | Barasertib at a dosage of 25 mg/kg, significantly reduces the growth and mass of tumors treated with AZD1152. Furthermore, Barasertib at 5 mg/kg improves the efficacy of vincristine or daunorubicin in curbing the growth of human MOLM13 leukemic xenografts[1]. When administered at doses ranging from 10 to 150 mg/kg/day, Barasertib effectively hampers the growth of xenografts of human colon, lung, and blood tumors in immunodeficient mice. The average inhibition of tumor growth observed was between 55% to 100%[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.70mL 0.34mL 0.17mL |
8.51mL 1.70mL 0.85mL |
17.02mL 3.40mL 1.70mL |
CAS号 | 722543-31-9 |
分子式 | C26H31FN7O6P |
分子量 | 587.54 |
别名 | Azd1152 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 35 mg/mL(59.57 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |