2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. TAK-901

TAK-901 是多靶点的的极光激酶 (aurora)抑制剂，对极光激酶A和B的IC50 值分别为21 和15 nM。

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TAK-901 Chemical Structure

TAK-901 Chemical Structure

CAS No. : 934541-31-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥888
In-stock
5 mg ￥800
In-stock
10 mg ￥1300
In-stock
50 mg ￥4700
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of TAK-901:

TAK-901 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.

IC50 & Target[1]

Aurora A

21 nM (IC50)

Aurora B

15 nM (IC50)

体外研究
(In Vitro)

TAK-901 对 Aurora B 展示了时间依赖性、紧密结合的抑制作用，但对Aurora A没有这种作用[1]。
TAK-901 在 PC3 细胞中以剂量依赖性方式抑制组蛋白 H3 的磷酸化，EC50 值为 0.16 μM[1]。
TAK-901 是P-糖蛋白(PgP) 药物外排泵的底物，如在子宫肉瘤 MES-SA 细胞中EC50从38 nM下降到在高表达PgP的耐药MES-SA/Dx5细胞中超过50 μM所示[1]。

Cell line EC50 (μM)
A2780 0.085
A375 0.39
A498 0.2
A549 0.13
COLO205 0.11
DLD1 1.5
H226 0.11
H358 0.077
H460 0.81
HT29 0.062
MDA-MB-435S 0.12
MES-SA 0.043
MKN-45 0.16
PC3 0.19
IMR-90 0.088

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TAK-901 相关抗体:
体内研究
(In Vivo)

TAK-901 (在 A2780 和 AML MV4-11 裸鼠异种移植模型中) 分别以30 和40 mg/kg/注射的剂量可抑制肿瘤生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

504.64

Formula

C28H32N4O3S
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 65 mg/mL (128.80 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9816 mL 9.9081 mL 19.8161 mL
5 mM 0.3963 mL 1.9816 mL 3.9632 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.84%

COA (293 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

Enzyme activities of Aurora A/TPX2 and Aurora B/INCENP complexes are assayed at room temperature in buffer containing serially diluted TAK-901, and the product is quantified using IMAP detection reagents. Aurora A/TPX2 (2 nM) is assayed with 100 nM FL-Kemptide and 1 mM ATP. Aurora B/INCENP (0.8 nM) is assayed with 100 nM 5-carboxy-fluorescein-GRTGRRNSI-NH2 (FL-PKAtide) and 10 mM ATP. For time-dependent inhibition, Aurora B/INCENP is incubated with TAK-901 for 1 hour at room temperature followed by addition of 150 mM ATP to initiate the reaction[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cell proliferation is determined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA. IMR-90 immortalized lung fibroblasts are seeded in 96-well microtiter plates and cultured for 3 to 4 days until confluent. Cells are then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay is conducted[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Tumor-bearing mice or rats are treated intravenously twice daily (b.i.d.) with either vehicle or TAK-901 on 2 consecutive days per week or every other day for 2 or 3 cycles. The antitumor activity of TAK-901 in human tumor and leukemia xenograft models are monitored[1].

Nude rats bearing A2780 tumors averaging 250 to 500 mg receive an intravenous dose of TAK-901. Plasma samples are collected by terminal cardiac puncture under CO2 anesthesia. Tumors are dissected and snap-frozen at -80°C[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

TAK-901 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9816 mL 9.9081 mL 19.8161 mL 49.5403 mL
5 mM 0.3963 mL 1.9816 mL 3.9632 mL 9.9081 mL
10 mM 0.1982 mL 0.9908 mL 1.9816 mL 4.9540 mL
15 mM 0.1321 mL 0.6605 mL 1.3211 mL 3.3027 mL
20 mM 0.0991 mL 0.4954 mL 0.9908 mL 2.4770 mL
25 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9816 mL
30 mM 0.0661 mL 0.3303 mL 0.6605 mL 1.6513 mL
40 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2385 mL
50 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
60 mM 0.0330 mL 0.1651 mL 0.3303 mL 0.8257 mL
80 mM 0.0248 mL 0.1239 mL 0.2477 mL 0.6193 mL
100 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4954 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAK-901934541-31-8TAK901TAK 901Aurora KinaseInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-12201
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