2. Cell Cycle/DNA Damage Epigenetics Autophagy
  3. Aurora Kinase Autophagy
  4. Danusertib

Danusertib  (Synonyms: 达鲁舍替; PHA-739358)

目录号: HY-10179 纯度: 99.44%
COA 产品使用指南

摩尔计算器

Danusertib 是一种极光激酶 (aurora kinase) 抑制剂，能够抑制 Aurora A，Aurora B 和 Aurora C 的活性，IC50 值分别为 13，79 和 61 nM。

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Danusertib Chemical Structure

Danusertib Chemical Structure

CAS No. : 827318-97-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1148
In-stock
1 mg ￥479
In-stock
2 mg ￥665
In-stock
5 mg ￥1100
In-stock
10 mg ￥1900
In-stock
50 mg ￥5163
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Danusertib 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

Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

IC50 & Target[1]

Aurora A

13 nM (IC50)

Aurora B

79 nM (IC50)

Aurora C

61 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.031 μM
Compound: 8, PHA-739358
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
[PMID: 19320489]
HCT-116 EC50
80 nM
Compound: 9d
Cell cycle arrest in HCT116 cells by accumulation at G2/M phase
Cell cycle arrest in HCT116 cells by accumulation at G2/M phase
[PMID: 17125279]
HeLa IC50
> 25 μM
Compound: 21; MMV676600
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
[PMID: 30647879]
MOLT-4 EC50
0.15 μM
Compound: 1, PHA-739358
Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay
Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay
[PMID: 22889561]
体外研究
(In Vitro)

Danusertib (0.01 to 50 μM) significantly decreases viability of C13 and A2780cp cells. The IC50s are 10.40 and 1.83 μM for C13 cells, and 19.89 and 3.88 μM for A2780cp cells after 24- and 48-h treatment. Danusertib induces cell cycle arrest in G2/M phase in C13 and A2780cp cells. Danusertib treatment results in a marked increase in the percentage of cells arrested in G2/M phase and an accumulation of polyploidy in C13 and A2780cp cells. Danusertib demotes the expression of CDK1/CDC2 and cyclin B1 but promotes the expression of p21 Waf1/Cip1, p27 Kip1, and p53. Danusertib induces autophagy in C13 and A2780cp cells with the involvement of PI3K/Akt/mTOR signaling pathway[1]. PHA-739358 strongly inhibits proliferation of all leukemic cell lines tested, with IC50 values ranging from 0.05 μM to 3.06 μM. PHA-739358 induces antiproliferative effects in BaF3-p210 cells, including IM-resistant M351T, E255K, and T315I mutants. PHA-739358 (5 μM) reduces phosphorylation of CrkL in BaF3-p210 wt cells and IM-resistant mutants[2]. Danusertibsertib leads to cell-cycle arrest and completely inhibits cell proliferation of the GEP-NET cells in vitro[3].

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

Danusertib 相关抗体:
体内研究
(In Vivo)

PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period[2]. In a subcutaneous murine xenograft model, danusertibsertib (2×15 mg/kg/d, i.p.) significantly reduces tumor growth in vivo compared with controls or mice treated with streptozotocine/5-fluorouracil[3].

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

474.55

Formula

C26H30N6O3
CAS 号
性状

固体

颜色

Off-white to yellow

中文名称

达鲁舍替；达努塞替
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 1 year
-20°C 6 months
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (105.36 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 2.1073 mL 10.5363 mL 21.0726 mL
5 mM 0.4215 mL 2.1073 mL 4.2145 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

  • 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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.38 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.38 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.44%

COA (197 KB) HNMR (190 KB) LCMS (404 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

The MTT assay is performed to examine the effect of danusertib on the viability of C13 and A2780cp cells. Briefly, cells are seeded in 96-well culture plates at a density of 8×l03 cells/well. After cells are attached, the cells are treated with danusertib at different concentrations (0.01-50 μM). The control cells receive the vehicle only. After 24-h incubation, 10 μL MTT (5 g/L) is added to each well and cultured for another 4 h. Then, the media is carefully aspirated and 100 μL DMSO is added. The absorbance at the 450 nm wavelength is measured with a Synergy H4 Hybrid microplate reader. The IC50 values are determined using the relative viability over danusertib concentration curve using GraphPad Prism 6.0.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

To evaluate the efficacy and toxicity of PHA-739358 in vivo, a subcutaneous animal model for CML is used; 5×107 K562 cells are injected into the flanks of female SCID mice and tumor growth is monitored daily by palpation. On day 7, when tumors reach an estimated weight of 100 to 150 mg, animals are assigned to 3 experimental groups by random selection and receive the following treatment for a period of 10 days: group 1, control, vehicle solution (7 mice); group 2, PHA-739358 twice a day intraperitoneally at a dose of 15 mg/kg (7 mice); and group 3, IM twice a day per os at 100 mg/kg. Tumor growth is assessed by caliper, and tumor weight is calculated according to the following formula: Tumor weight=[length (mm) × width2 (mm)]/2. Toxicity is monitored by changes in body weight and vitality of the animals.

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

Danusertib 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1073 mL 10.5363 mL 21.0726 mL 52.6815 mL
5 mM 0.4215 mL 2.1073 mL 4.2145 mL 10.5363 mL
10 mM 0.2107 mL 1.0536 mL 2.1073 mL 5.2681 mL
15 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5121 mL
20 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6341 mL
25 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7560 mL
40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3170 mL
50 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0536 mL
60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 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:

Danusertib827318-97-8PHA-739358达鲁舍替达努塞替PHA739358PHA 739358Aurora KinaseAutophagyInhibitorinhibitorinhibit

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