1. Cell Cycle/DNA Damage Epigenetics Autophagy
  2. Aurora Kinase Autophagy
  3. Tozasertib

Tozasertib  (Synonyms: 陶扎色替; VX 680; MK-0457)

目录号: HY-10161 纯度: 99.94%
COA 产品使用指南

Tozasertib (VX 680; MK-0457) 是 Aurora A/B/C 激酶抑制剂,Ki 值分别为 0.6,18,4.6 nM。

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Tozasertib Chemical Structure

Tozasertib Chemical Structure

CAS No. : 639089-54-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥891
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5 mg ¥266
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10 mg ¥426
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25 mg ¥810
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50 mg ¥1300
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100 mg ¥2100
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250 mg ¥3100
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1 g   询价  

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查看 Aurora Kinase 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.

IC50 & Target[1]

Aurora A

0.6 nM (Ki)

Aurora B

18 nM (Ki)

Aurora C

4.6 nM (Ki)

体外研究
(In Vitro)

Tozasertib 诱导相似的细胞毒性,IC50 约为 300 nM,并在用 ABL 或 FLT-3(突变型和野生型)激酶转染的 BaF3 细胞中表现出 G2/M 停滞、核内复制和细胞凋亡的 AUR B 样抑制表型。Tozasertib 以时间依赖性方式防止 CAL-62 增殖。Tozasertib 处理 14 天后,8305C 的菌落数量和大小显著降低了约 70%,CAL-62、8505C 和 BHT-101 的菌落数量和大小降低了 90%。Tozasertib 处理不同的 ATC 细胞可抑制增殖,IC50 在 25 和 150 nM 之间。Tozasertib 显著削弱不同细胞系在软琼脂中形成菌落的能力。caspase-3 活性分析表明 Tozasertib 在不同细胞系中诱导细胞凋亡。暴露于 Tozasertib 12 小时的 CAL-62 细胞显示 DNA 含量 ≥ 4N 的细胞积累。延时分析表明,经 Tozasertib 处理的 CAL-62 细胞在不分裂的情况下退出中期。此外,组蛋白 H3 磷酸化在 Tozasertib 处理后被废除[2]。Tozasertib 对患者来源样本中携带 T315I 突变的 BCR-Abl 具有显著的抑制活性[3]

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

Clinical Trial
分子量

464.59

Formula

C23H28N8OS

CAS 号
性状

固体

颜色

White to off-white

中文名称

陶扎色替

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 1 years; -20°C, 6 months (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 106.67 mg/mL (229.60 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1524 mL 10.7622 mL 21.5244 mL
5 mM 0.4305 mL 2.1524 mL 4.3049 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 years; -20°C, 6 months (protect from light)。-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

In Vivo:

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 (4.48 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。

    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 (4.48 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。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):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

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)。

*In solvent : -80°C, 1 years; -20°C, 6 months (protect from light)

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: 99.94%

参考文献
Kinase Assay
[3]

The consumption of ATP is coupled via the pyruvate kinase/lactic dehydrogenase enzyme pair to the oxidation of NADH, which can be monitored through the decrease in absorption at 340 nm. Reactions contains 100 mM Tris (pH 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM phosphoenolpyruvate, 0.6 mg/mL NADH, 75 units/mL pyruvate kinase, 105 units/mL lactate dehydrogenase, and 0.5 mM substrate peptide (sequence: EAIYAAPFAKKK). Reactions (75 μL) are started by adding sufficient kinase to bring the reactions to 30 nM kinase concentration and the decrease in absorbance is monitored over 30 minutes at 30°C in a microtiter plate spectrophotometer. Inhibitory constants are obtained through addition of 3.75 μL Tozasertib in 100% DMSO or DMSO alone. Ki values are calculated as follows, Ki=IC50/(1+[S]/Kd), where [S]=[ATP]=2.2 mM, and Kd (of ATP to Abl)=70 μM. These values are calculated assuming a Kd (ATP) of 70 μM for wild type and H396P Abl kinase domain.

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

Cell Assay
[2]

The CAL-62 cells are cultured in the absence (dimethyl sulfoxide, DMSO) or the presence of 500  nM Tozasertib for different periods of time (1-5 days). The dose-dependent effects of Tozasertib on cell proliferation are evaluated by treating the different ATC cells for 4 days with different concentrations of the Aurora inhibitor (5-500 nM). The cells are pulse labeled with 30 mM BrdU for 2  hours before the end of the incubation time. The BrdU incorporation is analyzed by means of a colorimetric immunoassay using the cell proliferation ELISA kit. The results from Tozasertib-treated cells are compared with those observed in control cells and expressed as a fold of variation versus control.

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

Animal Administration
[1]

For the HL-60 study, female athymic NCr-nu mice are inoculated subcutaneously with 107 HL-60(TB) leukemia cells into the right axillary area. Treatment is administered i.p. b.i.d. after tumors reached 150−200 mm3. Tozasertib is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. Cisplatin, formulated in saline, is administered i.p. q.4.d. for a total of three injections, at a dose of 5.4 mg/kg. For the MIA PaCa-2 studies, female MF1 nude mice are inoculated with 107 MIA PaCa-2 cells into the dorsal flank. Treatment is administered i.p. b.i.d. after tumors reach 175 mm3. Tozasertib is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. 5-fluorouracil, formulated in saline, is administered i.v. q.4.d. at a dose of 50 mg/kg. For the HCT116 study, female Hsd RH rnu/nu rats are inoculated with 107 HCT116 cells into the right flank. Treatment is administered once the tumors reached 700−950 mm3. Tozasertib is administered continuously through an indwelling femoral catheter, followed by a saline infusion for 4 d before repeating the dose cycle. For all studies, tumor volume is determined by caliper measurements three times a week.

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

参考文献

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 years; -20°C, 6 months (protect from light)。-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 2.1524 mL 10.7622 mL 21.5244 mL 53.8109 mL
5 mM 0.4305 mL 2.1524 mL 4.3049 mL 10.7622 mL
10 mM 0.2152 mL 1.0762 mL 2.1524 mL 5.3811 mL
15 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5874 mL
20 mM 0.1076 mL 0.5381 mL 1.0762 mL 2.6905 mL
25 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1524 mL
30 mM 0.0717 mL 0.3587 mL 0.7175 mL 1.7937 mL
40 mM 0.0538 mL 0.2691 mL 0.5381 mL 1.3453 mL
50 mM 0.0430 mL 0.2152 mL 0.4305 mL 1.0762 mL
60 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8968 mL
80 mM 0.0269 mL 0.1345 mL 0.2691 mL 0.6726 mL
100 mM 0.0215 mL 0.1076 mL 0.2152 mL 0.5381 mL
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