1. Cell Cycle/DNA Damage Apoptosis
  2. Polo-like Kinase (PLK) Apoptosis
  3. Onvansertib

Onvansertib  (Synonyms: NMS-1286937; NMS-P937)

目录号: HY-15828 纯度: 99.55%
COA 产品使用指南

nMS-1286937 是一种有效、高选择性、可口服的 PLK1 抑制剂,IC50 值为 2 nM。

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Onvansertib Chemical Structure

Onvansertib Chemical Structure

CAS No. : 1034616-18-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥762
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1 mg ¥295
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5 mg ¥650
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10 mg ¥1000
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50 mg ¥2600
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100 mg ¥4900
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查看 Polo-like Kinase (PLK) 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

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.

IC50 & Target[1]

PLK1

2 nM (IC50)

FLT3

510 nM (IC50)

MELK

744 nM (IC50)

CK2

826 nM (IC50)

体外研究
(In Vitro)

NMS-1286937 是一种有效的、选择性的、可口服的 PLK1 抑制剂,IC50 值为 2 nM。NMS-1286937 还显示出对 FLT3、MELK 和 CK2 的抑制活性,IC50 值分别为 510、744 和 826 nM[1]。NMS-P937 具有 ATP 竞争机制,可逆解离且无时间依赖性。NMS-P937 (10 μM) 具有选择性,对 PLK2PLK3 的抑制活性分别为 48% 和 40%。NMS-P937 对一组 137 种细胞系显示出抗增殖活性,137 种细胞系中有 60 种的 IC50 值低于 100 nM,137 种细胞系中只有 9 种的 IC50 值高于 1 μM[2]。NMS-P937 对 AML-NS8 细胞具有细胞毒活性,IC50 值为 36 nM[3]

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

体内研究
(In Vivo)

NMS-1286937 (45 mg/kg,iv) 在人 HCT116 结肠腺癌细胞异种移植 CD1 nu/nu 小鼠肿瘤模型中表现出良好的肿瘤生长抑制作用和可接受且可逆的体重减轻。NMS-1286937 (60 mg/kg,口服) 也抑制 HCT116 肿瘤异种移植模型上的肿瘤生长[1]。NMS-P937 (45 mg/kg,iv 或 60 mg/kg,po) 在携带 HCT116 肿瘤异种移植模型小鼠中抑制肿瘤生长至相当程度 (TGI,静脉内和口服分别为 83% 和 79%)。NMS-P937 (120 mg/kg given for 4 cycles of 2 consecutive days with 10-day rest) 和阿糖胞苷 (75 mg/kg for 4 cycles of 5 consecutive days with 7-day rest) 在播散性白血病模型中的组合 AML-PS 具有良好的耐受性,并清楚地显示小鼠存活率增加[2]。NMS-P937 (60 mg/kg bid os per day over 2 days with a 5 day rest) 与标准疗法相比显示出良好的疗效,在确定的疾病环境中显著增加了中位生存时间 (MST)[3]

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

Clinical Trial
分子量

532.52

Formula

C24H27F3N8O3

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 1 year
-20°C 6 months
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 21 mg/mL (39.44 mM; 超声加热助溶; 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 1.8779 mL 9.3893 mL 18.7786 mL
5 mM 0.3756 mL 1.8779 mL 3.7557 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。-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 mg/mL (3.76 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.0 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 mg/mL (3.76 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.0 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。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 0.5% MC  0.5% Tween-80

    Solubility: 10 mg/mL (18.78 mM); 悬浊液; 超声助溶

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)。
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: 99.55%

参考文献
Kinase Assay
[1]

The inhibitory activity of putative kinase inhibitors and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-γ-ATP, at optimized buffer and cofactors conditions. At the end of the phosphorylation reaction, more than 98% unlabeled ATP and radioactive ATP is captured by adding an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity. Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting. Inhibitory potency evaluation for all the tested kinases is performed at 25°C using a 60 min end-point assay where the concentrations of ATP and substrates are kept equal to 2 × αKm and saturated (>5 × αKm), respectively.

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

Cell Assay
[2]

Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells are treated in duplicate with serial dilutions of NMS-P937, and 72 hours later, the viable cell number is assessed by the CellTiter-Glo Assay. IC50 values are calculated with a sigmoidal fitting algorithm. Experiments are carried out independently at least twice.

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

Animal Administration
[2]

For carcinoma xenograft studies, 5- to 6-week-old female Hsd, athymic nu/nu mice (average weight, 20-22 g), are used. HCT116, HT29, Colo205 colorectal, and A2780 ovarian human carcinoma cell lines are inoculated subcutaneously. Mice bearing a palpable tumor (100-200 mm3) are treated with vehicle or NMS-P937 following doses and schedules starting from the day after randomization. Tumor dimensions are measured regularly with Vernier calipers, and tumor growth inhibition (TGI) is calculated. Toxicity is evaluated on the basis of body weight reduction. For leukemia studies, 5- to 6-week-old female severe combined immunodeficient mice (SCID; average weight, 20-22 g) are used. The AmL cell line HL-60 (5×106 cells) is injected subcutaneously and treatments initiated when tumor size reaches 200 to 250 mm3. Tumor dimensions and TGI are assessed. For disseminated models, 5×106 AmL primary cells (AmL-PS) are injected intravenously and treatments start after 2 days. Mice are monitored daily for clinical signs of disease, and the median survival time is determined for each group.

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。-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 1.8779 mL 9.3893 mL 18.7786 mL 46.9466 mL
5 mM 0.3756 mL 1.8779 mL 3.7557 mL 9.3893 mL
10 mM 0.1878 mL 0.9389 mL 1.8779 mL 4.6947 mL
15 mM 0.1252 mL 0.6260 mL 1.2519 mL 3.1298 mL
20 mM 0.0939 mL 0.4695 mL 0.9389 mL 2.3473 mL
25 mM 0.0751 mL 0.3756 mL 0.7511 mL 1.8779 mL
30 mM 0.0626 mL 0.3130 mL 0.6260 mL 1.5649 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.

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产品名称:
Onvansertib
目录号:
HY-15828
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