2. Cell Cycle/DNA Damage Cytoskeleton
  3. Mps1
  4. NMS-P715

NMS-P715 是一种选择性的，ATP 竞争性的 MPS1 抑制剂，IC50 值为 182 nM。

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NMS-P715 Chemical Structure

NMS-P715 Chemical Structure

CAS No. : 1202055-32-0

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规格 价格 是否有货 数量
1 mg ￥723
In-stock
2 mg ￥1053
In-stock
5 mg ￥1150
In-stock
10 mg ￥1800
In-stock
50 mg ￥5500
In-stock
100 mg 现货 询价
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500 mg   询价  

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Customer Review

Other Forms of NMS-P715:

NMS-P715 相关抗体

Top Publications Citing Use of Products

  • 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-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.

IC50 & Target[1]

Mps1

182 nM (IC50)

CK2

5.7 μM (IC50)

MELK

6.01 μM (IC50)

NEK6

6.02 μM (IC50)

体外研究
(In Vitro)

NMS-P715 is a selective inhibitor of MPS1, with an IC50 of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC50 value of 5 μM and only 3 kinases inhibited below 10 μM (CK2, MELK, and NEK6). NMS-P715 promotes massive spindle assembly checkpoint (SAC) override with an EC50 of 65 nM. NMS-P715 (1 μM) causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy and inhibits the proliferation of HCT116 cells. NMS-P715 (0.5, 1 μM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation[1]. NMS-P715 (1 μM) exhibits bypass of the spindle assembly checkpoint and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. NMS-P715 (0-25 μM) also selectively inhibits growth of PDAC cells[2].

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

NMS-P715 相关抗体:
体内研究
(In Vivo)

NMS-P715 (10 mg/kg) exhibits an oral bioavailability of 37% and good pharmacokinetic properties in nude mice bearing subcutaneous implanted human tumor cell xenografts. NMS-P715 (90 mg/kg, p.o.) is well tolerated and cuases no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model. NMS-P715 (100 mg/kg, p.o.) inhibits the tumor growth by appr 43% in the A375 melanoma xenograft model[1].

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

676.73

Formula

C35H39F3N8O3
CAS 号
性状

固体

颜色

White to off-white

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 : 2 mg/mL (2.96 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 1.4777 mL 7.3885 mL 14.7769 mL
5 mM --- --- ---
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

动物实验：

以下溶解方案，请直接配制工作液。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% CMC/saline water

    Solubility: 3.33 mg/mL (4.92 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

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: 98.41%

COA (193 KB) LCMS (97 KB)

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

The potency of the compound towards MPS1 and 60 additional kinases belonging to kinase selectivity screening (KSS) panel is determined using either a strong anion exchanger based assay or P81 Multiscreen plate. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 μM NaVO3, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE) and 8 μM ATP with 1.5 nM 33P-γ-ATP. The assay is run in a robotized format, 10 serial 1:3 compounds dilutions (including NMS-P715, from 30 μM to 1.5 nM) are tested and IC50 determined[1].

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

Cells lines are seeded in 384 well-plates in the appropiate complete medium and treated with compounds (NMS-P715, etc.) dissolved in 0.1% DMSO 24 hours after seeding. The cells are incubated at 37°C and 5% CO2 and after 72 hours the plates are processed using CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data using Assay Explorer software. IC50 of proliferation is calculated using sigmoidal interpolation curve fitting. Activity Ratio is calculated as the ratio of the single cell line IC50 and the IC50 average of all the cell lines tested[1].

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

Mice[1]
Athymic nu-nu mice, 5-6 weeks of age (20-22 g) are used in the assay. A2780 ovary carcinoma and A375 melanoma cells are transplanted s.c. into female nu-nu mice. Mice bearing a palpable tumor (100-200 mm3) are selected and randomized into control and treated groups. Treatment starts one day after randomization. NMS-P715 is typically administered by oral administration at doses of 90-100 mg/kg daily for more than seven days. Each group includs 8 animals. Tumor dimension is measured regularly by calipers during the experiments and tumor mass is calculated[1].

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

NMS-P715 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 1.4777 mL 7.3885 mL 14.7769 mL 36.9424 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:

NMS-P7151202055-32-0Mps1Monopolar spindle 1Inhibitorinhibitorinhibit

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产品名称：
NMS-P715
目录号：
HY-12382
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