Mps1-IN-2
(Synonyms: 9-环戊基-2-[[2-乙氧基-4-(4-羟基哌啶-1-基)苯基]氨基]-5-甲基-8,9-二氢-5H-嘧啶并[4,5-B][1,4]二氮杂卓-6(7H)-酮) 目录号 : GC15745
An inhibitor of Mps1
Cas No.:1228817-38-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-2), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay[1]. |
References: [1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. | |
Mps1-IN-2 is a potent and selective ATP-competitive inhibitor of Mps1 kinase with the IC50 value of 145nM [1].
Mps1-IN-2 has been reported to inhibit Mps1 kinase activity with the IC50 value of 145nM, when screened at 1μM ATP. In addition, Mps1-IN-2 has shown greater than 1000-fold selectivity to the Alk and Ltk enzyme. Moreover, Mps1-IN-2 has been revealed to bound to the ATP biding pocket of Mpa1 and formed a hydrogen bond with the hinge backbone (Glu603) at 2.74-Å resolution. Mps1-IN-2 has been noted to abrogate SAC function and override the checkpoint through direct inhibition of Mps1[1].
References:
[1] Kwiatkowski N1, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. doi: 10.1038/nchembio.345. Epub 2010 Apr 11.
| Cas No. | 1228817-38-6 | SDF | |
| 别名 | 9-环戊基-2-[[2-乙氧基-4-(4-羟基哌啶-1-基)苯基]氨基]-5-甲基-8,9-二氢-5H-嘧啶并[4,5-B][1,4]二氮杂卓-6(7H)-酮 | ||
| 化学名 | 9-cyclopentyl-2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5-methyl-7,8-dihydropyrimido[4,5-b][1,4]diazepin-6-one | ||
| Canonical SMILES | CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(CCC(=O)N4C)C5CCCC5 | ||
| 分子式 | C26H36N6O3 | 分子量 | 480.6 |
| 溶解度 | DMF: 1 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml,DMSO: 1 mg/ml,Ethanol: slightly soluble | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0807 mL | 10.4037 mL | 20.8073 mL |
| 5 mM | 0.4161 mL | 2.0807 mL | 4.1615 mL |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0807 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。