1. Cell Cycle/DNA Damage Cytoskeleton
  2. Mps1
  3. TC-Mps1-12

TC-Mps1-12 是一种高效、选择性的 Mps1 抑制剂,其 IC50 值为 6.4 nM。

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TC-Mps1-12 Chemical Structure

TC-Mps1-12 Chemical Structure

CAS No. : 1206170-62-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3711
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1 mg ¥1750
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5 mg ¥5200
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM[1].

IC50 & Target

IC50: 6.4 nM (Mps1)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.84 μM
Compound: 12
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
[PMID: 24900510]
A549 IC50
840 nM
Compound: 14; TC Mps1 12
Antiproliferative activity against human A549 cells by MTT assay
Antiproliferative activity against human A549 cells by MTT assay
[PMID: 31121430]
HCT-116 IC50
0.56 μM
Compound: 6
Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132
Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132
[PMID: 24256217]
HCT-116 GI50
1.6 μM
Compound: 6
Growth inhibition in human HCT116 cells after 72 hrs by MTT assay
Growth inhibition in human HCT116 cells after 72 hrs by MTT assay
[PMID: 24256217]
RERF-LC-AI IC50
131 nM
Compound: 12
Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting
Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting
[PMID: 24900510]
Sf9 IC50
0.011 μM
Compound: 6
Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay
Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay
[PMID: 24256217]
体外研究
(In Vitro)

TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay[1].
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM[1].

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

Cell Viability Assay[1]

Cell Line: 549 cells
Concentration:
Incubation Time: 72 hours
Result: Inhibited the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM.
体内研究
(In Vivo)

TC-Mps1-12 (25-100 mg/kg; p.o.; daily; for 19 days) inhibits the growth of A549 cells in a dose-dependent manner in vivo. At a dose of 100 mg/kg, TC-Mps1-12 exhibits 47% tumor growth inhibition without body weight loss[1].
TC-Mps1-12 shows good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL at an oral dose of 25 mg/kg[1].

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

Animal Model: A549 mouse xenograft model[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; for 19 days
Result: Inhibited the growth of A549 cells in a dose-dependent manner.
Animal Model: A549 mouse xenograft model (pharmacokinetic )[1]
Dosage: 25 mg/kg
Administration: Oral administration
Result: Cmax = 3542 ng/mL, AUC = 6604 ng h/mL
分子量

324.38

Formula

C17H20N6O

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 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (154.14 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 3.0828 mL 15.4140 mL 30.8280 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 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, 6 months; -20°C, 1 month。-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。

  • 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.76%

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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0828 mL 15.4140 mL 30.8280 mL 77.0701 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 mL 15.4140 mL
10 mM 0.3083 mL 1.5414 mL 3.0828 mL 7.7070 mL
15 mM 0.2055 mL 1.0276 mL 2.0552 mL 5.1380 mL
20 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8535 mL
25 mM 0.1233 mL 0.6166 mL 1.2331 mL 3.0828 mL
30 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5690 mL
40 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
50 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5414 mL
60 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
80 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
100 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 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:
TC-Mps1-12
目录号:
HY-110115
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