MPI-0479605

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MPI-0479605  纯度: 99.13%

MPI-0479605 是一种有效的，选择性的，ATP 竞争性的 Mps1 抑制剂，IC50 值为 1.8 nM。

MPI-0479605

MPI-0479605 Chemical Structure

CAS No. : 1246529-32-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1883 In-stock
2 mg ￥1300 In-stock
5 mg ￥2100 In-stock
10 mg ￥3800 In-stock
50 mg ￥13300 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.

IC50 & Target[1]

Mps1

1.8 nM (IC50)

ALK

0.26 μM (IC50)

B-RAF

3.2 μM (IC50)

ERK2

3.9 μM (IC50)

FAK1

2.7 μM (IC50)

FER

0.59 μM (IC50)

FLT3

0.08 μM (IC50)

INSR

0.38 μM (IC50)

JNK1

0.11 μM (IC50)

PLK4

3.3 μM (IC50)

STK33

1.1 μM (IC50)

体外研究
(In Vitro)

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM. MPI-0479605 (0.1-10 μM) reduces cell viability of HCT-116 cells in a dose-dependent manner. MPI-0479605 shows severe defects in the ability to align chromosomes at the metaphase plate, but causes complete cytokinesis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

MPI-0479605 (30 mg/kg daily or 150 mg/kg every fourth day (Q4D), i.p.) inhibits tumor growth by 49% and 74 % in HCT-116 xenografts. However, MPI-0479605 does not show inhibitory activity via daily dosing on the Colo-205 xenografts, and dosing every four days causes 63% tumor growth inhibition (TGI)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

407.51

Formula

C22H29N7O
CAS 号

1246529-32-7
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
In Vitro: 

DMSO : 11 mg/mL (26.99 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4539 mL 12.2696 mL 24.5393 mL
5 mM 0.4908 mL 2.4539 mL 4.9079 mL
10 mM 0.2454 mL 1.2270 mL 2.4539 mL

*

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。
参考文献

  • [1]. Tardif KD, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol Cancer Ther. 2011 Dec;10(12):2267-2275.
Animal Administration
[1]

HCT-116 or Colo-205 cells are transplanted subcutaneously into the flanks of nude (nu+/nu+) mice and compound (MPI-0479605) treatment is initiated when tumor masses reaches an average size of 100 mm3. MPI-0479605 is formulated in 5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300, ispinesib is formulated in 2% cremaphor/2% DMA, and 5-fluorouracil is formulated in 2% sodium bicarbonate. Tumor volume is measured using vernier calipers and tumor growth inhibition (TGI) is calculated as: %TGI= 100-100(change in median tumor volume of treated)/(change in median tumor volume control)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Tardif KD, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol Cancer Ther. 2011 Dec;10(12):2267-2275.

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