MPI-0479605

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MPI-0479605

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CAS NO:

1246529-32-7

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。

生物活性

MPI-0479605 is a potent and selective ATP-competitive inhibitor ofMps1, with anIC₅₀of 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 IC₅₀of 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].

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].

分子量

407.51

性状

Solid

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。