1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]

中文名称:

1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol

中文同义词:

1-[4-[[4-[[2-(异丙基磺酰基)苯基]氨基]-1H-吡咯并[2,3-B]吡啶-6-基]氨基]-3-甲氧基苯基]哌啶-4-醇;MPS1抑制剂(MPS1-IN-1)

英文名称:

1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol

英文同义词:

1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol;1-(4-(4-(2-(Isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl;Mps1-IN-1;1MPS1-IN-1;1-(4-(4-(2-(ISOPROPYLSULFONYL)PHENYLAMINO)-1H-PYRROLO[2,3-B]PYRIDIN-6-YLAMINO)-3-METHOXYPHENYL)PIPERIDIN-4-OL;Mps1 inhibitor;Mps1 inhibitor 1;4-Piperidinol, 1-[3-methoxy-4-[[4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-1H-pyrrolo[2,3-b]pyridin-6-yl]amino]phenyl]-

CAS号:

1125593-20-5

分子式:

C28H33N5O4S

分子量:

535.66

EINECS号:

604-604-1

相关类别:

细胞生物学试剂

Mol文件:

1125593-20-5.mol

密度 

1.354±0.06 g/cm3(Predicted)

酸度系数(pKa)

14.76±0.20(Predicted)

生物活性

Mps1-IN-1 是一种有效的，选择性的，ATP 竞争性的 Mps1 抑制剂，IC50 和 Kd 值分别为 367 nM 和 27 nM。

靶点

Mps1 367 nM (IC 50 ) Mps1 27 nM (Kd) ALK 21 nM (Kd) LTK 29 nM (Kd) PYK2 280 nM (Kd) FAK 440 nM (Kd) IGF1R 750 nM (Kd) INSR 470 nM (Kd) CLK1 1900 nM (Kd) ERK2 2900 nM (Kd) INSRR 1200 nM (Kd) TNK1 2600 nM (Kd) TNK2 3100 nM (Kd) GAK 1100 nM (Kd)

Mps1 367 nM (IC 50 )

Mps1 27 nM (Kd)

体外研究

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC 50 and a K d of 367 nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with K d s of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 (10 µM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 (5-10 µM) suppresses the proliferative capacity of HCT116.