| Identification | Back Directory | [Name]
1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol | [CAS]
1125593-20-5 | [Synonyms]
Mps1-IN-1
Mps1 inhibitor
Mps1 inhibitor 1
1-(4-(4-(2-(Isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl
1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol
1MPS1-IN-1;1-(4-(4-(2-(ISOPROPYLSULFONYL)PHENYLAMINO)-1H-PYRROLO[2,3-B]PYRIDIN-6-YLAMINO)-3-METHOXYPHENYL)PIPERIDIN-4-OL
4-Piperidinol, 1-[3-methoxy-4-[[4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-1H-pyrrolo[2,3-b]pyridin-6-yl]amino]phenyl]- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C28H33N5O4S | [MDL Number]
MFCD22124489 | [MOL File]
1125593-20-5.mol | [Molecular Weight]
535.66 |
| Chemical Properties | Back Directory | [density ]
1.354±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥16.05 mg/mL in DMSO; ≥9.26 mg/mL in EtOH | [form ]
solid | [pka]
14.76±0.20(Predicted) |
| Hazard Information | Back Directory | [Definition]
ChEBI: 1-[3-methoxy-4-[[4-(2-propan-2-ylsulfonylanilino)-1H-pyrrolo[2,3-b]pyridin-6-yl]amino]phenyl]-4-piperidinol is a member of piperidines. | [Biological Activity]
mps1-in-1 is a selective mps1 (monopolar spindle 1) kinase inhibitor with ic50 value of 367 nm.mps1 (monopolar spindle 1 kinase) is a crucial part of the spindle assembly checkpoint. it facilitates the formation of c-mad2 (closed mad2) conformer and the mcc (mitotic checkpoint complex) assembly, involved in the maintenance of chromosomal stability and tumor growth.mps1-in-1 abolishes the sac (spindle assembly checkpoint) function. in u2os cells, dose-dependent treatment of mps1-in-1 decreases the time spent in mitosis with almost 100% cells starting anaphase in 20 minutes. in contrast, just 10% of dmso-treated cells starting anaphase in the same period. acceleration of mitosis kinetics in mps1-in-1 treated cells affects genomic stability and causes aneuploidy. in addition, mps1-in-1 treated cells shows decrease in kinetochore-bound mad2 by 80%. mps1-in-1–treated cells spent roughly 40% less time in mitosis as compared to dmso-treated cells. moreover, mps1-in-1 disrupts the kinase activity of aurora b. mps1-in-1 treatment lead to decrease in the phosphorylation status of aurora b at thr232 in a dose-dependent manner. furthermore, mps1-in-1 increases multipolar cell divisions and decreases cell viability. | [in vitro]
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. It 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. | [target]
| Mps1 367 nM (IC 50 ) | Mps1 27 nM (Kd) | ALK 21 nM (Kd) < /p> | LTK 29 nM (Kd) | PYK2 280 nM (Kd) | FAK < /span> 440 nM (Kd) | IGF1R 750 nM (Kd) | INSR 470 nM (Kd) | CLK1 1900 nM (Kd) < /td> | ERK2 2900 nM (Kd) | INSRR 1200 nM (Kd) | TNK1 < /p> 2600 nM (Kd) | TNK2 3100 nM (Kd) | GAK 1100 nM (Kd) | | [References]
kwiatkowski n, jelluma n, filippakopoulos p et al. small-molecule kinase inhibitors provide insight into mps1 cell cycle function. nat chem biol. 2010 may;6(5):359-68. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
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| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Twochem Co.Ltd.
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| Tel: |
021-58111628 15800915896 |
| Website: |
http://cn.twochem.com |
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