1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol
- CAS No.
- 1125593-20-5
- Chemical Name:
- 1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol
- Synonyms
- Mps1-IN-1;Mps1 inhibitor;Mps1 inhibitor 1;Mps-1-IN-1,Mps1IN1,Mps1 IN 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]-
- CBNumber:
- CB62524940
- Molecular Formula:
- C28H33N5O4S
- Molecular Weight:
- 535.66
- MDL Number:
- MFCD22124489
- MOL File:
- 1125593-20-5.mol
- MSDS File:
- SDS
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P305+P351+P338 | |||||||||
NFPA 704 |
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1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol price More Price(13)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 19175 | Mps1-IN-1 ≥98% | 1125593-20-5 | 500μg | $34 | 2024-03-01 | Buy |
Cayman Chemical | 19175 | Mps1-IN-1 ≥98% | 1125593-20-5 | 1mg | $64 | 2024-03-01 | Buy |
Cayman Chemical | 19175 | Mps1-IN-1 ≥98% | 1125593-20-5 | 5mg | $216 | 2024-03-01 | Buy |
Cayman Chemical | 19175 | Mps1-IN-1 ≥98% | 1125593-20-5 | 10mg | $362 | 2024-03-01 | Buy |
AK Scientific | 3868AH | 1-(4-((4-((2-(Isopropylsulfonyl)phenyl)amino)-1H-pyrrolo[2,3-b]pyridin-6-yl)amino)-3-methoxyphenyl)piperidin-4-ol | 1125593-20-5 | 10mg | $500 | 2021-12-16 | Buy |
1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol Chemical Properties,Uses,Production
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.
1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol Preparation Products And Raw materials
Raw materials
Preparation Products
1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |
Shanghai Witofly Chemical Co.,Ltd | sales@witofly.com | China | 2867 | 52 | |
Xunteng International Trading Co.,Limited | China Hong Kong | 878 | 55 | ||
AdooQ Bioscience CHINA | 025-58849295 18951903616; | info@adooq.cn | China | 2989 | 60 |
LETOPHARM LIMITED | +86-21-5821 5861 | sales@letopharm.com | China | 2384 | 58 |
SPIRO PHARMA | eric_feng1954@126.com | China | 9254 | 55 |