ChemicalBook > CAS DataBase List > 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)piperidin-4-ol

Product Name
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
Formula Weight
535.66
MOL File
1125593-20-5.mol
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1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol Property

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)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19175
Product name
Mps1-IN-1
Purity
≥98%
Packaging
500μg
Price
$34
Updated
2024/03/01
Cayman Chemical
Product number
19175
Product name
Mps1-IN-1
Purity
≥98%
Packaging
1mg
Price
$64
Updated
2024/03/01
Cayman Chemical
Product number
19175
Product name
Mps1-IN-1
Purity
≥98%
Packaging
5mg
Price
$216
Updated
2024/03/01
Cayman Chemical
Product number
19175
Product name
Mps1-IN-1
Purity
≥98%
Packaging
10mg
Price
$362
Updated
2024/03/01
AK Scientific
Product number
3868AH
Product name
1-(4-((4-((2-(Isopropylsulfonyl)phenyl)amino)-1H-pyrrolo[2,3-b]pyridin-6-yl)amino)-3-methoxyphenyl)piperidin-4-ol
Packaging
10mg
Price
$500
Updated
2021/12/16
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1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-ol Chemical Properties,Usage,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

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

China 40 China Hong Kong 1 United States 9 Global 50
Musechem
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United States
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TargetMol Chemicals Inc.
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+1-781-999-5354 +1-00000000000
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marketing@targetmol.com
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Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
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TargetMol Chemicals Inc.
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ApexBio Technology
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Cayman Chemical Company
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Matrix Scientific
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1125593-20-5, 1-(4-(4-(2-(isopropylsulfonyl)phenylamino)-1H-pyrrolo[2,3-b]pyridin-6-ylamino)-3-methoxyphenyl)piperidin-4-olRelated Search:


  • 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]-
  • Mps-1-IN-1,Mps1IN1,Mps1 IN 1
  • 1125593-20-5