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

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

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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