ChemicalBook > CAS DataBase List > N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide

N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide

Product Name: N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide
CAS No.: 1191911-26-8
Chemical Name: N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide
Synonyms: CZC-25146;CHEMBL2397014;LRRK2 Inhibitor II;CZC-25146 freebase;CZC-25146, 10 mM in DMSO;LRRK2 INHIBITOR II;CZC25146;CZC 25146;N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide;N-(2-((5-fluoro-2-((2-methoxy-4- morpholinophenyl)amino)pyrimidin- 4- yl)amino)phenyl)methanesulfonamide;N-[2-[[5-Fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide;CZC-25146/N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide
CBNumber: CB72695999
Molecular Formula: C22H25FN6O4S
Formula Weight: 488.54
MOL File: 1191911-26-8.mol

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N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide Property

Boiling point:: 697.4±65.0 °C(Predicted)
Density: 1.436±0.06 g/cm3(Predicted)
storage temp.: under inert gas (nitrogen or Argon) at 2-8°C
solubility: ≥24.45 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
form: solid
pka: 8.48±0.10(Predicted)
color: Pale purple to purple

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 22931
Product name: CZC-25146
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 22931
Product name: CZC-25146
Purity: ≥98%
Packaging: 5mg
Price: $116
Updated: 2024/03/01

Cayman Chemical

Product number: 22931
Product name: CZC-25146
Purity: ≥98%
Packaging: 10mg
Price: $199
Updated: 2024/03/01

Cayman Chemical

Product number: 22931
Product name: CZC-25146
Purity: ≥98%
Packaging: 25mg
Price: $456
Updated: 2024/03/01

Tocris

Product number: 6071
Product name: CZC25146
Purity: ≥98%(HPLC)
Packaging: 10
Price: $235
Updated: 2021/12/16

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N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide Chemical Properties,Usage,Production

Description

CZC-25146 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 4.76 nM for the human recombinant kinase). It also inhibits LRRK2^G2019S, a mutant linked to neurotoxicity and Parkinson’s disease, with an IC₅₀ value of 6.87 nM. CZC-25146 is selective for LRRK2 over a panel of kinases in HeLa cell lysates, Jurkat/Ramos mixed cell lysates, as well as whole mouse brain extracts (IC₅₀s = >2 μM). It reduces LRRK2^G2019S-induced cell injury in rat primary cortical neurons.

Uses

CZC-25146 is a compound that acts as an inhibitor of LRRK2, a factor in the expression of Parkinsons’s disease, and is ATP-competitive.

in vivo

CZC-25146 (250 mg/kg; p.o.; 14 days) reduces the ATZ polymer levels in over expressing human polymeric ATZ mice^[3].
CZC-25146 (1 mg/kg for i.v.; 5 mg/kg for p.o.; single dosage) exhibits relatively good pharmacokinetic properties and an extensive distribution throughout animal body following intravenous injection into mice^[1].

Animal Model:	Genetically modified male mice (6 weeks; over expressing human polymeric ATZ)^[3]
Dosage:	250 mg/kg
Administration:	p.o.; 14 days
Result:	Dramatically and reproducibly reduced the ATZ polymer levels with an overall reduction from 60% in the control group to 37%.

Animal Model:

Male CD-1 mice^[1]

Dosage:

1 mg/kg for i.v.; 5 mg/kg for p.o.

Administration:

i.v. and p.o.; single dosage

Result:

Pharmacokinetic Parameters of CZC-25146 in male CD-1 mice^[1].

	i.v. (1 mg/kg)	p.o. (5 mg/kg)
CL (L/h/kg)	2.3
V_ss (L/kg)	5.4
t_1/2 (h)	1.6	1
t_max (h)	0	0.25
C_max (ng/mL)	154	1357
AUC_last (ng/mL·h)	419	2878
AUC_inf (ng/mL·h)	434	2894
F (%)		133

storage

Store at -20°C

References

[1] ramsden n, perrin j, ren z, et al. chemoproteomics-based design of potent lrrk2-selective lead compounds that attenuate parkinson’s disease-related toxicity in human neurons. acs chemical biology, 2011, 6(10): 1021-1028.
[2] troxler t, greenidge p, zimmermann k, et al. discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of lrrk2. bioorganic & medicinal chemistry letters, 2013, 23(14): 4085-4090.

N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide Preparation Products And Raw materials

Raw materials

Preparation Products

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N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide Suppliers

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View Lastest Price from N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide manufacturers

Career Henan Chemical Co

Product: N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide 1191911-26-8
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 200kg
Release date: 2019-12-26

1191911-26-8, N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMideRelated Search:

CZC-25146

N-[2-[[5-Fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide

N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide

N-(2-((5-fluoro-2-((2-methoxy-4- morpholinophenyl)amino)pyrimidin- 4- yl)amino)phenyl)methanesulfonamide

LRRK2 Inhibitor II

LRRK2 INHIBITOR II;CZC25146;CZC 25146

CHEMBL2397014

Methanesulfonamide, N-[2-[[5-fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-

CZC-25146/N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide

CZC-25146 freebase

Leucine-rich repeat kinase 2,Parkinson's disease,Inhibitor,LRRK2,CZC 25146,liver diseases,CZC25146,inhibit,neurons,CZC-25146,inflammatory,LRRK2 G2019S

CZC-25146, 10 mM in DMSO

1191911-26-8

C22H25FN6O4S

Amines, Aromatics, Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals

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