ChemicalBook > CAS DataBase List > Phthalazinone pyrazole

Phthalazinone pyrazole

Product Name: Phthalazinone pyrazole
CAS No.: 880487-62-7
Chemical Name: Phthalazinone pyrazole
Synonyms: Phthalazinone pyrazole;Phthalazinone pyrazole Exclusive;4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenylphthalazin-1-one;4-((5-Methyl-1H-pyrazol-3-yl)amino)-2-phenylphthalazin-1(2H)-one;4-[(5-Methyl-1H-pyrazol-3-yl)amino]-2-phenyl-2H-phthalazin-1-one;1(2H)-Phthalazinone, 4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenyl-;4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenyl-1,2-dihydrophthalazin-1-one;Phthalazinone pyrazole,inhibit,human embryonic stem cells,Aurora Kinase,hepatocyte-like cell,Inhibitor,HLCs,Aurora-A kinase,EMT,apoptosis,tumor growth,oral,epithelial-mesenchymal transition
CBNumber: CB72592005
Molecular Formula: C18H15N5O
Formula Weight: 317.34
MOL File: 880487-62-7.mol

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Phthalazinone pyrazole Property

Boiling point:: 557.7±52.0 °C(Predicted)
Density: 1.35±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in EtOH; insoluble in H2O; ≥7.14 mg/mL in DMSO
form: crystalline solid
pka: 13.83±0.10(Predicted)
color: Brown to gray

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 10735
Product name: Phthalazinone pyrazole
Purity: ≥98%
Packaging: 1mg
Price: $68
Updated: 2024/03/01

Cayman Chemical

Product number: 10735
Product name: Phthalazinone pyrazole
Purity: ≥98%
Packaging: 5mg
Price: $302
Updated: 2024/03/01

Cayman Chemical

Product number: 10735
Product name: Phthalazinone pyrazole
Purity: ≥98%
Packaging: 10mg
Price: $535
Updated: 2024/03/01

ApexBio Technology

Product number: C3823
Product name: Phthalazinonepyrazole
Packaging: 1mg
Price: $60
Updated: 2021/12/16

ApexBio Technology

Product number: C3823
Product name: Phthalazinonepyrazole
Packaging: 5mg
Price: $269
Updated: 2021/12/16

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Phthalazinone pyrazole Chemical Properties,Usage,Production

Description

Three Aurora kinases, A-C, are involved in phosphorylation events that are critical for the completion of mitosis. Aurora A, involved in centrosomal assembly and acentrosomal spindle assembly, is overexpressed in many tumors. Phthalazinone pyrazole is a potent inhibitor of Aurora A kinase (IC₅₀ = 31 nM). It does not inhibit Aurora B kinase at doses up to 100 μM. Phthalazinone pyrazole inhibits the proliferation of HCT116, COLO 205, and MCF-7 cells (IC₅₀ = 7.8, 2.9, and 1.6 μM, respectively).

Uses

Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells[1][2].

in vitro

phthalazinone pyrazole potently inhibited the activity of aurora a kinase with an ic50 of 31 nm. it showed no inhibitory effect on aurora b kinase at doses up to 100 μm. phthalazinone pyrazole inhibited the proliferation of hct116, colo205, and mcf-7 cells with ic50 values of 7.8, 2.9, and 1.6 μm, respectively [1].

IC 50

Aurora-A: 0.031 μM (IC₅₀)

References

[1] prime m e, courtney s m, brookfield f a, et al. phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of aurora-a kinase[j]. journal of medicinal chemistry, 2010, 54(1): 312-319.
[2] vader g, lens s m a. the aurora kinase family in cell division and cancer[j]. biochimica et biophysica acta (bba)-reviews on cancer, 2008, 1786(1): 60-72.

Phthalazinone pyrazole Preparation Products And Raw materials

Raw materials

Preparation Products

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880487-62-7, Phthalazinone pyrazoleRelated Search:

Phthalazinone pyrazole

Phthalazinone pyrazole Exclusive

4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenylphthalazin-1-one

1(2H)-Phthalazinone, 4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenyl-

4-[(5-Methyl-1H-pyrazol-3-yl)amino]-2-phenyl-2H-phthalazin-1-one

Phthalazinone pyrazole,inhibit,human embryonic stem cells,Aurora Kinase,hepatocyte-like cell,Inhibitor,HLCs,Aurora-A kinase,EMT,apoptosis,tumor growth,oral,epithelial-mesenchymal transition

4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenyl-1,2-dihydrophthalazin-1-one

4-((5-Methyl-1H-pyrazol-3-yl)amino)-2-phenylphthalazin-1(2H)-one

880487-62-7

88048-62-7