ChemicalBook--->CAS DataBase List--->722543-31-9

722543-31-9

722543-31-9 Structure

722543-31-9 Structure
IdentificationBack Directory
[Name]

AZD1152
[CAS]

722543-31-9
[Synonyms]

AZD1152
CS-1053
Barasertib (AZD1152)
BARASERTIB; AZD-1152; AZD 1152
5-[[7-[3-[Ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-3-acetamide
1H-Pyrazole-3-acetamide, 5-[[7-[3-[ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-
2-[[3-({4-[(5-{2-[(3-fluorophenyl)amino]-2-oxoethyl}-1H-pyrazol-3-yl)amino]quinazolin-7-yl}oxy)propyl](ethyl)amino]ethyl dihydrogen phosphate
[Molecular Formula]

C26H31FN7O6P
[MDL Number]

MFCD15146330
[MOL File]

722543-31-9.mol
[Molecular Weight]

587.54
Chemical PropertiesBack Directory
[density ]

1.463
[storage temp. ]

Keep in dark place,Inert atmosphere,2-8°C
[solubility ]

insoluble in H2O; insoluble in EtOH; ≥5.88 mg/mL in DMSO
[form ]

solid
[pka]

1.75±0.10(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Uses]

Barasertib. is a selective inhibitor of Aurora B kinase, which inhibits human tumor xenograft growth by inducing apoptosis.
[Definition]

ChEBI: AZT-1152 is a dihydrogen phosphate prodrug of a pyrazoloquinazoline aurora kinase inhibitor AZD1152-hydroxyquinazoline pyrazol anilide(HQPA) and is converted rapidly to the active AZD1152-HQPA in plasma. It has a role as a prodrug, an antineoplastic agent and an Aurora kinase inhibitor. It is a member of quinazolines, a monoalkyl phosphate, an anilide, a member of monofluorobenzenes, a member of pyrazoles, a secondary amino compound, a secondary carboxamide and a tertiary amino compound. It is functionally related to an AZD-1152.
[in vivo]

Barasertib (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors[1].
Barasertib (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts[1].
Barasertib (AZD1152, (10-150 mg/kg/d) potently inhibited the growth of human colon, lung, and hematologic tumor xenografts (mean tumor growth inhibition range, 55% to z100%; P < 0.05) in immunodeficient mice[2].

Animal Model:Female immune-deficient BALB/c nude mice (MOLM13 cells injected)[1].
Dosage:5 or 25 mg/kg.
Administration:Intraperitoneal injection 4 times a week or every another day.
Result:Inhibited the growth of human MOLM13 cells growing as xenografts using an immunodeficient murine model.
[IC 50]

Aurora B: 0.37 nM (IC50)
Spectrum DetailBack Directory
[Spectrum Detail]

AZD1152(722543-31-9)MS
AZD1152(722543-31-9)1HNMR
AZD1152(722543-31-9)31PNMR
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