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AZD1152

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AZD1152 Basic information

Product Name:
AZD1152
Synonyms:
  • 1H-Pyrazole-3-acetamide, 5-[[7-[3-[ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-
  • AZD1152
  • 5-[[7-[3-[Ethyl[2-(phosphonooxy)ethyl]amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-3-acetamide
  • BARASERTIB; AZD-1152; AZD 1152
  • Barasertib (AZD1152)
  • CS-1053
  • 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
  • 2-(Ethyl(3-((4-((3-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1H-pyrazol-5-yl)amino)quinazolin-7-yl)oxy)propyl)amino)ethyl dihydrogen phosphate
CAS:
722543-31-9
MF:
C26H31FN7O6P
MW:
587.54
Mol File:
722543-31-9.mol
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AZD1152 Chemical Properties

Density 
1.463
storage temp. 
under inert gas (nitrogen or Argon) at 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
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AZD1152 Usage And Synthesis

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)

AZD1152Supplier

Capot Chemical Co., Ltd
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+86 (0) 571 85 58 67 18
BOC Sciences
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1-631-485-4226; 16314854226
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info@bocsci.com
Shanghai Topbiochem Technology Co., Ltd
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021-58170097
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info@topbiochem.com
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Haoyuan Chemexpress Co., Ltd.
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021-58950125
Email
info@chemexpress.com
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AZD1152(722543-31-9)Related Product Information