AZD1152
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CAS No.:
722543-31-9
Content:
0.98%
Sample Available:
Yes
Price valid (until):
2026-11-13
Company Type:
Manufactory
Location:
United States
Payment Terms:
TT against copy of documents,D/P
Average Lead Time:
15 days
Qualification:
Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Description
ProductName AZD1152 Cat No CEI-1229 Product Overview AZD1152 is a highly selective inhibitor of Aurora kinases with IC50 values of 1.37 μM and 0.37 nM for Aurora A and Aurora B, respectively. AZD1152 is a dihydrogen phosphate pro-drug of HQPA which is a highly potent and specific inhibitor of the serine/threonine kinase Aurora kinases. The expression of Aurora kinase A and B are found to be related with the development of various cancers such as ovarian, pancreatic, breast and colon. Since that, the Aurora family is regarded as attractive target for anticancer treatment. As a selective Aurora kinase inhibitor, AZD1152 showed no significant effect on other kinases including JAK2, FLT3 and Abl. Besides that, AZD1152 exerted potent antitumor activities through inhibiting tumor cell proliferation and inducing apoptosis. AZD1152 treatment potently inhibited cell growth in various leukemic cells including ALL PALL-2, MV4-11 and MOLM13 with IC50 values of 5, 1 and 2.8 nM, respectively. AZD1152 also inhibited clone formation of freshly isolated leukemia cells with IC50 values of less than 3 nM. For the colon cancer HCT-116 cells, incubation of AZD1152 at dose of 30 nM for one day resulted in 80% cell number reduction after 4 days drug wash out. In prostate cancer DU145 and PC3 cells, AZD1152 caused decrease of G0/G1-phase cells and induced G2/M cell cycle arrest. Moreover, AZD1152 treatment enhanced the radio sensitivity of prostate cancer cells which were androgen-insensitive. In mice model with human MOLM13 cell xenografts, administration of AZD1152 at dose of 25 mg/kg significantly inhibited tumor growth. The combination treatment of AZD1152 at dose of 5 mg/kg and vincristine at dose of 0.2 mg/kg resulted in almost 100% inhibition of tumor growth of MOLM13 xenografts. In mice injected with MiaPaCa-2cells, the combination of AZD1152 and gemcitabine showed more than double effective than the single treatment. CAS No 722543-31-9 Molecular Weight 587.54 Purity 0.98 Storage Store at -20°C Synonyms Barasertib; AZD-1152; AZD 1152 Targets Aurora B kinase Molecular Formula C26H31FN7O6P Chemical Name 2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate Solubility Soluble in DMSO Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Specialty Chemicals(c26) cas_num 722543-31-9 ECHEMI Editorial ReferenceAZT-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 derives from an AZD-1152.|Barasertib has been used in trials studying the treatment of Tumors, Lymphoma, Solid Tumors, Solid Tumours, and Myeloid Leukemia, among others.|Barasertib is an orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152-hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, AZD1152-HQPA specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells. Aurora kinase B, a serine/threonine protein kinase that functions in the attachment of the mitotic spindle to the centromere, is overexpressed in a wide variety of cancer cell types.Basic Info-
Product Name:
AZD1152
Other Name: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 No.:722543-31-9
Molecular Formula:C26H31FN7O6P
InChIKeys:InChIKey=GBJVVSCPOBPEIT-UHFFFAOYSA-N
Molecular Weight:587.54
Exact Mass:587.54
UNII:16XC2U7W8N
DSSTox ID:DTXSID00222583
NCI Thesaurus Code:C62502
Color/Form:Off-white to light yellow
Categories:
Characteristics-
Density:
1.463
PKA:1.75±0.10(Predicted)
Critical Temperature & Pressure:under inert gas (nitrogen or Argon) at 2–8 °C
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15 days
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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