Barasertib-HQPA

SKU: orb1305276

Description

Barasertib-HQPA

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 722544-51-6
• MW: 507.56
• Purity: 98.85%
• Formula: C₂₆H₃₀FN₇O₃
• SMILES: CCN(CCO)CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)[nH]n3)ncnc2c1
• Target: Aurora Kinase,Apoptosis
• Solubility: Ethanol:3 mg/mL (5.91 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.5 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:250 mg/mL (492.55 mM)

Bioactivity

• Target IC50:
  Aurora B:0.37 nM (cell free)
• In Vivo:
  AZD1152 inhibite the proliferation of mL lines (HL-60, NB4, MOLM13), All line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), an the blast crisis of chronic myeloid leukemia K562 cells with an IC50 ranging from 3 nM to 40 nM. AZD1152 hQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line. Treatment of AZD1152 hQPA decreased expression of AR. AZD1152 potently inhibite the growth of human colon, lung, and hematologic tumor xenografts in immunodeficient mice. In colorectal SW620 tumor-bearing athymic rats treated i.v. With AZD1152, transient suppression of histone H3 phosphorylation followed by accumulation of 4N DNA in cells (2.4-fold higher compared with controls) and then an increased proportion of polyploid cells.
• In Vitro:
  Barasertib inhibite the proliferation of mL lines (HL-60, NB4, MOLM13), All line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), an the blast crisis of chronic myeloid leukemia K562 cells with an IC50 ranging from 3 nM to 40 nM. Barasertib-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line. Treatment of Barasertib-HQPA decreased expression of AR.
• Cell Research:
  LNCaP cells were cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum, in 5 % CO2 at 37℃he cells were treated with 5, 10, 50, 100, and 500 nM of AZD1152 hQPA for 48 h. After 48 h treatment with AZD1152 hQPA, cells were further incubated with 100 μL of MTT (0.5 mg/mL) at 37℃or 2 h. Precipitated formazan was solubilized with 100 μL of DMSO, an the optical densitometry was measured at a wavelength of570 nM. Cell treated with 0.1 % DMSO was defined a the control group.
• Animal Research:
  F Male immune-deficient BALB/c nude mice at 4 weeks of age were maintained in pathogen-free conditions with irradiated chow. Animals were bilaterally, Subcutaneously injected with 2 × 10^6 MOLM13 cells/tumor in 0.1 mL Matrigel. When MOLM13 cells formed palpable tumors, mice were divided andomly into control ( = ) and treatment groups ( = ), and treatment was begun. AZD1152 (5 or 25 mg/kg) with or without vincristine (0.2 mg/kg) was given to mice by intraperitoneal injection 4 times a week or every a Other day, respectively Daunorubicin (1 mg/kg) was given to mice by intraperitoneal injection 6 times during 2 weeks of treatment either alone or in combination with AZD1152 (5 mg/kg) the dose of these agents was determined by our preliminary studies (data not shown). Control diluent was given to the untreated control mice. Body weight and tumors were measured twice a week. Tumor sizes were calculated b the formula: a × b × c, where "a" in the length, "b" in the width, and "c" in the height in millimeters. At the end of the experiment, animals were killed by CO2 asphyxiation and tumor weights were measured after their careful resection. Tumor tissue was collected for analysis.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

INH34, INH-34, INH 34, Barasertib HQPA, BarasertibHQPA, Barasertib-HQPA, AuroraKinase, Aurora Kinase, Aurora B, AZD2811, AZD-2811, AZD1152-HQPA, AZD1152-HQPA, AZD 2811, AZD1152-HQPA, AZD-2811, AZD 2811, Apoptosis, colon

Compound Identifiers

PubChem CID

16007391