Barasertib (AZD1152-HQPA)

Catalog No.S1147

Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

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Barasertib (AZD1152-HQPA) Chemical Structure

Barasertib (AZD1152-HQPA) Chemical Structure
Molecular Weight: 507.56

Validation & Quality Control

8 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Barasertib (AZD1152-HQPA) is available in the following compound libraries:

Aurora Kinase Inhibitors with Unique Features

  • Pan Aurora Kinase Inhibitors

    Danusertib (PHA-739358) Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=13 nM/79 nM/61 nM. SNS-314 Mesylate Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=9 nM/31 nM/3 nM.

  • Most Potent Aurora Kinase Inhibitor

    MK-5108 (VX-689) Aurora A, IC50=0.064 nM.

  • Aurora Kinase Inhibitor in Clinical Trial

    Alisertib (MLN8237) Phase III for Relapsed/Refractory Peripheral T-Cell Lymphoma.

  • Classic Aurora Kinase Inhibitor

    Hesperadin Potently inhibits Aurora B with IC50 of 250 nM.

Product Information

  • Compare Aurora Kinase Inhibitors
    Compare Aurora Kinase Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Targets Aurora B [1]
(Cell-free assay)
Aurora A [1]
(Cell-free assay)
IC50 0.37 nM 1368 nM
In vitro AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying ~100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM. AZD1152 inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
LNCaPMofvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFftU|AxNTVyMDDuUS=>M3K1U|Q5yqCqMWfJR|UxRTJ3IH7NM2W0S|I2Ojd5NkW5
LNCaPNGTCVXJCeG:ydH;zbZMhSXO|YYm=MUCwMVUxOCCwTR?=MnnDOFjDqGh?MoXObY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bEB1cHKxdXfoJINie3Cjc3WtN{B2eHKnZ4XsZZRqd25?MWWyOVI4PzZ3OR?=
LNCaPNXnI[5k5TnWwY4Tpc44hSXO|YYm=MkDSOVAhdk1?NETRe2Q1QCCqNVjpSowxcW6mdXPld{BucWO{b371Z4xmcSC5aYToJIFv\XWpZX7pZ{Bu\WOqYX7pd40>NX\ybJJEOjV{N{e2OVk>
RamosM1uzO2Z2dmO2aX;uJGF{e2G7M1TSVlUxOCCwTR?=MlmwNE04OiCqMl36bY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOnNXzhc5pzOjF|N{G0OFY>
Daudi M1vGZWZ2dmO2aX;uJGF{e2G7NF3nVpU2ODBibl2=MXiwMVczKGh?Mm\KbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOnM3nYWlIyOzdzNES2
L540NVLNUGpRTnWwY4Tpc44hSXO|YYm=M322b|UxOCCwTR?=Mmf6NE04OiCqMWrpcohq[mm2czDBeZJwemFiQjDrbY5ie2V?Mm\tNlE{PzF2NE[=
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RamosMU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX61NFAhdk1?M3vNPFAuPzJiaB?=MkHQbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?=NF\ofFIzOTN5MUS0Oi=>
RajiNWrSR4tkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NI\m[Yo2ODBibl2=NUP3WGMxOC15MjDoMoTTbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?=NXjkUJRMOjF|N{G0OFY>
Daudi MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3qwbVUxOCCwTR?=NWHYV5NEOC15MjDoNX\Nc4lpcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=>MmTzNlE{PzF2NE[=
L428MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NYL1dZFqPTByIH7NMlLYNE04OiCqNF7zN4xqdmirYnn0d{Bk\WyuIHfyc5d1cA>?M4PnflIyOzdzNES2
KM-H2MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVu1NFAhdk1?NVSxW|J4OC15MjDoMXLpcohq[mm2czDj[YxtKGe{b4f0bC=>NXvKT|hDOjF|N{G0OFY>
HDLM-2NFzoV2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGPpRVE2ODBibl2=NVi2OlZTOC15MjDoM{PmNYlvcGmkaYTzJINmdGxiZ4Lve5RpMWqyNVM4OTR2Nh?=
L450MnTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NGjubFk2ODBibl2=NIHCN4gxNTd{IHi=M{W4dIlvcGmkaYTzJINmdGxiZ4Lve5RpMoHVNlE{PzF2NE[=
BJAJNGnzcIJCeG:ydH;zbZMhSXO|YYm=NEXBfIE2ODBibl2=M2nZTFAuPzJiaB?=M1L3dIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyNWe4Smc2OjF|N{G0OFY>
RamosM37VN2Fxd3C2b4Ppd{BCe3OjeR?=NETUXHg2ODBibl2=MVWwMVczKGh?NX;rT4ppcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI>NVG0Vm1UOjF|N{G0OFY>
RajiMXnBdI9xfG:|aYOgRZN{[Xl?MnnGOVAxKG6PNV;wZo9TOC15MjDoNWDCS3hQcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI>NUTqPWxHOjF|N{G0OFY>
Daudi NIrJc4ZCeG:ydH;zbZMhSXO|YYm=MVe1NFAhdk1?MVSwMVczKGh?MXPpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?=M4PWR|IyOzdzNES2
L428MVfBdI9xfG:|aYOgRZN{[Xl?Mmj6OVAxKG6PMnvGNE04OiCqNVnKR4FCcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI>NVf3copQOjF|N{G0OFY>
KM-H2MlroRZBweHSxc3nzJGF{e2G7NWrQdVl4PTByIH7NM4DvbVAuPzJiaB?=MmLubY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK=M1q1WlIyOzdzNES2
HDLM-2M{e3e2Fxd3C2b4Ppd{BCe3OjeR?=MUe1NFAhdk1?M2Tr[FAuPzJiaB?=M170O4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXyNXnOVIdEOjF|N{G0OFY>
L450M4rjR2Fxd3C2b4Ppd{BCe3OjeR?=NUHxdJpPPTByIH7NMXqwMVczKGh?NW\RUJV5cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI>NXTn[nF6OjF|N{G0OFY>
SW620NHPVVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Ml3MSWM2OD1zMNMxNk4yKG6PMoS5NlEzPDVyOUC=
HCT116MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWXNVXFTTUN3ME2xNeKyOy5|IH7NMlqyNlEzPDVyOUC=
MDA-MB-435NXPabXQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mk\oNE0yODByMDDuUS=>NWTrVYlQOi13IHS=MX3EUXNQM1jj[2lEPTB;MUK1JI5OMUeyNFE4PTl{Nh?=
MDA-MB-468NY\IVVJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4H1NFAuOTByMECgcm0>NGLYU2gzNTViZB?=M3XTXWROW09?Mo\YTWM2OD1zNDDuUS=>NV7wTGtOOjBzN{W5NlY>
MDA-MB-231M4i0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF7UWoQxNTFyMECwJI5OMlX2Nk02KGR?NXzXcHo1TE2VTx?=NX64cVZDUUN3ME2xNFUhdk1?MoLsNlAyPzV7Mk[=
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MDA-MB-361NIH6[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXfy[m16OC1zMECwNEBvVQ>?MnXJNk02KGR?Mor1SG1UVw>?M2L1TGlEPTB;N{Cgcm0>MWCyNFE4PTl{Nh?=
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HER18M{fNRWFxd3C2b4Ppd{BCe3OjeR?=MX:xNFAhdk1?NUHNSmZ{OC9{ND:0PEBpMlPpSG1UVw>?NE\F[GRqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?=Mkf4NlAyPzV7Mk[=
MDA-MB-231MWrBdI9xfG:|aYOgRZN{[Xl?NHfR[2IyODVibl2=MoW1NE8zPC92ODDoMoqySG1UVw>?NGrSRmRqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?=MnzpNlAyPzV7Mk[=
JHH-1NEPoR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYnm[mhsOC5|4pETNVAxOMLibl2=MWG3NkBpMXrFR|UxRTF5LkVCtVEvOCCwTR?=NXrrS2RnOTl7MUO5N|U>
JHH-2NVS0NpVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NX;kZm5jOC5|4pETNVAxOMLibl2=NX;BVI14PzJiaB?=M{SwN2VEPTB;MkG4MlDDuTFyLkigcm0>NITZ[GkyQTlzM{mzOS=>
JHH-4NUH6fnhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{XzOVAvO+LCk{GwNFDDqG6PNVPxXndPPzJiaB?=NYK1T4pWTUN3ME2xOVUvPsLzMU[uPEBvVQ>?NXvrTIdPOTl7MUO5N|U>
HuH-1M1fjZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MojBNE4{6oDVMUCwNOKhdk1?NVy4d5ZmPzJiaB?=NELXRnlGSzVyPUK3MlPDuTVwMDDuUS=>MWixPVkyOzl|NR?=
HuH-6MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVjpZ29tOC5|4pETNVAxOMLibl2=MXK3NkBpNGXmXJpGSzVyPUOuO:KyOC54IH7NNFXpZZgyQTlzM{mzOS=>
HuH-7Ml3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3W0elAvO+LCk{GwNFDDqG6PNULUUI1YPzJiaB?=M{fQVWVEPTB;Nj64xtExNjNibl2=MkjjNVk6OTN7M{W=
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HLFMm[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MX[wMlPjiJNzMECwxsBvVQ>?MXm3NkBpM1TRXGVEPTB;MUK2MlHDuTF{LkKgcm0>M3;PflE6QTF|OUO1
PLC/PRF/5MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlfxNE4{6oDVMUCwNOKhdk1?M4\jTlczKGh?MlH2SWM2OD15Nj65xtE6Njlibl2=MnrBNVk6OTN7M{W=
SK-Hep1MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGHFV2oxNjQkgKOxNFAxyqCwTR?=M3jFPFczKGh?NFnMZohGSzVyPUKxMlnDuTFwMjDuUS=>MV:xPVkyOzl|NR?=
Hep3BMki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MXiwMlPjiJNzMECwxsBvVQ>?NEizcWM4OiCqMXfFR|UxRTdwNtMxNU4zKG6PMYexPVkyOzl|NR?=
HepG2M2ThZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1vHSFAvO+LCk{GwNFDDqG6PMYG3NkBpMWnFR|UxRTF2LkhCtVEvPyCwTR?=Ml;tNVk6OTN7M{W=
RamosMVnBdI9xfG:|aYOgRZN{[Xl?NH;lVmgzPS93MD:xNFAhdk1?NYjNU494PDhiaB?=M4ntUIlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=>MUGxPVgzOzF4OB?=
Daudi MWrBdI9xfG:|aYOgRZN{[Xl?MnPTNlUwPTBxMUCwJI5ONUTseIh5PDhiaB?=NGS3d5dqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM>MnrRNVk5OjNzNki=
BALM-14MVPBdI9xfG:|aYOgRZN{[Xl?NGrZVZEyOi53L{K1M|UxKG6PNIHtTGY1QCCqMX3pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO=Mn60NVk5OjNzNki=
BALM-27MYPBdI9xfG:|aYOgRZN{[Xl?NF[3RWUyOi53L{K1M|UxKG6PM3T3PVQ5KGh?MoDabY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCzMV2xPVgzOzF4OB?=
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... Click to View More Cell Line Experimental Data

In vivo Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells. [1] In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner. [2]
Features

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines HL-60, NB4, MOLM13, PALL-2, MV4-11, EOL-1, and K562 cells
Concentrations Dissolved in DMSO, final concentrations ~100 nM
Incubation Time 24 or 48 hours
Method Cells are exposed to various concentrations of AZD1152 for 24 or 48 hours. Cell proliferation is measured by 3H-thymidine uptake (isotope added 6 hours before harvest), and the concentration that induced 50% growth inhibition (IC50) is calculated from dose-response curves. Cell cycle analysis is performed by flow cytometry. Cell apoptosis is measured by annexin V–FITC apoptosis detection kit.

Animal Study: [1]

Animal Models Female immune-deficient BALB/c nude mice subcutaneously injected with MOLM13 cells
Formulation Dissolved in 3M Tris, pH 9.0, at a concentration of 2.5 mg/mL
Dosages 5 or 25 mg/kg
Administration Intraperitoneal injection 4 times a week or every another day

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Yang J, et al. Blood, 2007, 110(6), 2034-2040.

[2] Wilkinson RW, et al. Clin Cancer Res, 2007, 13(12), 3682-3688.

Chemical Information

Download Barasertib (AZD1152-HQPA) SDF
Molecular Weight (MW) 507.56
Formula

C26H30FN7O3

CAS No. 722544-51-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms INH 34
Solubility (25°C) * In vitro DMSO 102 mg/mL (200.96 mM)
Ethanol 3 mg/mL (5.91 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% PEG 400+0.5% Tween 80+5% Propylene glycol 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide

Customer Product Validation(8)


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Rating
Source Nature 2014 508(7494), 118-22. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Long-term cell proliferation assays
Cell Lines A375-SOX10KD cells
Concentrations 0.5 uM
Incubation Time 4 weeks
Results Compared with controls, treatment of A375-SOX10KD cells with a combination of both vemurafenib and GDC0941 lead to proliferation arrest.

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Rating
Source J Exp Med 2014 10.1084/jem.20141123. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Giemsa staining
Cell Lines Primary MKPs
Concentrations
Incubation Time
Results Notably, Aurora B inhibitor (AZD-1152) treatment caused primary MKPs maturation and normal DNA ploidy.

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Rating
Source Clin Cancer Res 2010 16, 4572-4582. Barasertib (AZD1152-HQPA) purchased from Selleck
Method alamarBlue assay
Cell Lines NB TICs
Concentrations
Incubation Time 72 h
Results Proliferation of NB TICs is reduced following inhibition of AURKB, showing low micromolar EC50 values (1.5-4.6 μmol/L). In contrast to this, SKPs were less sensitive to AZD1152, exhibiting higher EC50 values (12.4 μmol/L).

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Rating
Source Oncogene 2014 33, 3550-60. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Western blot, time-lapse microscopy, flow cytometry
Cell Lines HeLa cells , HCT116 cells
Concentrations 6.25-50 nM
Incubation Time 2 h, 24 h, 48 h
Results Barasertib inhibits AURKB specifically and triggers mitotic slippage

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Rating
Source Oncogene 2012 31, 1217–1227. Barasertib (AZD1152-HQPA) purchased from Selleck
Method FACS
Cell Lines OVCAR10 cells
Concentrations
Incubation Time 3 h
Results Further, although a >4N hyperploid population was induced by treatment of cells with inhibitors selective for AURKA (MLN8257) or AURKB (AZD1152), only the combination of dasatinib with MLN8257 selectively reduced this population of cells.

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Rating
Source J Biol Chem 2011 286, 2236-44. Barasertib (AZD1152-HQPA) purchased from Selleck
Method luciferase reporter assay, Western blotting, mass spectrometry analysis, kinase assay, Immunoprecipitation Assay
Cell Lines U2OS cells, H1299 cells
Concentrations 0-120 nM
Incubation Time 12 h/16 h
Results As shown in Fig. A, whereas wild-type Aurora B efficiently suppressed p53 in a luciferase reporter assay, a kinase-inactive Aurora B mutant (K106R) had a minimal effect on p53 transcriptional activity. In line with this, treatment of U2OS cells, but not H1299 cells, with the Aurora B-specific inhibitor AZD1152 markedly induced Bax expression (Fig. B). As shown in Fig. C, AZD1152 significantly induced Bax expression in the cells released from mitosis, suggesting that Aurora B is required for p53 suppression in G 1 to early S-phase. To determine whether Aurora B directly phosphorylates p53, we performed an in vitro kinase assay using Aurora B protein expressed in insect cells as the kinase source and GST-p53 purified from bacteria as the substrate and confirmed that Aurora B directly phosphorylates p53 (Fig. D).

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Rating
Source J Pharmacol Exp Ther 2012 343(3), 617-27. Barasertib (AZD1152-HQPA) purchased from Selleck
Method ELISA/Kinase Assays
Cell Lines Mice-bearing tumors
Concentrations 25 mg/kg
Incubation Time 0-7 day
Results ABT-348 inhibited the VEGF response with a potency (ED 50 = 0.2 mg/kg i.v.) that is comparable with another potent anti-VEGF agent, ABT-869, which has intrinsic VEGFR2 potency similar to ABT-348 (IC 50 = 4 and 3 nM, respectively). On-target VEGF receptor inhibition was also implicated by the observation that administration of ABT-348 to tumor-bearing mice resulted in increased plasma levels of the proangiogenic PLGF (Fig. B). acute changes in the MRI signal were observed during treatment with ABT-348 (Fig. C). After a sharp decrease in Ktrans that was apparent within 24 h after the first treatment cycle of ABT-348, the MRI signal returned to pretreatment levels by 6 days when reassessed longitudinally, which was reflective of the Q7D-dosing sequence. (Fig. D) the reduction in Ktrans (75%) was similar in magnitude to that previously reported for the selective EGFR/PDGFR inhibitor.

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Rating
Source Dr. Gao Zhang of University of Pennsylvania. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Western blot
Cell Lines 1205Lu cells
Concentrations 50-500 nM, 2-8 μM
Incubation Time 48 h
Results AZD1152 treatment resulted in a reduction of Rb Ser780 phosphorylation at higher concentration.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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