Barasertib (AZD1152-HQPA) 化学構造
分子量: 507.56

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Quality Control & MSDS

製品説明

  • Compare Aurora Kinase Inhibitors
    Aurora Kinase製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Barasertib (AZD1152-HQPA)は、0.37nMのIC50による非常に選択的なオーロラB阻害剤です。
ターゲット Aurora B
IC50 0.37 nM [1]
In vitro試験 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
LNCaP NHPPbnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqwMVUxOCCwTR?= MVS0POKhcA>? NU\R[2VqUUN3ME2yOUBvVQ>? NYHYU|lyOjV{N{e2OVk>
LNCaP NUi2XlYxSXCxcITvd4l{KEG|c3H5 NGHSb44xNTVyMDDuUS=> NUTPUoUzPDkEoHi= MXzpcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYToJJRpem:3Z3igZ4F{eGG|ZT2zJJVxemWpdXzheIlwdg>? NHnjPHMzPTJ5N{[1PS=>
LNCaP MVHGeY5kfGmxbjDBd5NigQ>? MV61NEBvVQ>? M2\CSFQ5KGh? M2n2O4lv\HWlZYOgcYlkem:wdXPs[Ykhf2m2aDDhcoV2\2WwaXOgcYVkcGGwaYPt NWrUO3Z3OjV{N{e2OVk>
Ramos M2P4WWZ2dmO2aX;uJGF{e2G7 NV;NSlluPTByIH7N NEKySnIxNTd{IHi= NWD5e5VUcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl MX:yNVM4OTR2Nh?=
Daudi  Mn\JSpVv[3Srb36gRZN{[Xl? MkT3OVAxKG6P MWewMVczKGh? Mn7obY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn NGO4NG8zOTN5MUS0Oi=>
L540 MlfkSpVv[3Srb36gRZN{[Xl? M1vPPFUxOCCwTR?= MljhNE04OiCq M3i5SYlvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= MV:yNVM4OTR2Nh?=
BJAJ MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLrc4N{PTByIH7N NXjUWIpLOC15MjDo MnTrbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NYTsVZJtOjF|N{G0OFY>
Ramos M2GwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjvTms2ODBibl2= M324NFAuPzJiaB?= Mli5bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NXf2[XJ3OjF|N{G0OFY>
Raji M3TR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvMc4c2ODBibl2= MXKwMVczKGh? NEXWRmhqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MXSyNVM4OTR2Nh?=
Daudi  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nWSlUxOCCwTR?= MWKwMVczKGh? MUXpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NXT1Xm86OjF|N{G0OFY>
L428 M3HR[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zvWlUxOCCwTR?= NVj4e3dPOC15MjDo NHG5SIpqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NGDXeIQzOTN5MUS0Oi=>
KM-H2 NHrDdYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnFTZY2ODBibl2= MoXjNE04OiCq NIS2SnpqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MW[yNVM4OTR2Nh?=
HDLM-2 Mn[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm1NFAhdk1? NHfEeI4xNTd{IHi= Mn7BbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4jtXFIyOzdzNES2
L450 M{HubWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK1OVAxKG6P Mo\hNE04OiCq Mmq2bY5pcWKrdIOgZ4VtdCCpcn;3eIg> NV75e2hOOjF|N{G0OFY>
BJAJ NWnuVGNFSXCxcITvd4l{KEG|c3H5 M1W5elUxOCCwTR?= MWmwMVczKGh? MW\pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M4G3OVIyOzdzNES2
Ramos NGXRUJRCeG:ydH;zbZMhSXO|YYm= NFXGdXg2ODBibl2= Mlr2NE04OiCq MoTnbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M2LNPVIyOzdzNES2
Raji NYTlW|hnSXCxcITvd4l{KEG|c3H5 MnHGOVAxKG6P NH;tUGoxNTd{IHi= M1LUXIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MkX0NlE{PzF2NE[=
Daudi  MXnBdI9xfG:|aYOgRZN{[Xl? M4jiVFUxOCCwTR?= NIToUXUxNTd{IHi= NYX4d3NkcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NV7Ed|J{OjF|N{G0OFY>
L428 NGrMbXlCeG:ydH;zbZMhSXO|YYm= M3[zVlUxOCCwTR?= MVWwMVczKGh? NXn0VldHcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MYeyNVM4OTR2Nh?=
KM-H2 Mk\uRZBweHSxc3nzJGF{e2G7 NYjPSmFOPTByIH7N MXSwMVczKGh? MWLpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M2HCc|IyOzdzNES2
HDLM-2 MWDBdI9xfG:|aYOgRZN{[Xl? MWi1NFAhdk1? NF3uN3AxNTd{IHi= MYrpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NIW1RZozOTN5MUS0Oi=>
L450 Mlm1RZBweHSxc3nzJGF{e2G7 M1n1VlUxOCCwTR?= M3vDfVAuPzJiaB?= M1nNOIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NYDh[FVxOjF|N{G0OFY>
SW620 Mn\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoOwSWM2OD1zMNMxNk4yKG6P MWqyNVI1PTB7MB?=
HCT116 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\pRnFGSzVyPUGxxtE{NjNibl2= Ml7FNlEzPDVyOUC=
MDA-MB-435 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3hPZF4OC1zMECwNEBvVQ>? NEHkUZQzNTViZB?= NXfxc4I{TE2VTx?= MW\JR|UxRTF{NTDuUS=> NV;oUIZGOjBzN{W5NlY>
MDA-MB-468 NVHzNGNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17UVVAuOTByMECgcm0> M{Dy[|IuPSCm NVfDW3N{TE2VTx?= M4C5S2lEPTB;MUSgcm0> NFTlOIgzODF5NUmyOi=>
MDA-MB-231 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zBT|AuOTByMECgcm0> NV7Zc|l3Oi13IHS= NHnyd3lFVVOR MUXJR|UxRTFyNTDuUS=> MonFNlAyPzV7Mk[=
BT474 MnHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLRO2NCOC1zMECwNEBvVQ>? M2X5RVIuPSCm MVPEUXNQ NIqxWYVKSzVyPUigcm0> NFnsPVEzODF5NUmyOi=>
MDA-MB-361 M3z4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKwMVExODByIH7N MXWyMVUh\A>? MlP0SG1UVw>? MlPITWM2OD15MDDuUS=> Ml;FNlAyPzV7Mk[=
HER18 NInDeWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoCxNE0yODByMDDuUS=> MWGyMVUh\A>? MYDEUXNQ NViwc3FiUUN3ME2yNEBvVQ>? MX6yNFE4PTl{Nh?=
HER18 MYjBdI9xfG:|aYOgRZN{[Xl? NXzlZll7OTByIH7N NFHpcmcxNzJ2L{S4JIg> M3[xO2ROW09? MVnpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? NInqPJkzODF5NUmyOi=>
MDA-MB-231 M4TUdWFxd3C2b4Ppd{BCe3OjeR?= M3;ucFExPSCwTR?= NVu2ZplbOC9{ND:0PEBp NYrxc|JJTE2VTx?= MYDpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? MWGyNFE4PTl{Nh?=
JHH-1 NXLEemFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ntR|AvO+LCk{GwNFDDqG6P NEjLRpo4OiCq NX3tcIs4TUN3ME2xO{41yrFzLkCgcm0> MlvrNVk6OTN7M{W=
JHH-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H2Z|AvO+LCk{GwNFDDqG6P MXu3NkBp M{TI[mVEPTB;MkG4MlDDuTFyLkigcm0> M3LaTVE6QTF|OUO1
JHH-4 NVTVe29VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMlPjiJNzMECwxsBvVQ>? NY\XPJFHPzJiaB?= NHfoWI1GSzVyPUG1OU43yrFzNj64JI5O NUG5WmtwOTl7MUO5N|U>
HuH-1 NHLqe4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHXNE4{6oDVMUCwNOKhdk1? M{j5XVczKGh? M4jpZWVEPTB;MkeuN:KyPS5yIH7N MXexPVkyOzl|NR?=
HuH-6 MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nlWFAvO+LCk{GwNFDDqG6P MXi3NkBp NITPV4hGSzVyPUOuO:KyOC54IH7N NEjpVosyQTlzM{mzOS=>
HuH-7 NH3iWHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCwMlPjiJNzMECwxsBvVQ>? NHvrSZI4OiCq M3j0OmVEPTB;Nj64xtExNjNibl2= NWjpc|hkOTl7MUO5N|U>
HLE MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSwMlPjiJNzMECwxsBvVQ>? MmqxO|IhcA>? MnTNSWM2OD12NT65xtE3NjRibl2= MoTGNVk6OTN7M{W=
HLF MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWyNE4{6oDVMUCwNOKhdk1? Mlu1O|IhcA>? MVvFR|UxRTF{Nj6xxtEyOi5{IH7N NUi0To5rOTl7MUO5N|U>
PLC/PRF/5 NXLWVmxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPzPGtyOC5|4pETNVAxOMLibl2= MVy3NkBp M2DB[GVEPTB;N{[uPeKyQS57IH7N NXjt[Jh[OTl7MUO5N|U>
SK-Hep1 M3L5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjGTmkxNjQkgKOxNFAxyqCwTR?= MkXuO|IhcA>? NVvSN2s5TUN3ME2yNU46yrFzLkKgcm0> M2[xZVE6QTF|OUO1
Hep3B M{Xs[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoWzNE4{6oDVMUCwNOKhdk1? NVrkTXdvPzJiaB?= NYT6SWVVTUN3ME23MlbDuTFwMjDuUS=> MYCxPVkyOzl|NR?=
HepG2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMlPjiJNzMECwxsBvVQ>? NFjTT2E4OiCq NVi3fHdiTUN3ME2xOE44yrFzLkegcm0> M4\4NlE6QTF|OUO1
Ramos M{nKO2Fxd3C2b4Ppd{BCe3OjeR?= NX3OeJlSOjVxNUCvNVAxKG6P MYe0PEBp MXnpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= M3HDeVE6QDJ|MU[4
Daudi  NUnDe2h2SXCxcITvd4l{KEG|c3H5 NX7zT4RLOjVxNUCvNVAxKG6P NH\GenQ1QCCq NXXkendpcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MnjGNVk5OjNzNki=
BALM-14 MXLBdI9xfG:|aYOgRZN{[Xl? Ml3nNVIvPS9{NT:1NEBvVQ>? NFf1c4M1QCCq MnnUbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz MnXwNVk5OjNzNki=
BALM-27 NX65dVg1SXCxcITvd4l{KEG|c3H5 MoDZNVIvPS9{NT:1NEBvVQ>? NGDBOYw1QCCq NX7oWolPcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ Mm\INVk5OjNzNki=
NB4 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\IeIwxNjBzL{CuNU8yKM7:TR?= NWPMWpVJPDhiaB?= MXjpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MmnRNVg{Pjd2OES=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 A Phase I study to assess the safety and tolerability of AZD1152-HQPA in combination with low dose cytosine arabinoside (LDAC) in patients with acute myeloid leukaemia (AML) has been completed.
特集

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 HL-60, NB4, MOLM13, PALL-2, MV4-11, EOL-1, and K562 cells
濃度 Dissolved in DMSO, final concentrations ~100 nM
反応時間 24 or 48 hours
実験の流れ 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.

動物実験: [1]

動物モデル Female immune-deficient BALB/c nude mice subcutaneously injected with MOLM13 cells
製剤 Dissolved in 3M Tris, pH 9.0, at a concentration of 2.5 mg/mL
投薬量 5 or 25 mg/kg
投与方法 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 pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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

参考

化学情報

Download Barasertib (AZD1152-HQPA) SDF
分子量 507.56
化学式

C26H30FN7O3

CAS No. 722544-51-6
保管 2年-20℃
6月-80℃in solvent
別名 INH 34
溶解度 (25°C) * In vitro DMSO 102 mg/mL (200.96 mM)
エタノール 3 mg/mL (5.91 mM)
<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.
化学名 2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide

カスタマーフィードバック (8)


Click to enlarge
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.

Click to enlarge
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.

Click to enlarge
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).

Click to enlarge
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 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 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).

Click to enlarge
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.

Click to enlarge
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.

文献中の引用 (23)

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  • ML141

    ML141 is a potent, selective and reversible non-competitive inhibitor of Rho family GTPase cdc42 with IC50 of 200 nM.

  • Salirasib

    Salirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2.

  • Alisertib (MLN8237)

    Alisertib (MLN8237)は、1.2nMのIC50による選択的なオーロラA阻害剤です。

    Features:First orally available inhibitor of Aurora A.

  • VX-680 (Tozasertib, MK-0457)

    VX-680 (Tozasertib, MK-0457)は汎オーロラ・キナーゼ(AK)阻害剤、、オーロラA、オーロラBとオーロラCに作用すると、 Kiapp がそれぞれ 0.6 nM、18 nM 、 4.6 nMになる。

  • Danusertib (PHA-739358)

    Danusertib (PHA-739358)は ポ-ピラゾール分子が小さいauroraキナーゼとBcr-Ablキナーゼ阻害剤、auroraA, B, Cを作用すると、 IC50がそれぞれ 13 nM, 79 nM, 61 nMとなる.

  • ZM 447439

    ZM 447439は、オーロラ選択ATPです-競争的な阻害剤で、オーロラAキナーゼとオーロラBキナーゼに作用すると、IC50が それぞれ 110 nM と 130 nM,になる。

    Features:An Aurora selective ATP-competitive inhibitor.

  • MLN8054

    MLN8054は、4nMのIC50によるオーロラAキナーゼの強力で選択的な阻害剤です。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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