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 MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPjNE02ODBibl2= NIXwWZE1QMLiaB?= MoDNTWM2OD1{NTDuUS=> MonrNlUzPzd4NUm=
LNCaP MVzBdI9xfG:|aYOgRZN{[Xl? NX\kNY57OC13MECgcm0> NGDXcIY1QMLiaB?= MljGbY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bEB1cHKxdXfoJINie3Cjc3WtN{B2eHKnZ4XsZZRqd25? MUGyOVI4PzZ3OR?=
LNCaP MV3GeY5kfGmxbjDBd5NigQ>? M4rVV|UxKG6P NUO4PYtTPDhiaB?= NE\ZbphqdmS3Y3XzJI1q[3KxboXjcIVqKHerdHigZY5mfWenbnnjJI1m[2ijbnnzcS=> MUKyOVI4PzZ3OR?=
Ramos MVvGeY5kfGmxbjDBd5NigQ>? NHHjRZI2ODBibl2= NHjm[YwxNTd{IHi= M2i4OolvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= M2\QdVIyOzdzNES2
Daudi  MWTGeY5kfGmxbjDBd5NigQ>? Mlf3OVAxKG6P NYS5TVlYOC15MjDo NV7o[GVucW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl NG\1d4EzOTN5MUS0Oi=>
L540 MXnGeY5kfGmxbjDBd5NigQ>? M{\lRlUxOCCwTR?= MV[wMVczKGh? NGPK[XJqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= NYXo[XZQOjF|N{G0OFY>
BJAJ NYL2OJZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzVR2E2ODBibl2= NFzQNnUxNTd{IHi= MmjtbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXKyNVM4OTR2Nh?=
Ramos MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHToR3o2ODBibl2= MonjNE04OiCq M1m3fYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NGW3T3QzOTN5MUS0Oi=>
Raji M1vmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfRZWpTPTByIH7N NGmxXpYxNTd{IHi= M{ftNIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= Mn\ONlE{PzF2NE[=
Daudi  M3;kV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH6ZpJyPTByIH7N Mnm2NE04OiCq MUDpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MUSyNVM4OTR2Nh?=
L428 M1HzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkT2OVAxKG6P NELv[WcxNTd{IHi= MXzpcohq[mm2czDj[YxtKGe{b4f0bC=> MoXJNlE{PzF2NE[=
KM-H2 NYjaWnNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS1NFAhdk1? MVGwMVczKGh? MlnubY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4r6XlIyOzdzNES2
HDLM-2 NHrxeY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP4d2s2ODBibl2= MlrFNE04OiCq MYTpcohq[mm2czDj[YxtKGe{b4f0bC=> NILCNm8zOTN5MUS0Oi=>
L450 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S2WVUxOCCwTR?= NF;N[IsxNTd{IHi= NYnUUmxXcW6qaXLpeJMh[2WubDDndo94fGh? Mn7kNlE{PzF2NE[=
BJAJ MnPSRZBweHSxc3nzJGF{e2G7 MnjPOVAxKG6P M3;mbFAuPzJiaB?= NXGxW4ZmcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MX[yNVM4OTR2Nh?=
Ramos NH3PZ|NCeG:ydH;zbZMhSXO|YYm= MU[1NFAhdk1? NFPlNZUxNTd{IHi= NIH1NJRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M1HQ[lIyOzdzNES2
Raji NXTLRolPSXCxcITvd4l{KEG|c3H5 MkL6OVAxKG6P NUPSbIRIOC15MjDo M2\SbYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NYjifo5[OjF|N{G0OFY>
Daudi  MYLBdI9xfG:|aYOgRZN{[Xl? MX[1NFAhdk1? M33HUlAuPzJiaB?= MmLObY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MVWyNVM4OTR2Nh?=
L428 NXGwXZVISXCxcITvd4l{KEG|c3H5 MVS1NFAhdk1? MVewMVczKGh? NVHiXlZvcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NWLBZnJvOjF|N{G0OFY>
KM-H2 M{mxR2Fxd3C2b4Ppd{BCe3OjeR?= NIHM[3o2ODBibl2= NHy2UWcxNTd{IHi= MkPwbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MnP1NlE{PzF2NE[=
HDLM-2 MnvPRZBweHSxc3nzJGF{e2G7 NE[0NHA2ODBibl2= NHjMOmwxNTd{IHi= NHu5cFZqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M1fkTVIyOzdzNES2
L450 NIr2OIFCeG:ydH;zbZMhSXO|YYm= MXK1NFAhdk1? MoPuNE04OiCq NYjDT|FLcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MWiyNVM4OTR2Nh?=
SW620 M{fUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHUepJGSzVyPUGwxtEzNjFibl2= MVmyNVI1PTB7MB?=
HCT116 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\zd3hGSzVyPUGxxtE{NjNibl2= NVfVbWZtOjF{NEWwPVA>
MDA-MB-435 NVrHSmNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV20cIFlOC1zMECwNEBvVQ>? NXTtXGNVOi13IHS= NHfEZYVFVVOR MUXJR|UxRTF{NTDuUS=> MmPINlAyPzV7Mk[=
MDA-MB-468 M2Dsc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\Y[mJDOC1zMECwNEBvVQ>? NVftW3VQOi13IHS= M36yeWROW09? MXPJR|UxRTF2IH7N MYmyNFE4PTl{Nh?=
MDA-MB-231 M2q2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnqVG0xNTFyMECwJI5O NETlW2UzNTViZB?= M1LTR2ROW09? NX\yXnh7UUN3ME2xNFUhdk1? NFfZcnEzODF5NUmyOi=>
BT474 M1S1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXSNE0yODByMDDuUS=> NGL0NmMzNTViZB?= MXnEUXNQ MnHTTWM2OD16IH7N NXH1N5NJOjBzN{W5NlY>
MDA-MB-361 NIHWVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnrZnpzOC1zMECwNEBvVQ>? NWn3XnNiOi13IHS= M2G4cmROW09? M2LXO2lEPTB;N{Cgcm0> M1TiSVIxOTd3OUK2
HER18 NVj3OIx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFm0cXoxNTFyMECwJI5O MkHmNk02KGR? MVrEUXNQ MX\JR|UxRTJyIH7N NX7IPGlIOjBzN{W5NlY>
HER18 NHrKOmVCeG:ydH;zbZMhSXO|YYm= M4jCNVExOCCwTR?= NEO2S4oxNzJ2L{S4JIg> MoX3SG1UVw>? Ml\ybY5lfWOnczDhdI9xfG:|aYOgZY5lKHKnZIXj[ZMh[2yxbn;n[Y5q[yCyb4TlcpRq[Wx? NVLW[VBQOjBzN{W5NlY>
MDA-MB-231 MV;BdI9xfG:|aYOgRZN{[Xl? M1fvfVExPSCwTR?= NEXaZlUxNzJ2L{S4JIg> NHKyXJJFVVOR MljGbY5lfWOnczDhdI9xfG:|aYOgZY5lKHKnZIXj[ZMh[2yxbn;n[Y5q[yCyb4TlcpRq[Wx? MnHaNlAyPzV7Mk[=
JHH-1 M33sfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{n4fFAvO+LCk{GwNFDDqG6P M3i3[lczKGh? M2fmdmVEPTB;MUeuOOKyOS5yIH7N NYDld5czOTl7MUO5N|U>
JHH-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD3NE4{6oDVMUCwNOKhdk1? NHr2PJk4OiCq MYLFR|UxRTJzOD6wxtEyOC56IH7N NIPlWZUyQTlzM{mzOS=>
JHH-4 M4nlcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HsT|AvO+LCk{GwNFDDqG6P MmjWO|IhcA>? NIn3S5FGSzVyPUG1OU43yrFzNj64JI5O M4fLWFE6QTF|OUO1
HuH-1 NYLaTo51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fv[lAvO+LCk{GwNFDDqG6P MUO3NkBp NG[zWWtGSzVyPUK3MlPDuTVwMDDuUS=> MYWxPVkyOzl|NR?=
HuH-6 NU\YenBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPoNE4{6oDVMUCwNOKhdk1? MmHzO|IhcA>? MVTFR|UxRTNwN9MxNE43KG6P M4fxTlE6QTF|OUO1
HuH-7 Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlPjiJNzMECwxsBvVQ>? MVG3NkBp NF63RXBGSzVyPU[uPOKyOC5|IH7N NEH3WmYyQTlzM{mzOS=>
HLE NVXlSWNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjrNE4{6oDVMUCwNOKhdk1? NHyzRog4OiCq NXO3T5h4TUN3ME20OU46yrF4LkSgcm0> NWP5WHd2OTl7MUO5N|U>
HLF NXOzU29ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDpemoxNjQkgKOxNFAxyqCwTR?= NUnBPI9zPzJiaB?= NVS0SI17TUN3ME2xNlYvOcLzMUKuNkBvVQ>? M2m4XFE6QTF|OUO1
PLC/PRF/5 NHPDOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCwMlPjiJNzMECwxsBvVQ>? NGXkPFg4OiCq NXTETHNMTUN3ME23Ok46yrF7Lkmgcm0> M{XYflE6QTF|OUO1
SK-Hep1 MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nxSVAvO+LCk{GwNFDDqG6P MY[3NkBp M1WwcGVEPTB;MkGuPeKyOS5{IH7N Mm\nNVk6OTN7M{W=
Hep3B NYHK[YZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\wUZFIOC5|4pETNVAxOMLibl2= NFfGS484OiCq MkLpSWM2OD15LkdCtVEvOiCwTR?= MXixPVkyOzl|NR?=
HepG2 NH7aV5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrHNFN7OC5|4pETNVAxOMLibl2= NIfofYc4OiCq MmfxSWM2OD1zND63xtEyNjdibl2= M3GxO|E6QTF|OUO1
Ramos MUjBdI9xfG:|aYOgRZN{[Xl? Mly5NlUwPTBxMUCwJI5O NFHXXYY1QCCq MVLpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NIHBeI0yQTh{M{G2PC=>
Daudi  M1TTdGFxd3C2b4Ppd{BCe3OjeR?= M3LF[lI2NzVyL{GwNEBvVQ>? NF;CeZE1QCCq MnLTbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz MknUNVk5OjNzNki=
BALM-14 Ml7jRZBweHSxc3nzJGF{e2G7 MmrZNVIvPS9{NT:1NEBvVQ>? NXrT[JZJPDhiaB?= MXjpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= M4XRe|E6QDJ|MU[4
BALM-27 NWm5THJ{SXCxcITvd4l{KEG|c3H5 Ml64NVIvPS9{NT:1NEBvVQ>? M4fXUFQ5KGh? NHfJRpVqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NXnkbo1mOTl6MkOxOlg>
NB4 Mn7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrqUY93OC5yMT:wMlEwOSEQvF2= MVm0PEBp NIDSRotqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MlPqNVg{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)


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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.

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).

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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 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).

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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.

文献中の引用 (23)

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    CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

  • 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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