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

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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 NG\B[ZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTPNE02ODBibl2= NIHpPJE1QMLiaB?= M2rrfmlEPTB;MkWgcm0> Mn\TNlUzPzd4NUm=
LNCaP M2j4OWFxd3C2b4Ppd{BCe3OjeR?= M1;tRlAuPTByIH7N MojyOFjDqGh? M1zlZYlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIghfGi{b4XnbEBk[XOyYYPlMVMhfXC{ZXf1cIF1cW:w NXzkWG9HOjV{N{e2OVk>
LNCaP NFLNWnRHfW6ldHnvckBCe3OjeR?= NGL5TnA2OCCwTR?= NYTQPYdHPDhiaB?= MoPrbY5lfWOnczDtbYNzd263Y3zlbUB4cXSqIHHu[ZVo\W6rYzDt[YNp[W6rc32= M{LBRlI2Ojd5NkW5
Ramos NHXxW2ZHfW6ldHnvckBCe3OjeR?= MYC1NFAhdk1? MlHRNE04OiCq NVPTNZhTcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl NXnVN2pNOjF|N{G0OFY>
Daudi  M3PIOGZ2dmO2aX;uJGF{e2G7 NYTCVFRkPTByIH7N NH3PdmkxNTd{IHi= MVHpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? MUKyNVM4OTR2Nh?=
L540 NGrmN3NHfW6ldHnvckBCe3OjeR?= NWLTZZBEPTByIH7N MnPENE04OiCq NEfuS|lqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= NWPPUHRQOjF|N{G0OFY>
BJAJ MnzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;X[5A2ODBibl2= MlW3NE04OiCq NFzKZ3pqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MXOyNVM4OTR2Nh?=
Ramos NEfYdY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI[wPVI2ODBibl2= M1rhe|AuPzJiaB?= MoG1bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXiyNVM4OTR2Nh?=
Raji MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUS1NFAhdk1? MkHsNE04OiCq MknObY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NHq5flMzOTN5MUS0Oi=>
Daudi  NGXBelZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnGTm9zPTByIH7N MVOwMVczKGh? Ml7kbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NIP1dWczOTN5MUS0Oi=>
L428 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LJUVUxOCCwTR?= M4\Zd|AuPzJiaB?= NIjBeW1qdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHnPXJAzOTN5MUS0Oi=>
KM-H2 M1;QR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zJd|UxOCCwTR?= NYXJNVFkOC15MjDo NGLhe2FqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4PPNFIyOzdzNES2
HDLM-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\QToYxPTByIH7N NX23SIRPOC15MjDo M3zlW4lvcGmkaYTzJINmdGxiZ4Lve5Rp M3PUSlIyOzdzNES2
L450 NUj4[lhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf3[Go2ODBibl2= MlvVNE04OiCq NYfRZXZTcW6qaXLpeJMh[2WubDDndo94fGh? NEXs[mMzOTN5MUS0Oi=>
BJAJ NE\2U3lCeG:ydH;zbZMhSXO|YYm= NGfFSYg2ODBibl2= NVP3TmlsOC15MjDo MVjpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NGHYUZczOTN5MUS0Oi=>
Ramos M4e5bWFxd3C2b4Ppd{BCe3OjeR?= NWfH[4Y1PTByIH7N NVLTeos4OC15MjDo M{m3cYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M1jORVIyOzdzNES2
Raji NEfmZZpCeG:ydH;zbZMhSXO|YYm= MUm1NFAhdk1? MYiwMVczKGh? NYW1[HVUcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NYPXSI1DOjF|N{G0OFY>
Daudi  MkPiRZBweHSxc3nzJGF{e2G7 M4PxclUxOCCwTR?= MnKzNE04OiCq M{fvV4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M1\n[FIyOzdzNES2
L428 NGLlUJVCeG:ydH;zbZMhSXO|YYm= NFLO[HI2ODBibl2= MY[wMVczKGh? MXnpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NWXYTZhpOjF|N{G0OFY>
KM-H2 NFfkV|dCeG:ydH;zbZMhSXO|YYm= NYjyd4FpPTByIH7N MmnZNE04OiCq MV\pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NUT1TJhLOjF|N{G0OFY>
HDLM-2 NIT4UI5CeG:ydH;zbZMhSXO|YYm= NF;BNpQ2ODBibl2= MXewMVczKGh? NVS0Z5pmcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MlzHNlE{PzF2NE[=
L450 M2noVGFxd3C2b4Ppd{BCe3OjeR?= NIPhdmY2ODBibl2= NXjXN2kyOC15MjDo MnKybY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NVvaU4M5OjF|N{G0OFY>
SW620 NHnMdWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXFR|UxRTFywsGyMlEhdk1? M{Hae|IyOjR3MEmw
HCT116 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrPcYlqTUN3ME2xNeKyOy5|IH7N M{TaN|IyOjR3MEmw
MDA-MB-435 M3n0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDFVpkxNTFyMECwJI5O NVLMWZBXOi13IHS= MlfPSG1UVw>? NG\3bZFKSzVyPUGyOUBvVQ>? NHn6UmEzODF5NUmyOi=>
MDA-MB-468 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXq0OW5pOC1zMECwNEBvVQ>? MVWyMVUh\A>? M{LXZ2ROW09? MXfJR|UxRTF2IH7N M3zQ[|IxOTd3OUK2
MDA-MB-231 NFTYWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[wMVExODByIH7N NFPrPIwzNTViZB?= MnvmSG1UVw>? NVj0Z|RVUUN3ME2xNFUhdk1? MVuyNFE4PTl{Nh?=
BT474 NUDYV|V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLXd2YxNTFyMECwJI5O NETjN2kzNTViZB?= MXzEUXNQ MX;JR|UxRThibl2= NX3rc4lROjBzN{W5NlY>
MDA-MB-361 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW4NHdOOC1zMECwNEBvVQ>? MnH0Nk02KGR? M1ruSWROW09? MWfJR|UxRTdyIH7N MX:yNFE4PTl{Nh?=
HER18 NETtbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;6TXMxNTFyMECwJI5O M{LtN|IuPSCm M1;sVGROW09? M4LyW2lEPTB;MkCgcm0> MXGyNFE4PTl{Nh?=
HER18 NEfWfXpCeG:ydH;zbZMhSXO|YYm= Mn7qNVAxKG6P NX63S5RqOC9{ND:0PEBp NUG5OIl3TE2VTx?= NVfhNZc4cW6mdXPld{BieG:ydH;zbZMh[W6mIILl[JVk\XNiY3zvco9o\W6rYzDwc5RmdnSrYXy= NEP3NmozODF5NUmyOi=>
MDA-MB-231 MlXMRZBweHSxc3nzJGF{e2G7 NWPqRohsOTB3IH7N NUPVeXBoOC9{ND:0PEBp MYPEUXNQ NHjacXBqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= MlzmNlAyPzV7Mk[=
JHH-1 M2O4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\BPVAvO+LCk{GwNFDDqG6P NXTQb3BVPzJiaB?= MlniSWM2OD1zNz60xtEyNjBibl2= Ml\ZNVk6OTN7M{W=
JHH-2 NFP1eJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMlPjiJNzMECwxsBvVQ>? MUe3NkBp NGXM[WtGSzVyPUKxPE4xyrFzMD64JI5O MXSxPVkyOzl|NR?=
JHH-4 NHf1RZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMlPjiJNzMECwxsBvVQ>? NXvp[3lSPzJiaB?= Ml3VSWM2OD1zNUWuOuKyOTZwODDuUS=> NUjEco95OTl7MUO5N|U>
HuH-1 Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnLVVYxNjQkgKOxNFAxyqCwTR?= NF7xS244OiCq MVPFR|UxRTJ5LkRCtVUvOCCwTR?= NH3GcG0yQTlzM{mzOS=>
HuH-6 NYDjfo1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjEOoMxNjQkgKOxNFAxyqCwTR?= NFfCV|Y4OiCq M4T4NmVEPTB;Mz63xtExNjZibl2= MVexPVkyOzl|NR?=
HuH-7 Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWwMlPjiJNzMECwxsBvVQ>? MmqxO|IhcA>? MmHDSWM2OD14LklCtVAvOyCwTR?= Ml3aNVk6OTN7M{W=
HLE NIj6O5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLTNE4{6oDVMUCwNOKhdk1? M{DsZ|czKGh? MYDFR|UxRTR3LkpCtVYvPCCwTR?= NEDNR3UyQTlzM{mzOS=>
HLF MlLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XiOlAvO+LCk{GwNFDDqG6P MoHLO|IhcA>? MUjFR|UxRTF{Nj6xxtEyOi5{IH7N M3XLflE6QTF|OUO1
PLC/PRF/5 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DVPVAvO+LCk{GwNFDDqG6P MlXvO|IhcA>? M3vYdWVEPTB;N{[uPeKyQS57IH7N NE\6c|cyQTlzM{mzOS=>
SK-Hep1 NEHKPGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[wMlPjiJNzMECwxsBvVQ>? M4C5R|czKGh? MXPFR|UxRTJzLkpCtVEvOiCwTR?= MmHoNVk6OTN7M{W=
Hep3B NVPWcVNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PGclAvO+LCk{GwNFDDqG6P MmP4O|IhcA>? MVLFR|UxRTdwNtMxNU4zKG6P M4DtblE6QTF|OUO1
HepG2 MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3uU44xNjQkgKOxNFAxyqCwTR?= MnrWO|IhcA>? NWnQbW5HTUN3ME2xOE44yrFzLkegcm0> NHz3dIwyQTlzM{mzOS=>
Ramos M1vrXWFxd3C2b4Ppd{BCe3OjeR?= NEnQeGEzPS93MD:xNFAhdk1? NVXae4UyPDhiaB?= NYXwOI5tcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ NWK0blBzOTl6MkOxOlg>
Daudi  NUHaT5dHSXCxcITvd4l{KEG|c3H5 MUOyOU82OC9zMECgcm0> MXW0PEBp M1fP[olv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> NF\Zd4cyQTh{M{G2PC=>
BALM-14 MUPBdI9xfG:|aYOgRZN{[Xl? MX[xNk42NzJ3L{WwJI5O NVfBWYVuPDhiaB?= NEDzOXpqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NYGxe3QxOTl6MkOxOlg>
BALM-27 MV\BdI9xfG:|aYOgRZN{[Xl? MXOxNk42NzJ3L{WwJI5O M17IflQ5KGh? MXzpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NHi2XGYyQTh{M{G2PC=>
NB4 NGLpXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfLSpVtOC5yMT:wMlEwOSEQvF2= NHnMWHA1QCCq MVzpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NGnib4kyQDN4N{S4OC=>

... 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 3年-20℃
2年-80℃in solvent
別名 INH 34
溶解度 (25°C) * In vitro DMSO 102 mg/mL (200.96 mM)
Ethanol 3 mg/mL (5.91 mM)
Water <1 mg/mL
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

文献中の引用 (23)

Frequently Asked Questions

  • Question 1
    Can you let me know what solvent I can use for Barasertib, cat # S1147, for in vivo use? (IP injection in mice)

    Answer: S1147 Barasertib (AZD1152-HQPA) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30mg/ml as a clear solution. Usually, when prepare the solution, we will add organic solvents first, then add Tween 80, then water. But this compound can not dissolve in 30% PEG400/0.5% Tween80/5% Propylene glycol clearly. After water was added, it became a clear solution.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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