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

高品質保証

カスタマーフィードバック(8)

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 M{i3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S2fVAuPTByIH7N MmjpOFjDqGh? NYDuO4lMUUN3ME2yOUBvVQ>? MX2yOVI4PzZ3OR?=
LNCaP NYe4V|h3SXCxcITvd4l{KEG|c3H5 NXXiXJVwOC13MECgcm0> NGjQSZY1QMLiaB?= M4Hsd4lv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIghfGi{b4XnbEBk[XOyYYPlMVMhfXC{ZXf1cIF1cW:w NX:1PZlIOjV{N{e2OVk>
LNCaP MXjGeY5kfGmxbjDBd5NigQ>? NX7SbHFMPTBibl2= NH7K[nI1QCCq MUfpcoR2[2W|IH3pZ5JwdnWlbHXpJJdqfGhiYX7leYdmdmmlIH3lZ4hidmm|bR?= M{XsPVI2Ojd5NkW5
Ramos NHXHXWtHfW6ldHnvckBCe3OjeR?= NWPGR2E2PTByIH7N MXmwMVczKGh? MYrpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? NFfwVJEzOTN5MUS0Oi=>
Daudi  M1rkdmZ2dmO2aX;uJGF{e2G7 NU\UcoZoPTByIH7N NF\LSXIxNTd{IHi= MkjQbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn NHfGfXUzOTN5MUS0Oi=>
L540 MoiySpVv[3Srb36gRZN{[Xl? NIHGS4U2ODBibl2= NITLbY0xNTd{IHi= NFXvPJhqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= MmKyNlE{PzF2NE[=
BJAJ NH;Pe2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu2e2JEPTByIH7N M3HmfFAuPzJiaB?= MWHpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M3TCdlIyOzdzNES2
Ramos NI\PS3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX34eHhqPTByIH7N M1zEb|AuPzJiaB?= NHS5boNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NX;RZWxLOjF|N{G0OFY>
Raji NIjjWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDJOVAxKG6P NV\aS5RZOC15MjDo NFnIVnpqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M1;1WFIyOzdzNES2
Daudi  NIT6O29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LQXFUxOCCwTR?= M2\rXVAuPzJiaB?= Mn3RbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NVnw[W5lOjF|N{G0OFY>
L428 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLKcmJzPTByIH7N NYPvNZJkOC15MjDo NUjaXJZzcW6qaXLpeJMh[2WubDDndo94fGh? MkHNNlE{PzF2NE[=
KM-H2 M1TkfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7IOGp3PTByIH7N NFfiOHYxNTd{IHi= MmPrbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NYG1VHVbOjF|N{G0OFY>
HDLM-2 NYjHVII3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7WOVAxKG6P MoXtNE04OiCq NGCxUFNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4PkNFIyOzdzNES2
L450 NHPVSnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV61NFAhdk1? NYDQZlRzOC15MjDo M2j4folvcGmkaYTzJINmdGxiZ4Lve5Rp MnTBNlE{PzF2NE[=
BJAJ MXLBdI9xfG:|aYOgRZN{[Xl? NYO4bJFRPTByIH7N NILFc2sxNTd{IHi= MluxbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MlrFNlE{PzF2NE[=
Ramos M3yzSmFxd3C2b4Ppd{BCe3OjeR?= M4X3bFUxOCCwTR?= MWewMVczKGh? MV;pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NGrnfJYzOTN5MUS0Oi=>
Raji Mmm4RZBweHSxc3nzJGF{e2G7 M2T2[VUxOCCwTR?= MV2wMVczKGh? NUDiXmJJcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MlTMNlE{PzF2NE[=
Daudi  NWG0PG5nSXCxcITvd4l{KEG|c3H5 NV3CfGZUPTByIH7N NYrocppGOC15MjDo MX\pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MmTSNlE{PzF2NE[=
L428 NEjMZplCeG:ydH;zbZMhSXO|YYm= MUG1NFAhdk1? MUSwMVczKGh? NXvPbWdicW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NVnO[3Y1OjF|N{G0OFY>
KM-H2 NEDhWIpCeG:ydH;zbZMhSXO|YYm= NGXI[XY2ODBibl2= NHPIfFgxNTd{IHi= MX3pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MmHVNlE{PzF2NE[=
HDLM-2 NYDxU|B7SXCxcITvd4l{KEG|c3H5 M13DUlUxOCCwTR?= MoTFNE04OiCq M{jRbYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NES0TnAzOTN5MUS0Oi=>
L450 MlPHRZBweHSxc3nzJGF{e2G7 Mn7LOVAxKG6P NV\Zfow2OC15MjDo MVXpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M4jDVlIyOzdzNES2
SW620 NYnxfWcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDmfYs6TUN3ME2xNOKyOi5zIH7N NGPTSWozOTJ2NUC5NC=>
HCT116 NWPrSnNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnYbldVTUN3ME2xNeKyOy5|IH7N NIHFT3AzOTJ2NUC5NC=>
MDA-MB-435 NWW0R|J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWH3WpRmOC1zMECwNEBvVQ>? NWHvOWVJOi13IHS= MVPEUXNQ MmLiTWM2OD1zMkWgcm0> MYqyNFE4PTl{Nh?=
MDA-MB-468 NFz2XJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSwMVExODByIH7N MVmyMVUh\A>? MXPEUXNQ NXLod5RUUUN3ME2xOEBvVQ>? MkK4NlAyPzV7Mk[=
MDA-MB-231 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS2WGsxNTFyMECwJI5O MmnHNk02KGR? NVvhZVZOTE2VTx?= M1fhUmlEPTB;MUC1JI5O M2HB[FIxOTd3OUK2
BT474 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfLPVExNTFyMECwJI5O NE\kNnczNTViZB?= MmXHSG1UVw>? M3\yS2lEPTB;ODDuUS=> M330[lIxOTd3OUK2
MDA-MB-361 NFXqeGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;JRlAuOTByMECgcm0> MXiyMVUh\A>? M2TxTGROW09? M3HnS2lEPTB;N{Cgcm0> NWnnd4dbOjBzN{W5NlY>
HER18 MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33LeFAuOTByMECgcm0> MXqyMVUh\A>? MV3EUXNQ NIDDSoRKSzVyPUKwJI5O NXn2S49qOjBzN{W5NlY>
HER18 NHfXVWNCeG:ydH;zbZMhSXO|YYm= NXyySJFEOTByIH7N NELoNIYxNzJ2L{S4JIg> NHv6R4NFVVOR NETtRZpqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NVvaOoxMOjBzN{W5NlY>
MDA-MB-231 MmW4RZBweHSxc3nzJGF{e2G7 M3LrRlExPSCwTR?= MXGwM|I1NzR6IHi= NX2xO|V4TE2VTx?= MmHnbY5lfWOnczDhdI9xfG:|aYOgZY5lKHKnZIXj[ZMh[2yxbn;n[Y5q[yCyb4TlcpRq[Wx? MWWyNFE4PTl{Nh?=
JHH-1 NG\4ZldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS5NE4{6oDVMUCwNOKhdk1? MXq3NkBp NV:xSppITUN3ME2xO{41yrFzLkCgcm0> NX3lUVVpOTl7MUO5N|U>
JHH-2 NFG2cnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnpNE4{6oDVMUCwNOKhdk1? MYC3NkBp MXrFR|UxRTJzOD6wxtEyOC56IH7N NFn2XHYyQTlzM{mzOS=>
JHH-4 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrmd|ExNjQkgKOxNFAxyqCwTR?= MoDhO|IhcA>? MnnXSWM2OD1zNUWuOuKyOTZwODDuUS=> NETDUHYyQTlzM{mzOS=>
HuH-1 M2LLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PZe|AvO+LCk{GwNFDDqG6P M161[|czKGh? NH\3W2JGSzVyPUK3MlPDuTVwMDDuUS=> NWDIXXMzOTl7MUO5N|U>
HuH-6 M3TRTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHIeogxNjQkgKOxNFAxyqCwTR?= MXK3NkBp MnfOSWM2OD1|LkhCtVAvPiCwTR?= M{XOPFE6QTF|OUO1
HuH-7 M2K3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2wMlPjiJNzMECwxsBvVQ>? MlTUO|IhcA>? Mm\uSWM2OD14LklCtVAvOyCwTR?= MUexPVkyOzl|NR?=
HLE M4G0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXzNE4{6oDVMUCwNOKhdk1? M3LZZ|czKGh? NWXmWW1ITUN3ME20OU46yrF4LkSgcm0> MmKwNVk6OTN7M{W=
HLF MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[wMlPjiJNzMECwxsBvVQ>? NGnkOpY4OiCq MVrFR|UxRTF{Nj6xxtEyOi5{IH7N NUGzU|lqOTl7MUO5N|U>
PLC/PRF/5 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqwMlPjiJNzMECwxsBvVQ>? M2G4d|czKGh? NV[0U3FuTUN3ME23Ok46yrF7Lkmgcm0> NEnnPZQyQTlzM{mzOS=>
SK-Hep1 M{HG[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zjblAvO+LCk{GwNFDDqG6P M1HQe|czKGh? NHznUppGSzVyPUKxMlnDuTFwMjDuUS=> NXm3cHZpOTl7MUO5N|U>
Hep3B MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L5SVAvO+LCk{GwNFDDqG6P M{HlWFczKGh? MoPrSWM2OD15LkdCtVEvOiCwTR?= MVyxPVkyOzl|NR?=
HepG2 NVvDSFd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWwMlPjiJNzMECwxsBvVQ>? MnqyO|IhcA>? NWHI[2J6TUN3ME2xOE44yrFzLkegcm0> Mn7lNVk6OTN7M{W=
Ramos MXHBdI9xfG:|aYOgRZN{[Xl? MnLxNlUwPTBxMUCwJI5O M1jFbVQ5KGh? MnzEbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz NFP6eGQyQTh{M{G2PC=>
Daudi  MV\BdI9xfG:|aYOgRZN{[Xl? NYjme4VwOjVxNUCvNVAxKG6P M4HCVFQ5KGh? NHWyWVhqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NEC1cHUyQTh{M{G2PC=>
BALM-14 NETo[GZCeG:ydH;zbZMhSXO|YYm= NInaNlQyOi53L{K1M|UxKG6P NWjlbFIxPDhiaB?= NX;ORoZncW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MYWxPVgzOzF4OB?=
BALM-27 NHvzfZlCeG:ydH;zbZMhSXO|YYm= M2DsNVEzNjVxMkWvOVAhdk1? NXvTU4p[PDhiaB?= MW\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= MWCxPVgzOzF4OB?=
NB4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUewMlAyNzBwMT:xJO69VQ>? Mnm1OFghcA>? NIPJT3ZqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NIDEdpcyQDN4N{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 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

文献中の引用 (23)

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。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related オーロラ・キナーゼ 阻害剤

  • Ro-3306

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • CCG-1423

    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。

最近チェックしたアイテム

Tags: Barasertib (AZD1152-HQPA)を買う | Barasertib (AZD1152-HQPA)供給者 | Barasertib (AZD1152-HQPA)を購入する | Barasertib (AZD1152-HQPA)費用 | Barasertib (AZD1152-HQPA)生産者 | オーダーBarasertib (AZD1152-HQPA) | Barasertib (AZD1152-HQPA)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ