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 NVHIdVJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMVUxOCCwTR?= NF7zdI81QMLiaB?= M2jLbWlEPTB;MkWgcm0> M{HKNVI2Ojd5NkW5
LNCaP NGDqSXFCeG:ydH;zbZMhSXO|YYm= NGrqVFcxNTVyMDDuUS=> NUO2XGhkPDkEoHi= NFzte|BqdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKHSqcn;1[4gh[2G|cHHz[U0{KHWycnXneYxifGmxbh?= MUeyOVI4PzZ3OR?=
LNCaP MkOxSpVv[3Srb36gRZN{[Xl? NH\CPZM2OCCwTR?= M4f6WFQ5KGh? MlXrbY5lfWOnczDtbYNzd263Y3zlbUB4cXSqIHHu[ZVo\W6rYzDt[YNp[W6rc32= NEPsZlMzPTJ5N{[1PS=>
Ramos MoHxSpVv[3Srb36gRZN{[Xl? MljhOVAxKG6P MUOwMVczKGh? M3XreolvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= M3Pwc|IyOzdzNES2
Daudi  NIK5b2ZHfW6ldHnvckBCe3OjeR?= NE[3XVk2ODBibl2= MXewMVczKGh? M3riUIlvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= NYX3eVd2OjF|N{G0OFY>
L540 Ml3DSpVv[3Srb36gRZN{[Xl? MmDpOVAxKG6P M3Li[|AuPzJiaB?= NV\yWoNHcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl M1\6ZlIyOzdzNES2
BJAJ M3LM[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXNcVU2ODBibl2= MlzDNE04OiCq MYnpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NXPaXVR7OjF|N{G0OFY>
Ramos NYjhWZBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXRXmQ1PTByIH7N MXiwMVczKGh? NGSwcFhqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M2e2OlIyOzdzNES2
Raji M{fsU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jl[lUxOCCwTR?= NYH4[pREOC15MjDo MkX2bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M123elIyOzdzNES2
Daudi  M4m4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnjTlhDPTByIH7N M2D1TFAuPzJiaB?= MlPWbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MluxNlE{PzF2NE[=
L428 M3;R[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTCOVAxKG6P NYTC[XZ3OC15MjDo MXLpcohq[mm2czDj[YxtKGe{b4f0bC=> NFS3VYczOTN5MUS0Oi=>
KM-H2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljXOVAxKG6P MV:wMVczKGh? Mm\ybY5pcWKrdIOgZ4VtdCCpcn;3eIg> MlL3NlE{PzF2NE[=
HDLM-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzVUGlEPTByIH7N M3fzUFAuPzJiaB?= M{jhPYlvcGmkaYTzJINmdGxiZ4Lve5Rp NXfy[HJIOjF|N{G0OFY>
L450 NV63OI9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYq1NFAhdk1? MYqwMVczKGh? NVvKdlFycW6qaXLpeJMh[2WubDDndo94fGh? NV;VZXJlOjF|N{G0OFY>
BJAJ MYfBdI9xfG:|aYOgRZN{[Xl? NEXwVYc2ODBibl2= MoLoNE04OiCq M3rSR4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NGLLRpMzOTN5MUS0Oi=>
Ramos MmfWRZBweHSxc3nzJGF{e2G7 MVW1NFAhdk1? MmDWNE04OiCq MlXBbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= Mo\yNlE{PzF2NE[=
Raji MVHBdI9xfG:|aYOgRZN{[Xl? MXe1NFAhdk1? M{W0TlAuPzJiaB?= NGW4cYZqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M37tOlIyOzdzNES2
Daudi  MWDBdI9xfG:|aYOgRZN{[Xl? MVq1NFAhdk1? NWTTNnNWOC15MjDo M{nmZ4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M1fCc|IyOzdzNES2
L428 NHPNTXNCeG:ydH;zbZMhSXO|YYm= M1H6UVUxOCCwTR?= MYGwMVczKGh? M1LzTIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MUGyNVM4OTR2Nh?=
KM-H2 MlnxRZBweHSxc3nzJGF{e2G7 M3rQclUxOCCwTR?= NGP4R5IxNTd{IHi= NUjibXpwcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> M{XzfFIyOzdzNES2
HDLM-2 M2j6dmFxd3C2b4Ppd{BCe3OjeR?= NVLMcmpjPTByIH7N NWXFfWs4OC15MjDo MnTVbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M2\hOVIyOzdzNES2
L450 M3LKTGFxd3C2b4Ppd{BCe3OjeR?= MlzaOVAxKG6P NH;vbZMxNTd{IHi= NEfpc5hqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NU\HVGx4OjF|N{G0OFY>
SW620 NGDKeYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvQN4JNTUN3ME2xNOKyOi5zIH7N MY[yNVI1PTB7MB?=
HCT116 NGS3RpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDTSWM2OD1zMdMxN{4{KG6P MVGyNVI1PTB7MB?=
MDA-MB-435 M2Xp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUewMVExODByIH7N MWeyMVUh\A>? NX3kOY9rTE2VTx?= MYDJR|UxRTF{NTDuUS=> MWWyNFE4PTl{Nh?=
MDA-MB-468 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nrNVAuOTByMECgcm0> M1\oZVIuPSCm M2HBemROW09? M3jucGlEPTB;MUSgcm0> MYmyNFE4PTl{Nh?=
MDA-MB-231 NF\vemlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjaVmMxNTFyMECwJI5O MY[yMVUh\A>? M1HydWROW09? Mo\aTWM2OD1zMEWgcm0> NWHVfo9qOjBzN{W5NlY>
BT474 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2POTFAuOTByMECgcm0> NHfpRpIzNTViZB?= M{LyWmROW09? NX7vSW9LUUN3ME24JI5O MVeyNFE4PTl{Nh?=
MDA-MB-361 NWHaU3NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrldFN7OC1zMECwNEBvVQ>? MXWyMVUh\A>? MnzzSG1UVw>? MoXXTWM2OD15MDDuUS=> MXOyNFE4PTl{Nh?=
HER18 M4f2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHoNE0yODByMDDuUS=> MoTiNk02KGR? MmfzSG1UVw>? M1vRcWlEPTB;MkCgcm0> MUOyNFE4PTl{Nh?=
HER18 MkPORZBweHSxc3nzJGF{e2G7 MlXUNVAxKG6P MXmwM|I1NzR6IHi= NXflfod6TE2VTx?= NFXpT4tqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NUPXS|lJOjBzN{W5NlY>
MDA-MB-231 NEXHOppCeG:ydH;zbZMhSXO|YYm= MUexNFUhdk1? NXnlfph5OC9{ND:0PEBp MofqSG1UVw>? M4\lZ4lv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu Mlf4NlAyPzV7Mk[=
JHH-1 NWeyUolDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HKZlAvO+LCk{GwNFDDqG6P NVuwdY94PzJiaB?= MYXFR|UxRTF5LkVCtVEvOCCwTR?= MX:xPVkyOzl|NR?=
JHH-2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\5[lVFOC5|4pETNVAxOMLibl2= MmPtO|IhcA>? NVPxeoxYTUN3ME2yNVgvOMLzMUCuPEBvVQ>? M2T6PFE6QTF|OUO1
JHH-4 Mn3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIe2WHoxNjQkgKOxNFAxyqCwTR?= MknrO|IhcA>? MYXFR|UxRTF3NT62xtEyPi56IH7N NHXhcGMyQTlzM{mzOS=>
HuH-1 MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DvbFAvO+LCk{GwNFDDqG6P NWHROYdEPzJiaB?= NYXLNI5NTUN3ME2yO{4{yrF3LkCgcm0> MmLFNVk6OTN7M{W=
HuH-6 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuwMlPjiJNzMECwxsBvVQ>? NVe0V2Z6PzJiaB?= M17QVWVEPTB;Mz63xtExNjZibl2= MkPDNVk6OTN7M{W=
HuH-7 NHvSU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVKwMlPjiJNzMECwxsBvVQ>? NGnubFk4OiCq NFvpTZpGSzVyPU[uPOKyOC5|IH7N M{HteFE6QTF|OUO1
HLE M{DCVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPFSJExNjQkgKOxNFAxyqCwTR?= NG\aWZE4OiCq NVLpR29UTUN3ME20OU46yrF4LkSgcm0> NGXzNFMyQTlzM{mzOS=>
HLF MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TEOVAvO+LCk{GwNFDDqG6P M2nXb|czKGh? MlzoSWM2OD1zMk[uNeKyOTJwMjDuUS=> MVOxPVkyOzl|NR?=
PLC/PRF/5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3BNE4{6oDVMUCwNOKhdk1? Mlm5O|IhcA>? NGS3OoRGSzVyPUe2MlnDuTlwOTDuUS=> MnLTNVk6OTN7M{W=
SK-Hep1 M1nTdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVywMlPjiJNzMECwxsBvVQ>? NHK5cm44OiCq MWfFR|UxRTJzLkpCtVEvOiCwTR?= MWCxPVkyOzl|NR?=
Hep3B NEHVVnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXzd|IxNjQkgKOxNFAxyqCwTR?= Mm\lO|IhcA>? NHK5enpGSzVyPUeuOuKyOS5{IH7N NF24cpUyQTlzM{mzOS=>
HepG2 M{fWN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXsOIdGOC5|4pETNVAxOMLibl2= NIDIV2o4OiCq M{S2fGVEPTB;MUSuO:KyOS55IH7N MUKxPVkyOzl|NR?=
Ramos MVvBdI9xfG:|aYOgRZN{[Xl? M2LDZ|I2NzVyL{GwNEBvVQ>? NYL2bWtDPDhiaB?= NYnUVHlJcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ NGTwb|EyQTh{M{G2PC=>
Daudi  MY\BdI9xfG:|aYOgRZN{[Xl? M1fve|I2NzVyL{GwNEBvVQ>? M3nOflQ5KGh? M3K1NYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> MmfONVk5OjNzNki=
BALM-14 Ml20RZBweHSxc3nzJGF{e2G7 Mnq0NVIvPS9{NT:1NEBvVQ>? NWXObGp3PDhiaB?= MmnabY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz NXLQOHpWOTl6MkOxOlg>
BALM-27 M13EXmFxd3C2b4Ppd{BCe3OjeR?= MlTUNVIvPS9{NT:1NEBvVQ>? Ml;WOFghcA>? MYDpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NVHDVphROTl6MkOxOlg>
NB4 NXq4OoFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W2SlAvODFxMD6xM|Eh|ryP NX\EUGRzPDhiaB?= MUfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M2PReVE5OzZ5NEi0

... 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)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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