Barasertib (AZD1152-HQPA)

For research use only. Not for use in humans.

目录号:S1147 别名: AZD2811 中文名称:巴拉塞替

Barasertib (AZD1152-HQPA) Chemical Structure

CAS No. 722544-51-6

Barasertib (AZD1152-HQPA, AZD2811) 是一种高度选择性的Aurora B抑制剂,无细胞试验中IC50为0.37 nM,作用于Aurora B比作用于Aurora A选择性高3700倍左右。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1375.46 现货
RMB 976.12 现货
RMB 1718.83 现货
RMB 5477.43 现货
RMB 7944.3 现货
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客户使用Selleck生产的Barasertib (AZD1152-HQPA)发表文献76篇:

产品安全说明书

Aurora Kinase抑制剂选择性比较

生物活性

产品描述 Barasertib (AZD1152-HQPA, AZD2811) 是一种高度选择性的Aurora B抑制剂,无细胞试验中IC50为0.37 nM,作用于Aurora B比作用于Aurora A选择性高3700倍左右。
靶点
Aurora B [1]
(Cell-free assay)
0.37 nM
体外研究

AZD1152作用于Aurora B比作用于Aurora A选择性高3000多倍,IC50为1.368 μM。AZD1152作用于50种其他丝-苏氨酸和酪氨酸激酶,包括FLT3, JAK2, 和 Abl活性更低。AZD1152 抑制造血恶性细胞增殖,如HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, 和K562细胞,IC50为3-40 nM,效果比另一种Aurora激酶抑制剂ZM334739高100多倍,IC50为3-30 μM。AZD1152抑制MOLM13和MV4-11细胞克隆生长,IC50分别为1 nM和2.8 nM,也抑制新分离的抗Imatinib的白血病细胞,IC50 为1-3 nM, 比作用于骨髓单核细胞更有效,IC50>10 nM。AZD1152 诱导携带 4N/8N DNA的细胞累积,随后凋亡,这种作用存在剂量和时间依赖性。 [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCaP M{HESmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;ORVAuPTByIH7N MUW0POKhcA>? MlLwTWM2OD1{NTDuUS=> M2LCWlI2Ojd5NkW5
LNCaP NVz6Nnl6SXCxcITvd4l{KEG|c3H5 NIj3cXgxNTVyMDDuUS=> NW\D[nlYPDkEoHi= M3rC[Ilv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIghfGi{b4XnbEBk[XOyYYPlMVMhfXC{ZXf1cIF1cW:w NGfyTZEzPTJ5N{[1PS=>
LNCaP MnHXSpVv[3Srb36gRZN{[Xl? MV21NEBvVQ>? M4TQe|Q5KGh? MorEbY5lfWOnczDtbYNzd263Y3zlbUB4cXSqIHHu[ZVo\W6rYzDt[YNp[W6rc32= MYmyOVI4PzZ3OR?=
Ramos NUjQUGxxTnWwY4Tpc44hSXO|YYm= NXexSY05PTByIH7N NVHjV5FxOC15MjDo Mo\YbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn MVmyNVM4OTR2Nh?=
Daudi  NWm3doF[TnWwY4Tpc44hSXO|YYm= Mn3COVAxKG6P MY[wMVczKGh? MnzxbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn NUjhdo01OjF|N{G0OFY>
L540 M4PVb2Z2dmO2aX;uJGF{e2G7 M332Z|UxOCCwTR?= NH61R2cxNTd{IHi= NXixbJc1cW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl NWC4c|JoOjF|N{G0OFY>
BJAJ MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:5ZXNwPTByIH7N NWS1clg3OC15MjDo MUPpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M{jsO|IyOzdzNES2
Ramos MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;RNWw2ODBibl2= M3TtTlAuPzJiaB?= NVfGUHNmcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MlzrNlE{PzF2NE[=
Raji NW\B[4pRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPaOVAxKG6P M1e3WlAuPzJiaB?= M1vhNolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MYeyNVM4OTR2Nh?=
Daudi  Ml;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITwfJE2ODBibl2= Mnv6NE04OiCq MnnkbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NVKwVYlIOjF|N{G0OFY>
L428 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W3fFUxOCCwTR?= MmrjNE04OiCq NHfT[XlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M1fKS|IyOzdzNES2
KM-H2 NH3FR41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli0OVAxKG6P NUG3eFJyOC15MjDo MnfEbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NFXZSowzOTN5MUS0Oi=>
HDLM-2 NUHUTJp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUi1NFAhdk1? MnXuNE04OiCq NV7hWoQ{cW6qaXLpeJMh[2WubDDndo94fGh? NVjnW3RVOjF|N{G0OFY>
L450 NInZ[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzJN|A2ODBibl2= MXOwMVczKGh? NYf4SFJXcW6qaXLpeJMh[2WubDDndo94fGh? MkHoNlE{PzF2NE[=
BJAJ Mkf4RZBweHSxc3nzJGF{e2G7 NFLWS4Q2ODBibl2= NVXDXW9ROC15MjDo NYHybJBXcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MVqyNVM4OTR2Nh?=
Ramos M3zHSWFxd3C2b4Ppd{BCe3OjeR?= NFjCd|Q2ODBibl2= NIToZ2gxNTd{IHi= NYTP[FZ3cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> Mnz2NlE{PzF2NE[=
Raji NH\TbHJCeG:ydH;zbZMhSXO|YYm= NWHkd2J{PTByIH7N MWGwMVczKGh? MVLpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NVHTWFRxOjF|N{G0OFY>
Daudi  Ml7SRZBweHSxc3nzJGF{e2G7 NYrQblNpPTByIH7N MnTtNE04OiCq M4\QdIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NEKzXpozOTN5MUS0Oi=>
L428 MUHBdI9xfG:|aYOgRZN{[Xl? M1TYTFUxOCCwTR?= NEL5XoQxNTd{IHi= M{nSSIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NVLoOFZyOjF|N{G0OFY>
KM-H2 MlTKRZBweHSxc3nzJGF{e2G7 M2HscFUxOCCwTR?= MmTWNE04OiCq NF63NJhqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NH;0fIUzOTN5MUS0Oi=>
HDLM-2 MYnBdI9xfG:|aYOgRZN{[Xl? M1nIOlUxOCCwTR?= MkfyNE04OiCq NXrkd|B1cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NYO4VYxYOjF|N{G0OFY>
L450 NGLnUIpCeG:ydH;zbZMhSXO|YYm= MYS1NFAhdk1? MoTaNE04OiCq M3vTUIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MY[yNVM4OTR2Nh?=
SW620 NWTTe2V7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3BSWM2OD1zMNMxNk4yKG6P MWqyNVI1PTB7MB?=
HCT116 M1LifGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHhSWM2OD1zMdMxN{4{KG6P MYOyNVI1PTB7MB?=
MDA-MB-435 M1q2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXqwMVExODByIH7N NX7wcWU1Oi13IHS= MXnEUXNQ Mm[3TWM2OD1zMkWgcm0> MlrKNlAyPzV7Mk[=
MDA-MB-468 NYSyWGtQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PXNlAuOTByMECgcm0> NWPTSXp7Oi13IHS= MX\EUXNQ MnXyTWM2OD1zNDDuUS=> NIG5TJYzODF5NUmyOi=>
MDA-MB-231 NGL4fo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13zeVAuOTByMECgcm0> M2q1XVIuPSCm NHXVc3lFVVOR M2fnTmlEPTB;MUC1JI5O M1vn[VIxOTd3OUK2
BT474 NWS5c5NrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj2U2YxNTFyMECwJI5O M3;OXlIuPSCm MXHEUXNQ MUfJR|UxRThibl2= M3zHPFIxOTd3OUK2
MDA-MB-361 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\OV44xNTFyMECwJI5O M33kUVIuPSCm MkjVSG1UVw>? M3HDemlEPTB;N{Cgcm0> NIL3eWEzODF5NUmyOi=>
HER18 M2HkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLkboIxNTFyMECwJI5O MoTUNk02KGR? MWfEUXNQ MVzJR|UxRTJyIH7N MVmyNFE4PTl{Nh?=
HER18 MlLQRZBweHSxc3nzJGF{e2G7 M1;CTVExOCCwTR?= Ml7ZNE8zPC92ODDo M{HmfWROW09? Mn\MbY5lfWOnczDhdI9xfG:|aYOgZY5lKHKnZIXj[ZMh[2yxbn;n[Y5q[yCyb4TlcpRq[Wx? MXmyNFE4PTl{Nh?=
MDA-MB-231 NWHud3NzSXCxcITvd4l{KEG|c3H5 MnTRNVA2KG6P MWKwM|I1NzR6IHi= MnLlSG1UVw>? NGDuU4hqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= MlPkNlAyPzV7Mk[=
JHH-1 NFvmbXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXOT494OC5|4pETNVAxOMLibl2= M2jW[|czKGh? MkSxSWM2OD1zNz60xtEyNjBibl2= M{T4cVE6QTF|OUO1
JHH-2 NU\MW21RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHtNE4{6oDVMUCwNOKhdk1? MWG3NkBp MmntSWM2OD1{MUiuNOKyOTBwODDuUS=> NXLlW4p5OTl7MUO5N|U>
JHH-4 NH\Ge3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvYSIRsOC5|4pETNVAxOMLibl2= M1v5XlczKGh? NVzE[G5ZTUN3ME2xOVUvPsLzMU[uPEBvVQ>? NYnEe4gxOTl7MUO5N|U>
HuH-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HuWFAvO+LCk{GwNFDDqG6P NHLYZnY4OiCq NUD0ZpRyTUN3ME2yO{4{yrF3LkCgcm0> MUexPVkyOzl|NR?=
HuH-6 NYnkWXJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XtWlAvO+LCk{GwNFDDqG6P MWS3NkBp NXOwUlJnTUN3ME2zMlfDuTBwNjDuUS=> NITNTosyQTlzM{mzOS=>
HuH-7 M{LCOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjibFZwOC5|4pETNVAxOMLibl2= M3nyVFczKGh? NH\YNW5GSzVyPU[uPOKyOC5|IH7N MV2xPVkyOzl|NR?=
HLE MkLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj2NE4{6oDVMUCwNOKhdk1? NWjTbJJtPzJiaB?= MUjFR|UxRTR3LkpCtVYvPCCwTR?= NW\VSVJtOTl7MUO5N|U>
HLF NGrtU|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1y5e|AvO+LCk{GwNFDDqG6P M{fHeVczKGh? MmTCSWM2OD1zMk[uNeKyOTJwMjDuUS=> MVKxPVkyOzl|NR?=
PLC/PRF/5 NVrxcXhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\XNE4{6oDVMUCwNOKhdk1? MXG3NkBp MYTFR|UxRTd4LkpCtVkvQSCwTR?= MWmxPVkyOzl|NR?=
SK-Hep1 NHfr[3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jUeVAvO+LCk{GwNFDDqG6P NYDuT25{PzJiaB?= NVXoWWJzTUN3ME2yNU46yrFzLkKgcm0> M{LPXlE6QTF|OUO1
Hep3B MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfUem9ROC5|4pETNVAxOMLibl2= MX23NkBp M3fEcGVEPTB;Nz62xtEyNjJibl2= MY[xPVkyOzl|NR?=
HepG2 NUnjW3RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP5NE4{6oDVMUCwNOKhdk1? Mkm3O|IhcA>? M1\CZWVEPTB;MUSuO:KyOS55IH7N MWixPVkyOzl|NR?=
Ramos MoPDRZBweHSxc3nzJGF{e2G7 NUPQXnU1OjVxNUCvNVAxKG6P MUO0PEBp NUnNZZJrcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ NWTGbopSOTl6MkOxOlg>
Daudi  NVm0c4VDSXCxcITvd4l{KEG|c3H5 MUmyOU82OC9zMECgcm0> MYe0PEBp M1LXSolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> MYSxPVgzOzF4OB?=
BALM-14 M1nFeGFxd3C2b4Ppd{BCe3OjeR?= NUH3OG1LOTJwNT:yOU82OCCwTR?= MmrGOFghcA>? NYXKVIFTcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M4LnT|E6QDJ|MU[4
BALM-27 MmfmRZBweHSxc3nzJGF{e2G7 Mm\5NVIvPS9{NT:1NEBvVQ>? MmT4OFghcA>? MYTpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NXvaR4Y{OTl6MkOxOlg>
NB4 MkPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[3XYsxNjBzL{CuNU8yKM7:TR?= MlvEOFghcA>? NIm2eoxqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NWXZR5I2OTh|Nke0PFQ>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AURKB / pSer10 Histone H3 / TP53 / CDKN1A / MYCN; 

PubMed: 26497213     


Downstream effects of barasertib-induced AURKB inhibition on histone H3 phosphorylation and TP53 protein levels in IMR5 and SK-N-BE (2c) as indicated after 24h (left) and 48h (right). TP53 and its downstream effector CDKN1A were up-regulated by barasertib䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

p53 / p21 / p-p38 / p38 ; 

PubMed: 24782314     


U2OS cells were treated with 50 nm or 100 nm AZD1152 for 24 h. p21, p38, p-p38, and p53 levels were determined by immunoblotting β-actin served as a loading control.

26497213 24782314
Immunofluorescence
p21 ; 

PubMed: 24782314     


U2OS cells were treated as in H. Levels of p21 were analyzed by immunostaining. DNA was counterstained with Hoechst 33258.

24782314
Growth inhibition assay
Cell viability ; 

PubMed: 26497213     


Dose response curves to barasertib at 72h of incubation normalized to the DMSO control sample (mean ± SD, n = 5). The inset depicts the normalized AUCs of each response curve. 

26497213
体内研究 AZD1152 按25 mg/kg剂量单独处理MOLM13移植瘤,显著抑制肿瘤生长,平均肿瘤体积从1261 mm3 降低到 71 mm3,且平均肿瘤重量从583 mg降低到78 mg, 观察到坏死组织被吞噬细胞浸润。[1]此外, AZD1152 每天按10-150 mg/kg剂量处理多种人类实体移植瘤,包括 结肠癌,乳腺癌,和肺癌,显著抑制肿瘤生长,这种作用存在剂量依赖性。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: HL-60, NB4, MOLM13, PALL-2, MV4-11, EOL-1,和 K562
  • Concentrations: 溶于 DMSO, 终浓度为~100 nM
  • Incubation Time: 24或48小时
  • Method: 使用不同浓度AZD1152处理细胞 24或 48小时。通过测量 3H-胸甘摄取(在收集前6小时,加入同位素)而测量细胞增殖,根据剂量-反应曲线计算IC50值。通过流式细胞仪分析细胞周期。通过膜联蛋白V–FITC凋亡检测试剂盒测量细胞凋亡。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 皮下注射MOLM13细胞的雌性免疫缺陷BALB/c裸鼠
  • Dosages: 5 或25 mg/kg
  • Administration: 腹腔注射,每周4次,或每隔一天一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 102 mg/mL (200.96 mM)
Ethanol 3 mg/mL (5.91 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
7mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 507.56
化学式

C26H30FN7O3

CAS号 722544-51-6
储存条件 粉状
溶于溶剂
别名 AZD2811

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID