Birinapant

目录号:S7015 别名: TL32711

Birinapant Chemical Structure

Molecular Weight(MW): 806.94

Birinapant是一种SMAC模拟拮抗剂,对cIAP1最有效,无细胞试验中Kd为<1 nM,对XIAP作用较弱。Phase 2。

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产品安全说明书

IAP抑制剂选择性比较

生物活性

产品描述 Birinapant是一种SMAC模拟拮抗剂,对cIAP1最有效,无细胞试验中Kd为<1 nM,对XIAP作用较弱。Phase 2。
靶点
cIAP1 [1]
(Cell-free assay)
XIAP [1]
(Cell-free assay)
<1 nM(Kd) 45 nM(Kd)
体外研究

Birinapant与XIAP和CIAP1结合的Kd分别为45 nM和 <1 nM。在TRAIL不敏感的SUM190(ErbB2的过度表达)细胞中,Birinapant独自诱导细胞死亡(IC 50约为300 nM),并显著增加TRAIL诱导的TRAIL敏感SUM149(三阴性,EGFR活化)细胞的凋亡。 Birinapant导致CIAP1迅速降解,caspase活化,PARP裂解,和NF-κB的激活。[1] Birinapant与TNF-α联用表现出强烈的体外抗黑素瘤作用。 Birinapant和TNF-α(1 ng/mL)联用抑制人黑素瘤细胞系WTH202,WM793B,WM1366和WM164生长,IC50分别为1.8,2.5,7.9和9 nM,而两种化合物单独都无效。Birinapant单独处理可诱导对WM9细胞增殖的抑制作用,IC 50为2.4 nM。Birinapant显著抑制这些细胞系中靶蛋白CIAP1和cIAP2。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC-1 NX\MeZFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rtOFUxNzJyMD:1NFAhdk1? NFKxbHgxNTl4IHi= MkLvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NX7McYZ6OjZ{NUK5Olk>
Molm13  MXTGeY5kfGmxbjDBd5NigQ>? NHLibYgzNzJyL{KwNEBvVQ>? MYCyOEBp NHHHOW5l\WO{ZXHz[ZMh[0mDUEGgZY5lNCC2bzDhJI12[2hibHXzd4VzKGW6dHXueEwh[0mDUEKsJIFv\CC[SVHQJJVv\GW{II\hdolwfXNiY3;u[Il1cW:wcx?= NE[xeJEzPDV{Nke4Oy=>
WTH202 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV63NkBp NV;YOYlKUUN3ME2xMlghdk1uIHPvcYJqdmWmIIfpeIghOW6pL33sJHRPTi4QsR?= M2XtSFI{PDB|NkO0
WM793B M{D4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7vO|IhcA>? NXjuUFNTUUN3ME2yMlUhdk1uIHPvcYJqdmWmIIfpeIghOW6pL33sJHRPTi4QsR?= M{SwS|I{PDB|NkO0
WM9 NGfs[3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;GUIU4OiCq MnTUTWM2OD1{LkSgcm0> M3PpZ|I{PDB|NkO0
WM9 NG[x[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vLdlczKGh? MnrzTWM2OD1{Lkegcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? NYTYSG1EOjN2MEO2N|Q>
WM1366 M1;4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLBdlI4OiCq MmPNTWM2OD15Lkmgcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? NGXKdnIzOzRyM{[zOC=>
WM164 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTEWZA4OiCq NUjzcoF3UUN3ME25JI5ONCClb33ibY5m\CC5aYToJFFv\y:vbDDUUmYu|rF? NUCxT4NIOjN2MEO2N|Q>
451Lu NHjldYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLrNpE4OiCq NVfBV|FCUUN3ME2xOE4zKG6PLDDjc41jcW6nZDD3bZRpKDGwZz;tcEBVVkZvzsG= NF\lN|AzOzRyM{[zOC=>
WM1341D NWDsTodYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjWb3B6PzJiaB?= MWXJR|UxRTV5Lk[gcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? MXSyN|QxOzZ|NB?=
WM3130 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYi3NkBp M2jxcGlEPTB;NkSuN{BvVSxiY3;tZolv\WRid3n0bEAydmdxbXygWG5HNc7z Mn;oNlM1ODN4M{S=
WM1985 MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NImwcJM4OiCq MofYTWM2OD17NzDuUUwh[2:vYnnu[YQhf2m2aDCxcocwdWxiVF7GMe6y M3:ySVI{PDB|NkO0
WM3854 M3;p[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjVO|IhcA>? MkfHTWM2OD1{Mk[gcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? MXqyN|QxOzZ|NB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cIAP1 / cIAP2 / XIAP; 

PubMed: 24526787     


Molm13 cells were cultured under standard conditions, standard conditions with mesenchymal stromal cell (MSC) coculture, or hypoxic conditions without or with MSC coculture and treated with birinapant. cIAP1, cellular inhibitor of apoptosis protein-2 (cIAP2), and X-linked inhibitor of apoptosis protein (XIAP) levels were determined by Western blot at 24 hours.

NF-κB(p65) / IκBa / Bcl-xl / NF-κB(p100) / p52; 

PubMed: 24526787     


OCI-AML3 cells were treated with birinapant (bir) for 24 hours. Protein levels in total cell lysates were determined by western blot.

BIRC2 / ARC; 

PubMed: 25079338     


Birinapant treatment decreases BIRC2 and increases ARC protein levels in AML cells and MSCs. OCI-AML3 and Molm13 cells were co-cultured with mesenchymal stem cells (MSCs) and treated with birinapant (bir). Cell lysates from OCI-AML3 and Molm13 cells were collected at 48 and 72 h by combining unattached cells and cells washed off from MSCs; lysates of MSCs were obtained from MSCs co-cultured with Molm13 cells after washing off Molm13 cells. The protein levels were determined by Western blot.

24526787 25079338
Immunofluorescence
Caspase 3/7; 

PubMed: 28665401     


MC38-Ova cells were seeded in chamber slides then overlaid with Pfn−/− OT-I T cells. After 8 h, cells were fixed, stained as indicated, then visualized by confocal microscopy. A minimum of 50 cells was counted in each condition. Error bars represent the mean±S.E.M. of triplicate determinations from a representative experiment, *P<0.05 by unpaired Student's t test.

28665401
Growth inhibition assay
Cell viability; 

PubMed: 28460471     


Cell viability was determined by CCK-8 assay. The data are representative results of three independent experiments.

28460471
体内研究 Birinapant(30毫克/千克)显著诱导恶性黑色素瘤异种移植模型451LU的肿瘤生长。[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)

激酶实验:[1]
- 合并

荧光偏振测定法:

和化合物XIAP和CIAP1的亲和力是使用荧光底物来确定,并以Kd值表示。最初,荧光标记的修饰的Smac肽(AbuRPF -K (5-FAM)-NH 2; FP肽)的解离常数(Kd)是用固定浓度(5 nM)的肽和滴定不同浓度的蛋白质(0.075-5μM的半对数稀释)来确定。剂量-反应曲线是在5nM FP肽和50nM XIAP检测中用GraphPad Prism的单点结合模型的非线性最小二乘法生产的。各种浓度的Smac模拟物(100-0.001 μM在半对数稀释)添加到FP肽/蛋白质二元复合物,在含有100毫克/毫升牛c-球蛋白0.1M磷酸钾缓冲液中室温处理15分钟。多标签读板器采用485 nm激发滤光片和520nm的发射滤光片测量偏振值。
细胞实验:[2]
- 合并
  • Cell lines: 人黑色素瘤细胞系WM9
  • Concentrations: 1 nM-1 μM
  • Incubation Time: 3 天
  • Method: 细胞附着24小时,随后与Birinapant和/或TNF-α孵育24或72小时。随后用MTS法检测。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 人黑色素瘤异种移植451LU
  • Formulation: 12.5%的Captisol在蒸馏水中
  • Dosages: 30 毫克/千克
  • Administration: 每周腹腔注射3次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (123.92 mM)
Ethanol 55 mg/mL (68.15 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):
15% Captisol
5 mg/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 806.94
化学式

C42H56F2N8O6

CAS号 1260251-31-7
储存条件 粉状
溶于溶剂
别名 TL32711

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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IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID