Napabucasin (BBI608)

For research use only. Not for use in humans.

目录号:S7977 别名: BBI608

Napabucasin (BBI608) Chemical Structure

CAS No. 83280-65-3

Napabucasin (BBI608) 是一种口服具有活性的Stat3和癌细胞多能性抑制剂。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 958.23 现货
RMB 957.38 现货
RMB 3261.41 现货
RMB 8169.42 现货
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客户使用Selleck生产的Napabucasin (BBI608)发表文献18篇:

产品安全说明书

STAT抑制剂选择性比较

生物活性

产品描述 Napabucasin (BBI608) 是一种口服具有活性的Stat3和癌细胞多能性抑制剂。
靶点
Stat3 [1]
体外研究

Napabucasin下调Stat3驱动的干细胞基因表达和癌症干细胞性能,并有效抑制高度多功能性癌细胞的自我更新,IC50范围为0.291~1.19 μM,而对正常干细胞没有抑制作用。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human DU145 cells M2rYRmZ2dmO2aX;uJIF{e2G7 M1KwT|czKGh? M3\aZWFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC3NkBpenNiYomgXHRVKGG|c3H5MEBKSzVyPUCuNFI{ODRizszN MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDh{OUOxOkc,OTh6MkmzNVY9N2F-
human HaCaT cells NFfmfXNHfW6ldHnvckBie3OjeR?= M4PWZlQ5KGh? NXfFS5h[SW62aXj5dIVzeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCyaHHz[UBkd262cnHzeEBucWO{b4Pjc5B6NCCLQ{WwQVAvPSEQvF2= Mn\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6NEWwNVQoRjJ{OES1NFE1RC:jPh?=
human HaCaT cells M13SSXBzd2yrZnXyZZRqd25iYYPzZZk> MlTURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKYVPhWEBk\WyuczygTWM2OD1yLkWg{txO NGTrXGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMES3PVMyQSd-MUC0O|k{OTl:L3G+
KB cells NFPuT45EgXSxdH;4bYNqfHliYYPzZZk> NWfUbHV5TW[oZXP0bZZmKGO7dH;0c5hq[yCmb4PlJIFo[Wmwc4SgT2Ih[2WubIOge4F{KGW4YXz1ZZRm\CxiRVS1NF01NjJizszN NYXKRoo{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUi3N|YyQCd-OUi3N|YyQDxxYU6=
MDA-MB-231 MoPvR5l1d3SxeHnjbZR6KGG|c3H5 M{LsV|czKGi{cx?= MlGxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4{PCEQvF2u NVrsOJA1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OVg{OzNpPkK4OVU5OzN|PD;hQi=>
HepG2 NGjVcI5EgXSxdH;4bYNqfHliYYPzZZk> NEH5RYw4OiCqcoO= NUHNfnIzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuOlYh|ryPLh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV3OEOzN{c,Ojh3NUizN|M9N2F-
A549 M{fsSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NXXUN|hDPzJiaILz MkPNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC55NDFOwG0v MnKyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3NUizN|MoRjJ6NUW4N|M{RC:jPh?=
K562 NYnkcGdvSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXy0PEBpenN? M2f4ZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDt[YF{fXKnZDDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMTFOwG0v MojVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMEO3O|goRjNyMECzO|c5RC:jPh?=
MDA-MB-231 M1LueWZ2dmO2aX;uJIF{e2G7 MmG0OEBpenN? M4TjTWlvcGmkaYTpc44hd2ZiU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KFl5MEWgbY4hcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icnH0bY8hd2ZicHjvd5Bpd3K7bHH0[YQhW1SDVEOgeI8hfG:2YXygV3RCXDNibHX2[Ywh[W[2ZYKgOEBpenNiYomgTHRTTiCjc4PhfUwhTUN3MDC9JFEvQSEQvF2u NVyzS4l[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 MULGeY5kfGmxbjDhd5NigQ>? NVPlU2FrPCCqcoO= MVfJcohq[mm2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhPCCqcoOgZpkhUFSURjDhd5NigSxiRVO1NEA:KDJizszNMi=> NV3ZVYRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 M3q1WWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4jXUlQ5KGi{cx?= M2XWb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCvZXHzeZJm\CCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOi5zIN88UU4> NEPYTWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwN|c4QCd-M{CwNFM4Pzh:L3G+
HepG2 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MYG0PEBpenN? MkfTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLMVgh[XO|YYmsJGlEPTBiPTCxNE4zKM7:TT6= NEPaN3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[wOFU1Oyd-Mkm2NFQ2PDN:L3G+
L02 NVTYZplHSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1HJcVQ5KGi{cx?= MlPGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOMEKgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iMUiuO{DPxE1w MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZyNEW0N{c,Ojl4MES1OFM9N2F-
MDA-MB-231 M{n3SWZ2dmO2aX;uJIF{e2G7 NXvkcZdOOTByIIXN MU[xJIhz Mli1Rolv\GmwZzDh[oZqdmm2eTD0c{BUXEGWMzDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFExOCC3TTD0doVifGWmIH\vdkAyKGi{IH\vcIxwf2WmIHL5JJRp\XKvb3z5d4lvKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhTEGUVGOtW4V{fGW{bjDicI91KGGwYXz5d4l{ NXniSXVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFM4PzhpPkOwNFA{Pzd6PD;hQi=>
MDA-MB-231 NVroVodOTnWwY4Tpc44h[XO|YYm= MnK5OUB2dW:uL1y= NGfNTHEzPCCqcoO= M1fpPGlv\HWldHnvckBw\iC|dYDldo95cWSnIHflcoVz[XSrb36gbY4hcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDheEA2KHWvb3yvUEBu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgSGhGKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 MkjIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMEO3O|goRjNyMECzO|c5RC:jPh?=
MDA-MB-231 MV\GeY5kfGmxbjDhd5NigQ>? MWC1JJVud2xxTB?= MlK0NlQhcHK| NHSzWWpKdmS3Y4Tpc44hd2Zic4Xw[ZJwgGmmZTDn[Y5memG2aX;uJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhPSC3bX;sM2whdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHnuJJBz\XOnbnPlJI9nKE6TT{GgbY5pcWKrdH;yJIRq[2:3bXHyc4wh[nliRFjFJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6 M1TrelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMECzO|c5Lz5|MECwN|c4QDxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CDK4 / Cyclin D1; 

PubMed: 31277685     


U87MG and LN229 cells were treated with the vehicle or 5 μM Napabucasin for 48 h. Then, cell lysates were analyzed by western blotting.

STAT3 / β-catenin / c-Myc; 

PubMed: 31277685     


GSCs (glioma stem cells) under the indicated conditions were harvested and subjected to western blotting. 

c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin; 

PubMed: 25605917     


FaDu cancer stem cells were treated for 3, 6, or 24 h with BBI608 at either 1 or 2 μM or with DMSO (0). Cell lysates from these treated cells were then analyzed by Western blotting. BBI608 down-regulates a number of stemness related proteins involved in t䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

31277685 25605917
Immunofluorescence
STAT3; 

PubMed: 31277685     


IF was used to estimate the expression of STAT3 in U87MG and LN229 cells after treatment with Napabucasin (scale bar: 50 μm).

Cleaved caspase-3 ; 

PubMed: 31277685     


Immunofluorescence staining of glioma cells treated with the vehicle or Napabucasin. Nuclei were stained with DAPI (blue). Scale bar = 50 μm.

31277685
Growth inhibition assay
Cell viability ; 

PubMed: 31277685     


Proliferation of glioma cells treated with Napabucasin and detected by CCK-8 assays. Half maximal inhibitory concentrations (IC50) of Napabucasin in U87MG and LN229 cells were 6.4 and 5.6 μM respectively. 

31277685
体内研究 在负荷PaCa-2异种移植物的小鼠中,Napabucasin (20 mg/kg, i.p.)显著抑制肿瘤生长,复发和转移。[1]

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: 肿瘤干细胞 U87-MG,U118,COLO205,DLD1,SW480,HCT116,FaDu,ACHN,SNU-475,Huh7,HepG2,H1975,A549,H460,CAOV-3,SW-626,PaCa2
  • Concentrations: ~2 μM
  • Incubation Time: 72小时
  • Method:

    对于各种癌症干细胞,将球体解离,并在癌症干细胞培养条件下接种到镀层96孔板。培养72小时后,孔中加入指示剂量的化合物。加入72小时或24小时后,将CellTiter-Glo 2.0加入每个孔,荧光根据制造商的描述测量。IC50值使用GraphPad Prism软件通过将四参数剂量响应曲线拟合到标准数据计算。大部分细胞以5,000细胞/孔接种到96孔板。接种24小时后,细胞用指示浓度的化合物处理。存活率在72小时根据如上所述测定。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 负荷 PaCa-2 移植物的小鼠
  • Dosages: 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 10 mg/mL (41.63 mM)
Water Insoluble
Ethanol 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):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
1mg/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 240.21
化学式

C14H8O4

CAS号 83280-65-3
储存条件 粉状
溶于溶剂
别名 BBI608

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、SDS / 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、SDS / 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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03525405 Completed Drug: napabucasin ADME|Healthy Sumitomo Dainippon Pharma Oncology Inc May 18 2018 Phase 1
NCT03416816 Terminated Drug: DSP-0337 Neoplasms Sumitomo Dainippon Pharma Oncology Inc|Syneos Health May 15 2018 Phase 1

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID