Napabucasin (BBI608)
别名: BBI608
Napabucasin (BBI608) 是一种口服具有活性的Stat3和癌细胞多能性抑制剂。
Napabucasin (BBI608) Chemical Structure
CAS: 83280-65-3
产品质控
批次：
纯度：
99.72%
99.72
Napabucasin (BBI608)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MDA-MB-231 | Function assay | 100 uM | 1 hr | Binding affinity to STAT3 in human MDA-MB-231 cells at 100 uM treated for 1 hr followed by thermolysin addition measured after 30 mins by DARTS-Western blot analysis | 30003778 |
| MDA-MB-231 | Function assay | 5 umol/L | 24 hrs | Induction of superoxide generation in human MDA-MB-231 cells at 5 umol/L measured after 24 hrs by DHE staining based flow cytometry | 30003778 |
| MDA-MB-231 | Function assay | 5 umol/L | 24 hrs | Induction of superoxide generation in human MDA-MB-231 cells at 5 umol/L measured after 24 hrs in presence of NQO1 inhibitor dicoumarol by DHE staining based flow cytometry | 30003778 |
| human HaCaT cells | Function assay | 48 h | Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy, IC50=0.5 μM | 22845014 | |
| human DU145 cells | Function assay | 72 h | Anticancer activity against human DU145 cells after 72 hrs by XTT assay, IC50=0.02304 μM | 18829316 | |
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.34 μM. | 28558333 | |
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.66 μM. | 28558333 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.74 μM. | 28558333 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay, IC50 = 1 μM. | 30003778 | |
| MDA-MB-231 | Function assay | 4 hrs | Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells assessed as reduction in ratio of phosphorylated STAT3 to total STAT3 level after 4 hrs by HTRF assay, EC50 = 1.9 μM. | 30003778 | |
| MDA-MB-231 | Function assay | 4 hrs | Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells after 4 hrs by HTRF assay, EC50 = 2 μM. | 30003778 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay, IC50 = 2.1 μM. | 30003778 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay, IC50 = 10.2 μM. | 29604543 | |
| L02 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay, IC50 = 18.7 μM. | 29604543 | |
| human HaCaT cells | Proliferation assay | Antiproliferative activity against human HaCaT cells, IC50=0.5 μM | 10479319 | ||
| KB cells | Cytotoxicity assay | Effective cytotoxic dose against KB cells was evaluated, ED50=4.2 μM | 9873618 | ||
| 点击查看更多细胞系数据 | |||||
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 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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] | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | 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 | ||
| 浓度 | ~2 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CDK4 / Cyclin D1 STAT3 / β-catenin / c-Myc c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin |
|
31277685 | |
| Immunofluorescence | STAT3 Cleaved caspase-3 |
|
31277685 | |
| Growth inhibition assay | Cell viability |
|
31277685 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 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] | |
|---|---|---|
| 动物实验 | Animal Models | 负荷 PaCa-2 移植物的小鼠 |
| Dosages | 20 mg/kg | |
| Administration | i.p. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03525405 | Completed | ADME|Healthy |
Sumitomo Pharma America Inc. |
May 18 2018 | Phase 1 |
| NCT03416816 | Terminated | Neoplasms |
Sumitomo Pharma America Inc.|Syneos Health |
May 15 2018 | Phase 1 |
| NCT02279719 | Completed | Hepatocellular Carcinoma |
Sumitomo Pharma America Inc. |
December 2014 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 240.21 | 分子式 | C14H8O4 |
| CAS号 | 83280-65-3 | SDF | Download Napabucasin (BBI608) SDF |
| Smiles | CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 14 mg/mL ( (58.28 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
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）
mg/kg
g
μL
只
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
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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