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Napabucasin (BBI608)

別名: BBI608

Napabucasin (BBI608) 是一種口服具有活性的Stat3和癌細(xì)胞多能性抑制劑。

Napabucasin (BBI608) Chemical Structure

Napabucasin (BBI608) Chemical Structure

CAS: 83280-65-3

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 958.23 現(xiàn)貨
5mg 957.38 現(xiàn)貨
25mg 3261.41 現(xiàn)貨
100mg 8169.42 現(xiàn)貨
1g 30876.3 現(xiàn)貨
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Napabucasin (BBI608)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Napabucasin (BBI608) 是一種口服具有活性的Stat3和癌細(xì)胞多能性抑制劑。
靶點(diǎn)
Stat3 [1]
體外研究(In Vitro)
體外研究活性 Napabucasin下調(diào)Stat3驅(qū)動(dòng)的干細(xì)胞基因表達(dá)和癌癥干細(xì)胞性能,并有效抑制高度多功能性癌細(xì)胞的自我更新,IC50范圍為0.291~1.19 μM,而對(duì)正常干細(xì)胞沒有抑制作用。[1]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 腫瘤干細(xì)胞 U87-MG,U118,COLO205,DLD1,SW480,HCT116,F(xiàn)aDu,ACHN,SNU-475,Huh7,HepG2,H1975,A549,H460,CAOV-3,SW-626,PaCa2
濃度 ~2 μM
孵育時(shí)間 72小時(shí)
方法

對(duì)于各種癌癥干細(xì)胞,將球體解離,并在癌癥干細(xì)胞培養(yǎng)條件下接種到鍍層96孔板。培養(yǎng)72小時(shí)后,孔中加入指示劑量的化合物。加入72小時(shí)或24小時(shí)后,將CellTiter-Glo 2.0加入每個(gè)孔,熒光根據(jù)制造商的描述測(cè)量。IC50值使用GraphPad Prism軟件通過(guò)將四參數(shù)劑量響應(yīng)曲線擬合到標(biāo)準(zhǔn)數(shù)據(jù)計(jì)算。大部分細(xì)胞以5,000細(xì)胞/孔接種到96孔板。接種24小時(shí)后,細(xì)胞用指示濃度的化合物處理。存活率在72小時(shí)根據(jù)如上所述測(cè)定。

實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot CDK4 / Cyclin D1 STAT3 / β-catenin / c-Myc

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