Ibrutinib (PCI-32765)

目录号:S2680

Ibrutinib (PCI-32765) Chemical Structure

Molecular Weight(MW): 440.5

Ibrutinib (PCI-32765)是一种有效的,高选择性的Brutons tyrosine kinase (Btk)抑制剂,无细胞试验中IC50为0.5 nM,对Bmx, CSK, FGR, BRK及HCK适度有效,对EGFR, Yes, ErbB2, JAK3等作用效果较弱。

规格 价格 库存 购买数量  
In DMSO RMB 2226.41 现货
RMB 1392.54 现货
RMB 2617.71 现货
RMB 7922.62 现货
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产品安全说明书

BTK抑制剂选择性比较

生物活性

产品描述 Ibrutinib (PCI-32765)是一种有效的,高选择性的Brutons tyrosine kinase (Btk)抑制剂,无细胞试验中IC50为0.5 nM,对Bmx, CSK, FGR, BRK及HCK适度有效,对EGFR, Yes, ErbB2, JAK3等作用效果较弱。
靶点
BTK [1]
(Cell-free assay)
BLK [1]
(Cell-free assay)
Bmx [1]
(Cell-free assay)
CSK [1]
(Cell-free assay)
FGR [1]
(Cell-free assay)
0.5 nM 0.5 nM 0.8 nM 2.3 nM 2.3 nM
体外研究

Ibrutinib有效可逆且选择性抑制Btk酶活性。Ibrutinib作用于 BCR 通路激活的 DOHH2细胞系, 抑制Btk自磷酸化, Btk's 生理底物 PLCγ磷酸化, 和更远一点的下游激酶ERK的磷酸化,IC50分别为11 nM, 29 nM 和 13 nM。[1] Ibrutinib作用于慢性淋巴细胞白血病 (CLL) 细胞,诱导细胞毒性,这种作用存在剂量和时间依赖性。此外, Ibrutinib诱导 caspase依赖性细胞死亡通路激活,且在TLR信号后,抑制CLL细胞增殖能力。[2] 最新研究显示Ibrutinib抑制 BCR激活的原代 B细胞增殖,IC50 为8 nM,且抑制 原代单核细胞中TNFα, IL-1β 和 IL-6产量, IC50 分别为2.6 nM, 0.5 nM, 和 3.9 nM。 [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells MYnGeY5kfGmxbjDhd5NigQ>? M2rYOFEhcA>? MoS4TY5pcWKrdHnvckBw\iCqdX3hckBnfWyuLXzlcod1cCCEVFug[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHSU1vU4LjeIll\SCyZYD0bYRmKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZnwxIxiSVO1NF0xNjVibl2u M3rkVlIyQTV6NUS3
human Pfeiffer cells M{jkbGZ2dmO2aX;uJIF{e2G7 NXTl[o9UPzJiaB?= NIXPUlNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBR\mWrZn\ldkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yJI5ONg>? NEL4UJkzPDlzNUK5NS=>
human Ramos cells NETFeplHfW6ldHnvckBie3OjeR?= NWDJZlJNOSCq NWW1N3liUW6qaXLpeIlwdiCxZjDCeIshcW5iaIXtZY4hWmGvb4OgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCSTFOt[4FudWF{IIDoc5NxcG:{eXzheIlwdiCjdDDUfZIyOjF5IHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxRTF2IH7NMi=> MYGyOFkyPTJ7MR?=
Sf9 cells MoP4SpVv[3Srb36gZZN{[Xl? NX;GPWk6OSCq MnXMTY5pcWKrdHnvckBw\iCOWV6tRUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4PhfUwhUUN3ME2wMlIh|ryPLh?= MWiyNVk2QDV2Nx?=
human DOHH2 cells MkLjR5l1d3SxeHnjxsBie3OjeR?= MWO3NkBp NXvwWHR5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTE:KSEKgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NUDPxE1w M1;QXlI1QTF3Mkmx
human SU-DHL6 cells MYrDfZRwfG:6aXRCpIF{e2G7 MYW3NkBp NX;VPHRTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1VvRFjMOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU5KM7:TT6= NUjLV4d4OjR7MUWyPVE>
human WSU-NHL cells NECxOHVEgXSxdH;4bYPDqGG|c3H5 NGey[oc4OiCq M33Ud2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHdUXS2QSFygZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wPUDPxE1? M4DsVlI1QTF3Mkmx
human Rec1 cells M2Lv[GZ2dmO2aX;uJIF{e2G7 MlvJNk42KM7:TR?= MW[2JIg> M{H0c2lvcGmkaYTpc44hd2ZiTInuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDS[YMyKGOnbHzzJIF1KDJwNTD1UUBqdmO3YnH0[YQh\m:{IE[gbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l MXOyOVIzOjh5Nx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pEGFR(Tyr1068) / EGFR; 

PubMed: 28061447     


Ibrutinib inhibitory effects on EGFRY1068 auto-phosphorylation in the HCC827 cell line at different time points by removal of drug after 4 h pretreatment.

pBTK / pPLCγ2 / pAKT / pERK / pJNK; 

PubMed: 23940282     


Mino (left panel) or Jeko1 (right panel) cells pretreated with vehicle or ibrutinib 10, 100, or 1000 nM were either stimulated with anti-IgM, CXCL12, or CXCL13 or treated with medium (Med) for 15 minutes and then immunoblotted for pBTK, pPLCγ2, pAKT, pERK, and pJNK.

28061447 23940282
Immunofluorescence
CD11b; 

PubMed: 30231870     


BV2 microglial cells were pretreated with ibrutinib (1 μM) or vehicle (1% DMSO) for 30 min, followed by treatment with LPS (1 μg/ml) or PBS for 5.5 h and immunostaining with an anti-CD11b antibody. Scale bar = 20 μm.

COX-2; 

PubMed: 30231870     


BV2 microglial cells were treated with vehicle (1% DMSO) or ibrutinib (1 μM) for 30 min, followed by PBS or LPS (1 μg/ml) for 5.5 h, and immunocytochemistry was conducted with anti-CD11b and anti-COX-2 antibodies. 

30231870
ELISA
hTNFα; 

PubMed: 26627823     


PBMs were isolated and pretreated with 1, 5, or 10 μm ibrutinib (IB) or left untreated (UT, −). Pretreated PBMs were incubated for 24 h in 96-well plates precoated without (PBS) or with 10 μg/ml whole human IgG. Cleared supernatants were collected and analyzed by ELISA for TNFα (n = 3).

IL-10; 

PubMed: 27792904     


LMP2A-negative (vector.1/.2) and -positive (express LMP2A) B cell lines were incubated in the absence or presence of increasing concentrations of Ibrutinib for 24 hours and supernatants were isolated for analysis using an IL-10 ELISA.

26627823 27792904
体内研究 Ibrutinib 作用于胶原诱导的关节炎模型,通过抑制B细胞活性,显著降低足肿胀和关节发炎等临床关节炎症状。Ibrutinib 作用于 MRL-Fas(lpr) 狼疮模型 ,降低肾疾病和自身抗体产量。[1] Ibrutinib 每天按25 mg/kg剂量作用于过继转移TCL1 的CLL小鼠模型, 产生短暂的早期淋巴细胞增多症,且延迟CLL 疾病进展。[4]

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

激酶实验:

激酶, 33P-ATP, Ibrutinib, 和底物 [0.2 mg/mL 聚(EY)(4:1)]温育1小时后,使用33P 过滤结合实验测量体外激酶IC50值。
细胞实验:[2]
- 合并
  • Cell lines: 慢性淋巴细胞白血病 (CLL) 细胞
  • Concentrations: 0.01 μM到100 μM
  • Incubation Time: 48小时
  • Method: 进行MTT实验测定细胞毒性。细胞(CLL B 细胞或健康志愿者T 细胞或 NK细胞) 和不同浓度 Ibrutinib温育48小时。加入MTT试剂,实验板再温育20小时,然后使用溶于PBS的硫酸鱼精蛋白冲洗。加入DMSO,通过分光光度法使用Labsystems 酶标仪,在540 nm处测定吸光值。使用膜联蛋白/PI 流式细胞仪在不同时间点测量细胞活力。使用 Expo-ADC32 软件包分析数据。结果表示为总阳性细胞与对照组之比的百分数。加入100μM Z-VAD检测caspase依赖性凋亡。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: MRL-Fas(lpr) 狼疮模型和胶原诱导的关节炎模型
  • Formulation: Ibrutinib溶于DMSO
  • Dosages: ≤50 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 88 mg/mL (199.77 mM)
Ethanol 45 mg/mL (102.15 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):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/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 440.5
化学式

C25H24N6O2

CAS号 936563-96-1
储存条件 粉状
溶于溶剂
别名 N/A

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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04042376 Not yet recruiting Drug: Ibrutinib Waldenstrom Macroglobulinemia Janssen Research & Development LLC November 15 2019 Phase 4
NCT04115059 Not yet recruiting Drug: Dasatinib Waldenstrom Macroglobulinemia|DASATINIB Jorge J. Castillo MD|Bristol-Myers Squibb|Dana-Farber Cancer Institute November 2019 Phase 1
NCT03679624 Recruiting Drug: Ibrutinib|Drug: Daratumumab Waldenstrom Macroglobulinemia|Waldenstrom''s Disease|Waldenström; Hypergammaglobulinemia|Waldenstrom''s Macroglobulinemia Recurrent|Waldenstrom''s Macroglobulinemia of Lymph Nodes|Waldenstrom''s Macroglobulinaemia Without Mention of Remission|Waldenstrom''s Macroglobulinemia Refractory Weill Medical College of Cornell University|Janssen Scientific Affairs LLC|Mayo Clinic October 2019 Phase 2
NCT04062448 Not yet recruiting Drug: Ibrutinib|Drug: Rituximab Waldenstrom Macroglobulinemia Janssen Pharmaceutical K.K. September 11 2019 Phase 2
NCT03943342 Not yet recruiting Drug: Ibrutinib|Drug: Venetoclax Chronic Lymphocytic Leukemia|Loss of Chromosome 17p Kerry Rogers|National Cancer Institute (NCI)|Janssen Research & Development LLC|Ohio State University Comprehensive Cancer Center September 1 2019 Phase 2

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操作手册

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  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to reconstitute the compound S2680 for in vivo studies?

  • 回答:

    For in vivo study, we suggest to use 5% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 10mg/ml.

BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID