- 抑制劑
- 化合物庫
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- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
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Ibrutinib (PCI-32765)
別名: PCI-32765 中文名稱：依魯替尼，伊布替尼
Ibrutinib是一種有效的，高選擇性的Brutons tyrosine kinase (Btk)抑制劑，無細(xì)胞試驗(yàn)中IC50為0.5 nM，對Bmx， CSK， FGR， BRK及HCK適度有效，對EGFR， Yes， ErbB2， JAK3等作用效果較弱。Ibrutinib 可作為Btk配體用于合成包括P13I在內(nèi)的一系列PROTAC。
Ibrutinib (PCI-32765) Chemical Structure
CAS: 936563-96-1
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
常與Ibrutinib (PCI-32765)一起在實(shí)驗(yàn)中被使用的化合物
Acalabrutinib (ACP-196) 和 Ibrutinib 與 BTK 活性位點(diǎn)的半胱氨酸殘基 (Cys481) 形成共價(jià)鍵，從而抑制 BTK 酶活性。 它們被用作抗腫瘤劑。
Ibrutinib (PCI-32765)相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | (+)-JQ1 Quizartinib (AC220) | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)化合物庫 | 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫 | 點(diǎn)擊展開 |
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(PMID) |
|---|---|---|---|---|---|
| human Rec1 cells | Function assay | 2.5 μM | 6 h | Inhibition of Lyn phosphorylation in human Rec1 cells at 2.5 uM incubated for 6 hrs by Western blotting method | 25222877 |
| human Ramos cells | Function assay | 1 h | Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis, IC50=14 nM. | 24915291 | |
| Sf9 cells | Function assay | 1 h | Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay, IC50=0.2 μM. | 21958547 | |
| human DOHH2 cells | Cytotoxic?assay | 72 h | Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.41 μM. | 24915291 | |
| human SU-DHL6 cells | Cytotoxic?assay | 72 h | Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=0.58 μM. | 24915291 | |
| human WSU-NHL cells | Cytotoxic?assay | 72 h | Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=1.09 μM | 24915291 | |
| human Pfeiffer cells | Function assay | 72 h | Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50=2 nM. | 24915291 | |
| Sf9 cells | Function assay | 1 h | Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay， IC50=0.5 nM. | 21958547 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.0003 μM | 29146136 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.00034 μM | 27912175 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.00034 μM | 28432946 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.00034 μM | 27956037 | |
| Sf9 cells | Function assay | 60 mins | IC50 = 0.0004 μM | 30006143 | |
| Sf9 cells | Function assay | 60 mins | IC50 = 0.0005 μM | 21958547 | |
| Ramos cells | Function assay | 1 h | IC50 = 0.0005 μM | 28280261 | |
| Sf9 cells | Function assay | 60 mins | IC50 = 0.001 μM | 30077608 | |
| Pfeiffer cells | Cytotoxicity assay | 72 h | GI50 = 0.002 μM | 24915291 | |
| B cells | Function assay | 1 h | IC50 = 0.0046 μM | 30290988 | |
| Sf9 insect cells | Function assay | 2 to 60 mins | Ki = 0.0048 μM | 28315597 | |
| Ramos cells | Function assay | 1 h | IC50 = 0.0075 μM | 24915291 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.008 μM | 28315597 | |
| TMD8 cells | Antiproliferative activity assay | 72 h | IC50 = 0.01 μM | 29715023 | |
| CD19+ B cells | Function assay | 1 h | IC50 = 0.012 μM | 29457982 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.012 μM | 28315597 | |
| Ramos cells | Function assay | 1 h | IC50 = 0.014 μM | 24915291 | |
| Sf9 insect cells | Function assay | 1 h | IC50 = 0.0144 μM | 29715023 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.0161 μM | 29146136 | |
| HCC827 cells | Antiproliferative activity assay | 72 h | IC50 = 0.039 μM | 28734581 | |
| PC9 cells | Function assay | 72 h | GI50 = 0.05 μM | 28282122 | |
| Sf9 cells | Function assay | 60 mins | IC50 = 0.1 μM | 30006143 | |
| H3255 cells | Function assay | 72 h | GI50 = 0.11 μM | 28282122 | |
| BaF3 cells | Function assay | 72 h | GI50 = 0.12 μM | 26630553 | |
| BAF3 cells | Antiproliferative activity assay | 72 h | GI50 = 0.12 μM | 28956923 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.123 μM | 28315597 | |
| Sf9 insect cells | Function assay | 60 mins | IC50 = 0.146 μM | 28315597 | |
| BAF3 cells | Function assay | 72 h | GI50 = 0.16 μM | 28282122 | |
| Sf9 cells | Function assay | 60 mins | IC50 = 0.2 μM | 21958547 | |
| MV4-11 cells | Antiproliferative activity assay | 72 h | GI50 = 0.33 μM | 26630553 | |
| MV4-11 cells | Antiproliferative activity assay | 72 h | GI50 = 0.33 μM | 28956923 | |
| DOHH2 cells | Cytotoxicity assay | 72 h | GI50 = 0.41 μM | 24915291 | |
| HCC827 cells | Antiproliferative activity assay | 96 h | EC50 = 0.45 μM | 28853575 | |
| SU-DHL6 cells | Cytotoxicity assay | 72 h | GI50 = 0.58 μM | 24915291 | |
| NCI-H1975 cells | Antiproliferative activity assay | 96 h | EC50 = 0.64 μM | 28853575 | |
| HEK293T cells | Function assay | 1 h | IC50 = 0.9 μM | 28280261 | |
| Ramos cells | Antiproliferative activity assay | 72 h | IC50 = 0.92 μM | 29715023 | |
| BA/F3 cells | Antiproliferative activity assay | 72 h | IC50 = 1 μM | 26258521 | |
| WSU-NHL cells | Cytotoxicity assay | 72 h | GI50 = 1.09 μM | 24915291 | |
| NCI-H1975 cells | Function assay | 72 h | GI50 = 1.2 μM | 28282122 | |
| NCI-H1975 cells | Antiproliferative activity assay | 72 h | IC50 = 1.27 μM | 28734581 | |
| Raji cells | Antiproliferative activity assay | 48 h | IC50 = 1.49 μM | 29567295 | |
| A431 cells | Antiproliferative activity assay | 96 h | EC50 = 2.38 μM | 28853575 | |
| BAF3 cells | Antiproliferative activity assay | 72 h | GI50 = 2.5 μM | 28956923 | |
| Ramos cells | Antiproliferative activity assay | 72 h | IC50 = 5.14 μM | 30006143 | |
| Ramos cells | Antiproliferative activity assay | 48 h | IC50 = 5.14 μM | 27956037 | |
| Ramos cells | Antiproliferative activity assay | 48 h | IC50 = 5.88 μM | 28432946 | |
| Ramos cells | Antiproliferative activity assay | 72 h | IC50 = 6.62 μM | 29146136 | |
| K562 cells | Antiproliferative activity assay | 48 h | IC50 = 7.5 μM | 30077608 | |
| HL60 cells | Antiproliferative activity assay | 48 h | IC50 = 8 μM | 30077608 | |
| Ramos cells | Antiproliferative activity assay | 48 h | IC50 = 8.11 μM | 27994736 | |
| Ramos cells | Antiproliferative activity assay | 48 h | IC50 = 8.26 μM | 29567295 | |
| BAF3 cells | Cytotoxicity assay | 72 h | GI50 = 10 μM | 26630553 | |
| BAF3 cells | Antiproliferative activity assay | 72 h | GI50 = 10 μM | 28956923 | |
| BAF3 cells | Growth inhibition assay | 72 h | GI50 = 10 μM | 28282122 | |
| NAMALWA cells | Antiproliferative activity assay | 72 h | IC50 = 10.45 μM | 29146136 | |
| Ramos cells | Antiproliferative activity assay | 48 h | IC50 = 12.6 μM | 27912175 | |
| Raji cells | Antiproliferative activity assay | 48 h | IC50 = 14.2 μM | 30077608 | |
| Raji cells | Antiproliferative activity assay | 48 h | IC50 = 15.2 μM | 27994736 | |
| MIAPaCa2 cells | Cytotoxicity assay | 3 days | IC50 = 16.6 μM | 27077228 | |
| HeLa cells | Cytotoxicity assay | 3 days | IC50 = 16.8 μM | 27077228 | |
| Raji cells | Antiproliferative activity assay | 48 h | IC50 = 19.3 μM | 27912175 | |
| Raji cells | Antiproliferative activity assay | 48 h | IC50 = 19.3 μM | 28432946 | |
| Raji cells | Antiproliferative activity assay | 72 h | IC50 = 19.5 μM | 30006143 | |
| Raji cells | Antiproliferative activity assay | 48 h | IC50 = 19.5 μM | 27956037 | |
| NAMALWA cells | Antiproliferative activity assay | 72 h | IC50 = 19.6 μM | 30006143 | |
| A2780 cells | Cytotoxicity assay | 3 days | EC50 = 20.1 μM | 27077228 | |
| Raji cells | Antiproliferative activity assay | 72 h | IC50 = 20.88 μM | 29146136 | |
| A549 cells | Antiproliferative activity assay | 72 h | IC50 = 21.79 μM | 28734581 | |
| SW480 cells | Cytotoxicity assay | 3 days | IC50 = 25.6 μM | 27077228 | |
| Ramos cells | Cytotoxicity assay | 24 h | IC50 = 28.7 μM | 28274675 | |
| sf9 cells | Function assay | IC50 = 0.0003 μM | 27994736 | ||
| MV411 cells | Growth inhibition assay | GI50 = 0.25 μM | 28315597 | ||
| M07e cells | Growth inhibition assay | GI50 = 0.59 μM | 28315597 | ||
| SU-DHL-2 cells | Growth inhibition assay | GI50 = 0.64 μM | 28315597 | ||
| Pfeiffer cells | Growth inhibition assay | GI50 = 1.6 μM | 28315597 | ||
| U937 cells | Growth inhibition assay | GI50 = 2.9 μM | 28315597 | ||
| NB4 cells | Growth inhibition assay | GI50 = 3 μM | 28315597 | ||
| Ramos cells | Growth inhibition assay | GI50 = 3.4 μM | 28315597 | ||
| SKM1 cells | Growth inhibition assay | GI50 = 3.6 μM | 28315597 | ||
| U2932 cells | Growth inhibition assay | GI50 = 4.4 μM | 28315597 | ||
| OCI-AML3 cells | Growth inhibition assay | GI50 = 9.2 μM | 28315597 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Ibrutinib是一種有效的，高選擇性的Brutons tyrosine kinase (Btk)抑制劑，無細(xì)胞試驗(yàn)中IC50為0.5 nM，對Bmx， CSK， FGR， BRK及HCK適度有效，對EGFR， Yes， ErbB2， JAK3等作用效果較弱。Ibrutinib 可作為Btk配體用于合成包括P13I在內(nèi)的一系列PROTAC。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Ibrutinib有效可逆且選擇性抑制Btk酶活性。Ibrutinib作用于 BCR 通路激活的 DOHH2細(xì)胞系, 抑制Btk自磷酸化, Btk's 生理底物 PLCγ磷酸化, 和更遠(yuǎn)一點(diǎn)的下游激酶ERK的磷酸化，IC50分別為11 nM, 29 nM 和 13 nM。[1] Ibrutinib作用于慢性淋巴細(xì)胞白血病 (CLL) 細(xì)胞，誘導(dǎo)細(xì)胞毒性，這種作用存在劑量和時(shí)間依賴性。此外, Ibrutinib誘導(dǎo) caspase依賴性細(xì)胞死亡通路激活，且在TLR信號后，抑制CLL細(xì)胞增殖能力。[2] 最新研究顯示Ibrutinib抑制 BCR激活的原代 B細(xì)胞增殖,IC50 為8 nM，且抑制 原代單核細(xì)胞中TNFα, IL-1β 和 IL-6產(chǎn)量， IC50 分別為2.6 nM, 0.5 nM, 和 3.9 nM。 [3] |
|||
|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 激酶實(shí)驗(yàn) | |||
| 激酶, 33P-ATP, Ibrutinib, 和底物 [0.2 mg/mL 聚(EY)(4:1)]溫育1小時(shí)后，使用33P 過濾結(jié)合實(shí)驗(yàn)測量體外激酶IC50值。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | 慢性淋巴細(xì)胞白血病 (CLL) 細(xì)胞 | ||
| 濃度 | 0.01 μM到100 μM | |||
| 孵育時(shí)間 | 48小時(shí) | |||
| 方法 | 進(jìn)行MTT實(shí)驗(yàn)測定細(xì)胞毒性。細(xì)胞(CLL B 細(xì)胞或健康志愿者T 細(xì)胞或 NK細(xì)胞) 和不同濃度 Ibrutinib溫育48小時(shí)。加入MTT試劑,實(shí)驗(yàn)板再溫育20小時(shí)，然后使用溶于PBS的硫酸魚精蛋白沖洗。加入DMSO，通過分光光度法使用Labsystems 酶標(biāo)儀，在540 nm處測定吸光值。使用膜聯(lián)蛋白/PI 流式細(xì)胞儀在不同時(shí)間點(diǎn)測量細(xì)胞活力。使用 Expo-ADC32 軟件包分析數(shù)據(jù)。結(jié)果表示為總陽性細(xì)胞與對照組之比的百分?jǐn)?shù)。加入100μM Z-VAD檢測caspase依賴性凋亡。 |
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| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | pEGFR(Tyr1068) / EGFR pBTK / pPLCγ2 / pAKT / pERK / pJNK |
|
28061447 | |
| Immunofluorescence | CD11b COX-2 |
|
30231870 | |
| ELISA | hTNFα IL-10 |
|
26627823 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Ibrutinib 作用于膠原誘導(dǎo)的關(guān)節(jié)炎模型，通過抑制B細(xì)胞活性，顯著降低足腫脹和關(guān)節(jié)發(fā)炎等臨床關(guān)節(jié)炎癥狀。Ibrutinib 作用于 MRL-Fas(lpr) 狼瘡模型 ,降低腎疾病和自身抗體產(chǎn)量。[1] Ibrutinib 每天按25 mg/kg劑量作用于過繼轉(zhuǎn)移TCL1 的CLL小鼠模型, 產(chǎn)生短暫的早期淋巴細(xì)胞增多癥，且延遲CLL 疾病進(jìn)展。[4] |
|
|---|---|---|
| 動物實(shí)驗(yàn) | Animal Models | MRL-Fas(lpr) 狼瘡模型和膠原誘導(dǎo)的關(guān)節(jié)炎模型 |
| Dosages | ≤50 mg/kg | |
| Administration | 口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06084923 | Not yet recruiting | Chronic Lymphocytic Leukemia |
Gruppo Italiano Malattie EMatologiche dell''Adulto |
May 2024 | -- |
| NCT06224452 | Not yet recruiting | Hematological Malignancy|Atrial Fibrillation |
University Hospital Caen |
March 1 2024 | -- |
| NCT05694312 | Recruiting | Autoimmune Hemolytic Anemia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Monoclonal B-Cell Lymphocytosis CLL-Type |
Gruppo Italiano Malattie EMatologiche dell''Adulto |
November 24 2023 | Phase 2 |
|
化學(xué)信息&溶解度
| 分子量 | 440.5 | 分子式 | C25H24N6O2 |
| CAS號 | 936563-96-1 | SDF | Download Ibrutinib (PCI-32765) SDF |
| Smiles | C=CC(=O)N1CCCC(C1)N2C3=NC=NC(=C3C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)N | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 88 mg/mL ( (199.77 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 8 mg/mL (18.16 mM) Water : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
在訂購、運(yùn)輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱[email protected]，直接聯(lián)系到我們。我們會在24小時(shí)內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項(xiàng)
常見問題及建議解決方法
問題 1:
How to reconstitute it 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 for it.
