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Ibrutinib

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,無細胞試驗中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在內的一系列PROTAC

Ibrutinib  Chemical Structure

Ibrutinib Chemical Structure

CAS: 936563-96-1

規(guī)格 價格 庫存 購買數量
10mM (1mL in DMSO) 876.33 現貨
5mg 712.43 現貨
50mg 3349.71 現貨
200mg 7944.3 現貨
1g 12039.3 現貨
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常與Ibrutinib 一起在實驗中被使用的化合物

Acalabrutinib (ACP-196)


Acalabrutinib (ACP-196) 和 Ibrutinib 與 BTK 活性位點的半胱氨酸殘基 (Cys481) 形成共價鍵,從而抑制 BTK 酶活性。 它們被用作抗腫瘤劑。

Zanubrutinib


兩種 BTKi 抑制劑治療均可使淋巴細胞亞群頻率正常化并減少 T 細胞上的 PD-1 表達。

Venetoclax (ABT-199)


聯合治療可導致 MCL1 蛋白減少并產生協同效應。

Jain N, et al. N Engl J Med. 2019 May 30;380(22):2095-2103.

Olaparib (AZD2281)


依魯替尼加奧拉帕尼可進一步抑制 MCL 細胞培養(yǎng)物生長并影響細胞存活和細胞周期調節(jié)。

Curtis AD, et al. Cancer Research. Vol. 77. 615 AMER ASSOC CANCER RESEARCH, 2017.

Osimertinib (AZD9291)


依魯替尼通過抑制層粘連蛋白 α5/FAK 信號傳導逆轉 IL-6 誘導的奧希替尼耐藥。

Li L, et al. Commun Biol. 2022 Feb 23;5(1):155.

Ibrutinib 相關產品

細胞實驗數據示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
點擊查看更多細胞系數據

生物活性

產品描述 Ibrutinib是一種有效的,高選擇性的Brutons tyrosine kinase (Btk)抑制劑,無細胞試驗中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在內的一系列PROTAC。
靶點
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)
點擊更多
0.5 nM 0.5 nM 0.8 nM 2.3 nM 2.3 nM
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細胞系, 抑制Btk自磷酸化, Btk's 生理底物 PLCγ磷酸化, 和更遠一點的下游激酶ERK的磷酸化,IC50分別為11 nM, 29 nM 和 13 nM。[1] Ibrutinib作用于慢性淋巴細胞白血病 (CLL) 細胞,誘導細胞毒性,這種作用存在劑量和時間依賴性。此外, Ibrutinib誘導 caspase依賴性細胞死亡通路激活,且在TLR信號后,抑制CLL細胞增殖能力。[2] 最新研究顯示Ibrutinib抑制 BCR激活的原代 B細胞增殖,IC50 為8 nM,且抑制 原代單核細胞中TNFα, IL-1β 和 IL-6產量, IC50 分別為2.6 nM, 0.5 nM, 和 3.9 nM。 [3]

激酶實驗 激酶實驗
激酶, 33P-ATP, Ibrutinib, 和底物 [0.2 mg/mL 聚(EY)(4:1)]溫育1小時后,使用33P 過濾結合實驗測量體外激酶IC50值。
細胞實驗 細胞系 慢性淋巴細胞白血病 (CLL) 細胞
濃度 0.01 μM到100 μM
孵育時間 48小時
方法

進行MTT實驗測定細胞毒性。細胞(CLL B 細胞或健康志愿者T 細胞或 NK細胞) 和不同濃度 Ibrutinib溫育48小時。加入MTT試劑,實驗板再溫育20小時,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 酶標儀,在540 nm處測定吸光值。使用膜聯蛋白/PI 流式細胞儀在不同時間點測量細胞活力。使用 Expo-ADC32 軟件包分析數據。結果表示為總陽性細胞與對照組之比的百分數。加入100μM Z-VAD檢測caspase依賴性凋亡。

實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot pEGFR(Tyr1068) / EGFR pBTK / pPLCγ2 / pAKT / pERK / pJNK 28061447
Immunofluorescence CD11b COX-2 30231870
ELISA hTNFα IL-10 26627823
體內研究(In Vivo)
體內研究活性

Ibrutinib 作用于膠原誘導的關節(jié)炎模型,通過抑制B細胞活性,顯著降低足腫脹和關節(jié)發(fā)炎等臨床關節(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量。[1] Ibrutinib 每天按25 mg/kg劑量作用于過繼轉移TCL1 的CLL小鼠模型, 產生短暫的早期淋巴細胞增多癥,且延遲CLL 疾病進展。[4]

動物實驗 Animal Models MRL-Fas(lpr) 狼瘡模型和膠原誘導的關節(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

化學信息&溶解度

分子量 440.5 分子式

C25H24N6O2

CAS號 936563-96-1 SDF Download Ibrutinib 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
批次:

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

摩爾濃度計算器

體內溶解度
批次:

現配現用,請按從左到右的順序依次添加,澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內配方計算器(澄清溶液)

第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)

mg/kg g μL

第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

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,:如該濃度超過該批次藥物DMSO溶解度,請先聯系Selleck);

體內配方配制方法: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。

體內配方配制方法: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。

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常見問題及建議解決方法

問題 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.

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