伊布替尼|T1835

Ibrutinib
936563-96-1

￥488 5mg 起订

￥788 10mg 起订

￥1995 50mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 伊布替尼

英文名称：: Ibrutinib

CAS号：: 936563-96-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.79%

产品类别：: 抑制剂

货号：: T1835

Product Introduction

Bioactivity

名称	Ibrutinib
描述	Ibrutinib (PCI-32765) is a Bruton's tyrosine kinase (BTK) inhibitor (IC50=0.5 nM) with irreversible and selective properties. Ibrutinib blocks BTK to inhibit the proliferation and survival of B cells, and possesses antitumor activity, which can be used for the treatment of chronic lymphocytic leukemia, among others.
细胞实验	CD20+ B and CD3+ T cells were purified by negative selection (RosetteSep, >90% purity) from buffy coat PBMCs and viably frozen in 10% DMSO. Cells were thawed at 37 °C and maintained in growth media (RPMI media containing 10% FCS). B cells were stimulated with goat anti-human IgM F(ab′)2 (10 μg/mL) and T cells were stimulated with anti-CD3/CD28 coated beads at a 1:1 bead/cell ratio. Cells were stained with PE-CD69 and analyzed by flow cytometry, gating on viable lymphocytes. PCI-32765 at concentrations lower than 10 μM did not decrease B- or T-cell viability during the course of the experiment, although PCI-32765 did block the modest survival benefit of anti-IgM stimulation in B cells. For washout experiments, cells were rinsed three times in 10 volumes of growth media, a protocol that was confirmed to completely wash away inhibition of BCR signaling by PCI-29732, a reversible Btk inhibitor [1].
激酶实验	In vitro kinase IC50s were measured using 33P filtration binding assay after 1 h incubation of kinase, 33P-ATP, inhibitor, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays were performed at Reaction Biology [1].
动物实验	ale DBA/1 mice were immunized with type II collagen plus Freund adjuvant and boosted 21 d later. On a rolling basis, as significant swelling appeared in at least one paw, mice were enrolled and randomized. PCI-32765 or dexamethasone (0.2 mg/kg) was administered orally once per day for 11 d. Arthritis scores (0–5) were assigned to the mice based on the degree and extent of paw swelling. Mouse anti-type II collagen antibody and total IgG levels were measured by ELISA. Female MRL/MpJ-Faslpr mice received PCI-32765 by oral gavage once per day from week 8 through week 20. Proteinuria was monitored weekly. At week 20, serum was collected and analyzed for BUN and mouse anti-dsDNA antibody levels. Kidney histology was scored according to established criteria (26). No drug-induced weight loss was observed at any of the dose levels tested. These studies were carried out at Boulder Biopath according to approved animal care protocols. Results are presented as the mean ± SEM. Statistical significance between groups were evaluated with repeated measures one-way ANOVA or one-way ANOVA using GraphPad Prism with Tukey or Bonferroni multicomparison posttest [1].
体外活性	方法：人 B 细胞淋巴瘤细胞 DOHH2 用 Ibrutinib (0.00064-2 µM) 孵育 1 h，再用 anti-IgG F(ab′)2 (30 µg/mL) 刺激 2 min，使用 Western Blot 检测靶点蛋白表达水平。结果：Ibrutinib 抑制 Btk 的自体磷酸化 (IC50=11 nM)，Btk 的生理底物 PLCγ 的磷酸化 (IC50=29 nM)，和进一步的下游激酶 ERK 的磷酸化 (IC50=13 nM)。[1] 方法：原代人类B淋巴细胞用 Ibrutinib (1-1000 nM) 处理 30 min，然后用 anti-IgM F(ab')2 (10 µg/mL)、anti-CD3/CD28 (5 µg/mL) 或 PMA (0.5 µg/mL) 刺激细胞 72 h，使用 Cell Titer Glo reagent 检测细胞增殖。结果：Ibrutinib 剂量依赖性地抑制抗 IgM 刺激的 B 淋巴细胞增殖 (IC50=8 nM)，但不抑制 PMA 刺激的增殖，PMA 激活PKC途径。[2]
体内活性	方法：为检测体内抗炎活性，将 Ibrutinib (3.125-50 mg/kg) 灌胃给药给关节炎 DBA/1 小鼠，每天一次，持续十一天。结果：在所有剂量下治疗的小鼠中观察到临床关节炎评分的显著抑制。在分别以 3.125 和 12.5 mg/kg/天的剂量治疗 9 至 11 天后，疾病的临床症状出现部分和几乎完全消除。与体内抑制 B 细胞活化一致，抗胶原自身抗体的产生显著减少，总 IgG 水平适度降低。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.2 mg/mL (18.62 mM), Suspension. Working solution is recommended to be prepared and used immediately. Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 45 mg/mL (102.16 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	inhibit \| PCI 32765 \| Ligands for Target Protein for PROTAC \| Target Protein-binding Moiety \| PCI32765 \| Inhibitor \| Btk \| Ibrutinib \| Bruton tyrosine kinase
相关产品	Gefitinib \| Ruxolitinib \| Nintedanib
相关库	抗癌上市药物库 \| 抗癌活性化合物库 \| 经典已知活性库 \| EMA 上市药物库 \| FDA 上市药物库 \| 酪氨酸激酶分子库 \| 抗癌临床化合物库

依鲁替尼|||伊布替尼|||PCI-32765|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子