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(±)-Zanubrutinib/(±)-泽布替尼 {[allProObj[0].p_purity_real_show]}

货号:A444177 同义名: (±)-BGB-3111

(±)-Zanubrutinib 也称为 (±)-BGB-3111,是一种有效的、选择性的口服 BTK 抑制剂,表现出纳摩尔级的 BTK 抑制活性。

(±)-Zanubrutinib/(±)-泽布替尼 化学结构 CAS号:1633350-06-7
(±)-Zanubrutinib/(±)-泽布替尼 化学结构
CAS号:1633350-06-7
(±)-Zanubrutinib/(±)-泽布替尼 3D分子结构
CAS号:1633350-06-7
(±)-Zanubrutinib/(±)-泽布替尼 化学结构 CAS号:1633350-06-7
(±)-Zanubrutinib/(±)-泽布替尼 3D分子结构 CAS号:1633350-06-7
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(±)-Zanubrutinib/(±)-泽布替尼 纯度/质量文件 产品仅供科研

货号:A444177 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 BTK 其他靶点 纯度
CGI-1746 +++

BTK, IC50: 1.9 nM

98%
Spebrutinib ++++

BTK, IC50: <0.5 nM

98+%
Acalabrutinib ++

BTK, IC50: 3nM

98%
CNX-774 +++

BTK, IC50: <1 nM

99%+
Ibrutinib ++++

BTK, IC50: 0.5 nM

98%
ONO-4059 analog +

BTK, IC50: 23.9 nM

98%
RN486 ++

BTK, IC50: 4 nM

99%+
(Z)-LFM-A13 +

BTK, Ki: 1.4 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

(±)-Zanubrutinib/(±)-泽布替尼 生物活性

描述 (±)-Zanubrutinib, also known as (±)-BGB-3111, is an efficacious, selective, oral Btk inhibitor that exhibits nanomolar-level Btk inhibitory activity. In various MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR-triggered autophosphorylation of Btk, blocks downstream PLC-γ2 signaling, and effectively suppresses cell proliferation. Compared to PCI-32765, (±)-Zanubrutinib demonstrates more restricted off-target activity against a panel of kinases, including ITK[1].

(±)-Zanubrutinib/(±)-泽布替尼 细胞实验

Cell Line
Concentration Treated Time Description References
697 cells 193 nM 3 days Evaluate the antiproliferative effect of zanubrutinib on 697 cells, IC50 = 193 nM Blood Adv. 2024 Jun 11;8(11):2846-2860.
RCH-ACV cells 220 nM 3 days Evaluate the antiproliferative effect of zanubrutinib on RCH-ACV cells, IC50 = 220 nM Blood Adv. 2024 Jun 11;8(11):2846-2860.
HEK293 cells 0.1, 0.3, 5 μM 10 minutes Evaluate whether zanubrutinib is a substrate of OATP1B1, OATP1B3, OAT1, OAT3, or OCT2, finding uptake ratios <2 at all concentrations, indicating zanubrutinib is unlikely to be a substrate of these transporters Pharmacol Res Perspect. 2021 Dec;9(6):e00870.
BCRP vesicles 0.1, 5 μM 5 minutes Assess whether zanubrutinib is a BCRP substrate, finding uptake ratios of 0.970 ± 0.101-fold at 0.1 µM and 0.720 ± 0.209-fold at 5 µM, suggesting zanubrutinib is unlikely to be a BCRP substrate Pharmacol Res Perspect. 2021 Dec;9(6):e00870.
MDCK-MDR1 cells 1, 10 μM 90 minutes Evaluate whether zanubrutinib is a P-gp substrate, finding efflux ratios of 3.46 at 1 µM and 2.19 at 10 µM, indicating zanubrutinib is a potential P-gp substrate Pharmacol Res Perspect. 2021 Dec;9(6):e00870.
Human hepatocytes 0.3, 3, 30 μM 2 days Assess the induction potential of zanubrutinib on CYP1A2, CYP2B6, and CYP3A4 mRNA expression and enzymatic activity, finding significant induction of CYP3A4 mRNA (15.0-fold) and CYP2C8 mRNA (9.8-fold) at 30 μM Pharmacol Res Perspect. 2021 Dec;9(6):e00870.
Recombinant CYP enzymes 1 μM 15 minutes Identify the major CYP isoform responsible for zanubrutinib metabolism, finding that only rCYP3A4 led to a remarkable disappearance of zanubrutinib Pharmacol Res Perspect. 2021 Dec;9(6):e00870.
Human liver microsomes 10 μM 60 minutes Evaluate the in vitro metabolic pathways of zanubrutinib, identifying 11 metabolites with major pathways including hydroxylation of the phenoxy phenyl (M5) and oxidation and ring opening of the piperidine (M3, M7/M8, M9, M10, M11) Pharmacol Res Perspect. 2021 Dec;9(6):e00870.
TMD8 cells 0.7 nM 6 days To evaluate the anti-proliferative effects of BGB-10188 and zanubrutinib in TMD8 cells. Results showed that the combination of BGB-10188 and zanubrutinib had synergistic anti-proliferative effects. Neoplasia. 2024 Nov;57:101053.
Human platelets 0.5-2.0 μM 10 minutes To study the effect of BTK inhibitors on α- and dense granule release. Both ibrutinib and zanubrutinib significantly inhibited rhodocytin- and CRP-XL-induced P-selectin expression and dense granule release. Blood Adv. 2019 Dec 23;3(24):4298-4311.
Human platelets 0.5 μM 30 minutes To study platelet adhesion and thrombus formation on collagen, VWF, or fibrinogen. Ibrutinib significantly reduced platelet adhesion and thrombus formation, while zanubrutinib was similar to the control. Blood Adv. 2019 Dec 23;3(24):4298-4311.
Maver-1 5 μM 3 hours To evaluate the effect of BGB-3111 on Akt phosphorylation, results showed that BGB-3111 significantly inhibited Akt phosphorylation at 5 μM concentration. Mol Cancer Ther. 2019 Feb;18(2):267-277.
Mino 5 μM 1 hour To evaluate the inhibitory effect of BGB-3111 on BTK phosphorylation, results showed that BGB-3111 significantly inhibited BTK phosphorylation at 5 μM concentration. Mol Cancer Ther. 2019 Feb;18(2):267-277.
Jeko-1 5 μM and 15 μM 72 hours To evaluate the inhibitory effect of BGB-3111 on MCL cell proliferation, results showed that BGB-3111 significantly inhibited cell proliferation at 5 μM and 15 μM concentrations. Mol Cancer Ther. 2019 Feb;18(2):267-277.
OCI-Ly-10 (ABC DLBCL cell line) 1.5 nM 72 hours Evaluate single-agent antitumor activity, showing activity in the nanomolar range Haematologica. 2019 Jul;104(7):e307-e309.
TMD8 (ABC DLBCL cell line) 0.4 nM 72 hours Evaluate single-agent antitumor activity, showing activity in the nanomolar range Haematologica. 2019 Jul;104(7):e307-e309.
REC1 (MCL cell line) 0.9 nM 72 hours Evaluate single-agent antitumor activity, showing activity in the nanomolar range Haematologica. 2019 Jul;104(7):e307-e309.
RAW264.7, mouse leukemia cells of monocyte macrophage 1 μmol L−1 24 hours ZB reduced β-AR-induced macrophage pro-inflammatory cytokine production. Molecules. 2023 Aug 12;28(16):6035.
Primary neonatal rat cardiac fibroblasts (NRCFs) 1 μmol L−1 24 hours ZB alleviated β-AR-induced cardiac fibroblast activation, including proliferation, trans-differentiation, and ECM synthesis. Molecules. 2023 Aug 12;28(16):6035.

(±)-Zanubrutinib/(±)-泽布替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice E2A-PBX1+/preBCR+ leukemia model Intraperitoneal injection 10 mg/kg Once daily for 20 days Evaluate the effect of zanubrutinib monotherapy and combination with dasatinib on survival in leukemia mice, combination significantly prolonged disease-free survival Blood Adv. 2024 Jun 11;8(11):2846-2860.
Mice Farage subcutaneous xenograft model Oral 7.5 mg/kg Twice daily for 22 days To evaluate the anti-tumor effects of BGB-10188 and zanubrutinib in the Farage subcutaneous xenograft model. Results showed that the combination of BGB-10188 and zanubrutinib significantly enhanced anti-tumor activity. Neoplasia. 2024 Nov;57:101053.
C57BL/6 mice Thrombosis model Oral gavage 10 mg/kg Single dose, tested after 2 hours To study the effect of ibrutinib and zanubrutinib on thrombus formation. Ibrutinib significantly inhibited thrombus growth, while zanubrutinib was similar to the control. Blood Adv. 2019 Dec 23;3(24):4298-4311.
NSG mice MCL PDX model Oral gavage 30 mg/kg Twice daily for 25 days To evaluate the antitumor activity of BGB-3111 in the MCL PDX model, results showed that BGB-3111 significantly inhibited tumor growth. Mol Cancer Ther. 2019 Feb;18(2):267-277.
Male C57BL/6J mice ISO-induced cardiac fibrosis model Oral gavage 20 mg/kg Once daily for 7 days ZB ameliorates β-AR-induced cardiac fibrosis and inflammation by the BTK, STAT3, NF-κB, and PI3K/Akt signal pathways both in vivo and in vitro. Molecules. 2023 Aug 12;28(16):6035.

(±)-Zanubrutinib/(±)-泽布替尼 动物研究

Animal study In the REC-1 MCL xenograft animal model, either subcutaneously or systemically transplanted, (±)-Zanubrutinib induces a dose-dependent antitumor effect through intravenous injection via the tail vein. A preliminary 14-day toxicity study in rats with subcutaneous xenografts showed excellent tolerance for (±)-Zanubrutinib, with doses up to 250 mg/kg/day without reaching the maximum tolerated dose[1].

(±)-Zanubrutinib/(±)-泽布替尼 参考文献

[1]Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597

(±)-Zanubrutinib/(±)-泽布替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.60mL

2.12mL

1.06mL

21.21mL

4.24mL

2.12mL

(±)-Zanubrutinib/(±)-泽布替尼 技术信息

CAS号1633350-06-7
分子式C27H29N5O3
分子量 471.55
SMILES Code O=C(C1=C2NCCC(C3CCN(C(C=C)=O)CC3)N2N=C1C4=CC=C(OC5=CC=CC=C5)C=C4)N
MDL No. MFCD30738015
别名 (±)-BGB-3111
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 30 mg/mL(63.62 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 8 mg/mL(16.97 mM),注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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