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/ BTK / ARQ 531

ARQ 531 {[allProObj[0].p_purity_real_show]}

货号：A630399 同义名： Nemtabrutinib;MK-1026

ARQ-531 is a potent and orally active BTK inhibitor with potential antineoplastic activity.

ARQ 531 化学结构 CAS号：2095393-15-8
ARQ 531 化学结构
CAS号：2095393-15-8
ARQ 531 3D分子结构
CAS号：2095393-15-8
ARQ 531 化学结构 CAS号：2095393-15-8
ARQ 531 3D分子结构 CAS号：2095393-15-8
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ARQ 531 纯度/质量文件 产品仅供科研

货号：A630399 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

ARQ 531 生物活性

描述 The Bruton’s tyrosine kinase (BTK) has been shown to drive the development of chronic lymphocytic leukemia (CLL). ARQ 531 is an ATP-competitive, reversible inhibitor of BTK with IC50 values of 0.85 and 0.39nM for wild-type BTK and C481S BTK, respectively. ARQ 531 also shows inhibitory activities against Src family kinases (LCK, YES, BLK, HCK, LYNa, FGR, FYN, FRK), TEK kinases (BMX, TEC, TXK), and Trk kinases (TrkB, TrkA, TrkC) with IC50 values ranging from 2.5–48nM. ARQ 531 at 0.1, 1, and 10μM decreased the viability of CLL cells by 19%, 40%, and 59%, respectively. Treatment with 1μM ARQ 531 significantly decreased the transcription of MYC, MCL1, and CD40 in CLL cells by 73%, 23%, 40%, respectively, compared to the vehicle controls. ARQ 531 at 1μM also decreased the migration of primary CLL cells towards CXCL12 and CXCL13 by 51% and 66%, respectively. In an Eμ-TCL1 mouse model of CLL, ARQ 531 treatment at either 50 or 75mg/kg significantly improved the survival of animals over ibrutinib (25mg/kg) treatment. In a murine model of aggressive lymphoma, ARQ 531 at a dosage of 75mg/kg prolonged survival (median survival = 47 days) compared to ibrutinib-treated (median survival = 38 days) and vehicle-treated (median survival = 35.5 days) groups[1].

ARQ 531 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03162536 Lymphoma, B-Cell ... 展开 >> Small Lymphocytic Lymphoma Chronic Lymphocytic Leukemia Waldenstrom Macroglobulinemia Mantle Cell Lymphoma Diffuse Large B Cell Lymphoma 收起 << Phase 1 Recruiting April 2019 United States, Ohio ... 展开 >> Wexner Medical Center at The Ohio State University Recruiting Columbus, Ohio, United States, 43210 Contact    781-994-0300    ClinicalTrials@arqule.com    United States, Tennessee Sarah Cannon Research Institute Recruiting Nashville, Tennessee, United States, 37203 Contact    781-994-0300    ClinicalTrials@arqule.com    United States, Utah University of Utah, Huntsman Cancer Institute Recruiting Salt Lake City, Utah, United States, 84112 Contact    781-994-0300    ClinicalTrials@arqule.com 收起 <<

ARQ 531 参考文献

[1]Reiff SD, Mantel R, Smith LL, Greene JT, Muhowski EM, Fabian CA, Goettl VM, Tran M, Harrington BK, Rogers KA, Awan FT, Maddocks K, Andritsos L, Lehman AM, Sampath D, Lapalombella R, Eathiraj S, Abbadessa G, Schwartz B, Johnson AJ, Byrd JC, Woyach JA. The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation. Cancer Discov. 2018 Oct;8(10):1300-1315.

ARQ 531 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.44mL

2.09mL

1.04mL

20.88mL

4.18mL

2.09mL

ARQ 531 技术信息

CAS号2095393-15-8
分子式C25H23ClN4O4
分子量 478.928
别名 Nemtabrutinib;MK-1026
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C
溶解度

DMSO: 50 mg/mL(104.4 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
动物实验配方

Tags: Nemtabrutinib | 2095393-15-8 | ARQ-531 | MK-1026 | ARQ531 | ARQ 531 | MK1026 | MK 1026 | MK-1026 | BTK Inhibitor | Protein Tyrosine Kinase/RTK | Btk | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | ARQ 531 纯度/质量文件 | ARQ 531 亚型比较 | ARQ 531 生物活性 | ARQ 531 临床数据 | ARQ 531 参考文献 | ARQ 531 实验方案 | ARQ 531 技术信息

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