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/ BTK / RN486

RN486 {[allProObj[0].p_purity_real_show]}

货号：A694095

RN486 是一种有效、选择性、口服活性的Btk 抑制剂，IC50 为 4.0 nM，Kd 为 0.31 nM，对其他激酶活性较低， 可用于类风湿性关节炎和系统性红斑狼疮的研究。

RN486 化学结构 CAS号：1242156-23-5
RN486 化学结构
CAS号：1242156-23-5
RN486 3D分子结构
CAS号：1242156-23-5
RN486 化学结构 CAS号：1242156-23-5
RN486 3D分子结构 CAS号：1242156-23-5
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RN486 纯度/质量文件 产品仅供科研

货号：A694095 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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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。

RN486 生物活性

靶点

  • BTK

    BTK, IC50:4 nM
描述 RN486 is a selective Btk inhibitor with an IC50 Value of 4.0 nM.

RN486 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293/B1G2 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
HEK293/G2 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
HEK293/B1 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
HEK293/PEL 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
S1-M1-80 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
S1 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
NCI-H460/MX20 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
NCI-H460 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
NCI-H2228 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
NCI-H1975 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
Calu-6 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
SK-Lu-1 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
Murine neonatal cardiomyocytes (CMs) 25 μM 24 hours To evaluate the protective effect of NG-R1 on hypoxia/reoxygenation-induced apoptosis. Results showed that NG-R1 significantly inhibited apoptosis, reduced LDH release, and improved cell viability. Front Cell Dev Biol. 2020 Aug 27;8:865.

RN486 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57/BL6 mice Myocardial ischemia/reperfusion injury model Intraperitoneal injection 25 mg/kg Every 2 hours for a total of 3 times, starting 30 minutes before ischemic surgery To evaluate the protective effect of NG-R1 on myocardial ischemia/reperfusion injury. Results showed that NG-R1 significantly reduced myocardial infarction area, alleviated myocardial cell damage, and improved cardiac function. Front Cell Dev Biol. 2020 Aug 27;8:865.

RN486 参考文献

[1]Hsu J, Gu Y, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104.

[2]Xu D, Kim Y, et al. RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.

RN486 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.24mL

1.65mL

0.82mL

16.48mL

3.30mL

1.65mL

RN486 技术信息

CAS号1242156-23-5
分子式C35H35FN6O3
分子量 606.69
SMILES Code O=C1N(C2=CC=CC(C(C=C3NC4=NC=C(N5CCN(C)CC5)C=C4)=CN(C)C3=O)=C2CO)C=CC6=C1C(F)=CC(C7CC7)=C6
MDL No. MFCD24682729
别名
运输蓝冰
InChI Key ZTUJNJAKTLHBEX-UHFFFAOYSA-N
Pubchem ID 46908026
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 20 mg/mL(32.97 mM)，配合低频超声，并水浴加热至45℃助溶，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

Tags: RN486 | 1242156-23-5 | RN 486 | RN-486 | Btk Inhibitor | Protein Tyrosine Kinase/RTK | Btk | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | RN486 纯度/质量文件 | RN486 亚型比较 | RN486 生物活性 | RN486 参考文献 | RN486 实验方案 | RN486 技术信息

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