Ralimetinib dimesylate | p38 MAPK | AmBeed-信号通路专用抑制剂

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Ralimetinib dimesylate 98%

货号：A413122

LY2228820 is a potent p38MAPK inhibitor with IC50 of 7 nM and 3 nM for p38αMAPK and p38βMAPK.

Ralimetinib dimesylate 化学结构
CAS号：862507-23-1

Ralimetinib dimesylate 3D分子结构
CAS号：862507-23-1

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Ralimetinib dimesylate 纯度/质量文件产品仅供科研

货号：A413122 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

p38 MAPK 亚型比较

产品名称	p38 MAPK ↓ ↑	p38α ↓ ↑	p38β ↓ ↑	其他靶点	纯度
BMS-582949	+++ p38 MAPK, IC50: 13 nM				98%
SB 203580					99%+
Pexmetinib	✔			Tie-2	99%+
Skepinone-L		++++ p38α, IC50: 5 nM			98%
Doramapimod		++++ p38α, Kd: 0.1 nM p38α, IC50: 38 nM			99%+
VX-702					99%+
Ralimetinib dimesylate		++++ p38α, IC50: 7 nM			98%
SB 202190		++ p38α, IC50: 50 nM	++ p38β, IC50: 100 nM		99%+
Losmapimod		++++ p38α, pKi: 8.1	+++ p38β, pKi: 7.6		99%+
Neflamapimod		+++ p38α, IC50: 10 nM	+ p38β, IC50: 220 nM		99%+
PH-797804		++ p38α, IC50: 26 nM	+ p38β, IC50: 102 nM		98%
TAK-715		++++ p38α, IC50: 7.1 nM	+ p38β, IC50: 0.20 μM		99%+
SB 239063		++ p38α, IC50: 44 nM	++ p38β, IC50: 44 nM		99%+
Pamapimod		+++ p38α, IC50: 0.014 μM	+ p38β, IC50: 0.48 μM		98%+
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。

Ralimetinib dimesylate 生物活性

靶点

p38α

p38α, IC50:7 nM

描述

p38α mitogen-activated protein kinase (MAPK) is activated in cancer cells in response to environmental factors, oncogenic stress, radiation, and chemotherapy. p38α MAPK phosphorylates a number of substrates, including MAPKAP-K2 (MK2), and regulates the production of cytokines in the tumor microenvironment, such as TNF-α, interleukin-1β (IL-1β), IL-6, and CXCL8 (IL-8)^[3]. LY2228820 is a novel and effective p38α MAPK inhibitor with an IC₅₀ value of 7 nM in cell free assay. To assess p38α activity in cells more directly, RAW 264.7 cells were treated with LY2228820. It inhibited p38α and the level of pMK2 (phospho-MAPKAP-K2) with IC₅₀s of 7 nM and 34.3 nM, respectively. LY2228820 was orally dosed in Balb/c mice followed by iv LPS administration after 2 h. And the threshold minimum 50% effective dose (TMED₅₀) was less than 1 mg/kg. In the rat CIA (collagen induced arthritis) model, LY2228820 effectively acting on foot swelling, bone erosion, and cartilage destruction, with the TMED₅₀ of 1.5 mg/kg^[4].

Ralimetinib dimesylate 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A-2780	1 μM	Function assay		reduces tumor-driven cord formation	23335506
A549	~20 μM	Function assay		inhibits LPS-induced CXCL8 production with IC50 of 144.9 nM	24356814
CD14+	~800 nM	Function assay		inhibits osteoclastogenesis from CD14 positive cells	18397345
INA-6	~800 nM	Kinase assay		inhibits phosphorylation of HSP27	18397345

Ralimetinib dimesylate 参考文献

[1] Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity

[2]Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties

Ralimetinib dimesylate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.63mL

0.33mL

0.16mL

8.16mL

1.63mL

0.82mL

16.32mL

3.26mL

1.63mL

Ralimetinib dimesylate 技术信息

CAS号	862507-23-1
分子式	C₂₆H₃₇FN₆O₆S₂
分子量	612.737

别名
运输	蓝冰

存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 60 mg/mL(97.92 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

H₂O: 30 mg/mL(48.96 mM)

动物实验配方

PO 0.5% CMC-Na 20 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A-2780	1 μM	Function assay	reduces tumor-driven cord formation	23335506
A549	~20 μM	Function assay	inhibits LPS-induced CXCL8 production with IC50 of 144.9 nM	24356814
CD14+	~800 nM	Function assay	inhibits osteoclastogenesis from CD14 positive cells	18397345
INA-6	~800 nM	Kinase assay	inhibits phosphorylation of HSP27	18397345
INA-6	~1000 nM	Cytoxicity assay	no significant cytotoxicity	18397345
LXFA-629	1 μM	Function assay	reduces tumor-driven cord formation	23335506
MCF-7	~10 μM	Function assay	suppresses DKK-1 expression	26407843
MDA-231	~10 μM	Function assay	suppresses DKK-1 expression	26407843
MDA-435	~10 μM	Function assay	suppresses DKK-1 expression	26407843
MDA-MB-231	1 μM	Function assay	reduces tumor-driven cord formation	23335506
MM.1S	~800 nM	Kinase assay	inhibits phosphorylation of HSP27	18397345
MM.1S	~1000 nM	Cytoxicity assay	no significant cytotoxicity	18397345
mouse peritoneal macrophages	~20 μM	Function assay	LPS/IFN-γ–stimulated TNF-α production with IC50 of 6.3 nM	24356814
NCI-H1650	1 μM	Function assay	reduces tumor-driven cord formation	23335506
PC3	~10 μM	Function assay	suppresses DKK-1 expression	26913608
PC-3	1 μM	Function assay	reduces tumor-driven cord formation	23335506
RAW264.7	~20 μM	Function assay	inhibits Anisomycin-stimulated MK2 phosphorylation with IC50 of 35.3 nM	24356814
RPMI-8226	~800 nM	Kinase assay	inhibits phosphorylation of HSP27	18397345
RPMI-8226	~1000 nM	Cytoxicity assay	no significant cytotoxicity	18397345
RPMI-Dox40	~800 nM	Kinase assay	inhibits phosphorylation of HSP27	18397345
RPMI-Dox40	~1000 nM	Cytoxicity assay	no significant cytotoxicity	18397345
RPMI-LR5	~800 nM	Kinase assay	inhibits phosphorylation of HSP27	18397345
RPMI-LR5	~1000 nM	Cytoxicity assay	no significant cytotoxicity	18397345
SK-OV-3	1 μM	Function assay	reduces tumor-driven cord formation	23335506
U266	~800 nM	Kinase assay	inhibits phosphorylation of HSP27	18397345
U266	~1000 nM	Cytoxicity assay	no significant cytotoxicity	18397345
U-87-MG	1 μM	Function assay	reduces tumor-driven cord formation	23335506

Ralimetinib dimesylate 98%

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Ralimetinib dimesylate 98%

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Ralimetinib dimesylate 生物活性

Ralimetinib dimesylate 细胞研究

Ralimetinib dimesylate 参考文献

Ralimetinib dimesylate 实验方案

Ralimetinib dimesylate 技术信息

最近浏览的产品

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