Ralimetinib (LY2228820) dimesylate

Ralimetinib (LY2228820) dimesylate 是一种新型有效的p38 MAPK抑制剂,无细胞试验中IC50为7 nM,不改变p38 MAPK的活化。Phase 1/2。

Ralimetinib (LY2228820) dimesylate Chemical Structure

Ralimetinib (LY2228820) dimesylate Chemical Structure

CAS: 862507-23-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2344.86 现货
5mg RMB 1403.05 现货
50mg RMB 7927.27 现货
1g RMB 24488.1 现货
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客户使用Selleck的Ralimetinib (LY2228820) dimesylate发表文献76

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批次: 纯度: 99.66%
99.58

Ralimetinib (LY2228820) dimesylate相关产品

相关信号通路图

p38 MAPK抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
U-87-MG Function assay 1 μM reduces tumor-driven cord formation 23335506
CD14+ Function assay ~800 nM inhibits osteoclastogenesis from CD14 positive cells 18397345
INA-6 Cytoxicity assay ~1000 nM no significant cytotoxicity 18397345
RPMI-LR5 Cytoxicity assay ~1000 nM no significant cytotoxicity 18397345
RPMI-Dox40 Cytoxicity assay ~1000 nM no significant cytotoxicity 18397345
MM.1S Cytoxicity assay ~1000 nM no significant cytotoxicity 18397345
U266 Cytoxicity assay ~1000 nM no significant cytotoxicity 18397345
RPMI-8226 Cytoxicity assay ~1000 nM no significant cytotoxicity 18397345
INA-6 Kinase assay ~800 nM inhibits phosphorylation of HSP27 18397345
RPMI-LR5 Kinase assay ~800 nM inhibits phosphorylation of HSP27 18397345
RPMI-Dox40 Kinase assay ~800 nM inhibits phosphorylation of HSP27 18397345
MM.1S Kinase assay ~800 nM inhibits phosphorylation of HSP27 18397345
U266 Kinase assay ~800 nM inhibits phosphorylation of HSP27 18397345
RPMI-8226 Kinase assay ~800 nM inhibits phosphorylation of HSP27 18397345
MDA-MB-231 Function assay 1 μM reduces tumor-driven cord formation 23335506
A-2780 Function assay 1 μM reduces tumor-driven cord formation 23335506
SK-OV-3 Function assay 1 μM reduces tumor-driven cord formation 23335506
LXFA-629 Function assay 1 μM reduces tumor-driven cord formation 23335506
NCI-H1650 Function assay 1 μM reduces tumor-driven cord formation 23335506
PC-3 Function assay 1 μM reduces tumor-driven cord formation 23335506
RAW264.7 Function assay ~20 μM inhibits Anisomycin-stimulated MK2 phosphorylation with IC50 of 35.3 nM 24356814
mouse peritoneal macrophages Function assay ~20 μM LPS/IFN-γ–stimulated TNF-α production with IC50 of 6.3 nM 24356814
A549 Function assay ~20 μM inhibits LPS-induced CXCL8 production with IC50 of 144.9 nM 24356814
MDA-231 Function assay ~10 μM suppresses DKK-1 expression 26407843
MCF-7 Function assay ~10 μM suppresses DKK-1 expression 26407843
MDA-435 Function assay ~10 μM suppresses DKK-1 expression 26407843
PC3 Function assay ~10 μM suppresses DKK-1 expression 26913608
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
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生物活性

产品描述 Ralimetinib (LY2228820) dimesylate 是一种新型有效的p38 MAPK抑制剂,无细胞试验中IC50为7 nM,不改变p38 MAPK的活化。Phase 1/2。
特性 LY2228820是新型有效的p38有丝分裂原活化蛋白激酶(MAPK)通路抑制剂。
靶点
p38α [1]
(Cell-free assay)
7 nM
体外研究(In Vitro)
体外研究活性 LY2228820作用于RAW 264.7细胞,抑制p38α,和磷酸MAPKAPK-2(pMK2)水平,IC50分别为7 nM 和 34.3 nM。而且, LY2228820作用于小鼠腹腔巨噬细胞,抑制脂多糖 (LPS)-诱导的TNFα形成, IC50为5.2 nM。[1] 200 nM-800 nM LY2228820作用于多发性骨髓瘤(MM)细胞, 包括INA6, RPMI-8226, U266, 和RPMI-Dox40,通过抑制HSP27磷酸化而显著抑制p38MAPK信号, HSP27是p38MAPK下游靶点,不影响 HSP27表达水平。200 nM-400 nM LY2228820增强Bortezomib诱导的细胞毒性和凋亡, 但是LY2228820 单独处理不会抑制MM.1S细胞生长。200 nM-800 nM LY2228820作用于长期骨髓基质干细胞(LT-BMSCs),骨髓单个核细胞(BMMNCs),外周血(PB)CD138+,CD138-或外周血(PB)CD14+细胞,也抑制IL-6和MIP-1α分泌。400 nM-800 nM LY2228820也抑制CD14+ 细胞形成破骨细胞。[2]
激酶实验 抑制p38α实验
使用重组人p38α 在标准过滤器中使用ATP[γ-33P] 和EGFR 21肽底物测定抑制p38α的效果。在LY2228820存在时,使用LPS刺激,在小鼠腹腔巨噬细胞测定抑制TNFα效果。在使用LY2228820处理,然后用Anisomycin刺激的RAW 264.7细胞中测定p38α活性。使用磷酸MAPKAPK-2(pMK2)(Thr 334)抗体测定p38α活性水平。
细胞实验 细胞系 MM细胞,包括 INA6, RPMI-8226, U266,和RPMI-Dox40
浓度 200 nM-800 nM
孵育时间 48小时
方法 进行MTT实验和APO 2.7 染色分别测定细胞增殖和凋亡诱导。测定活细胞百分数作为可活力。通过APO 2.7染色测定凋亡。为了测定凋亡细胞中线粒体膜蛋白7A6的表达,用APO 2.7试剂处理细胞20分钟。使用EPICS XL流式细胞仪测定APO 2.7的表达。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27 p-S6K 23335506
体内研究(In Vivo)
体内研究活性 LY2228820 作用于LPS诱导的小鼠,有效抑制TNFα 形成,半数有效剂量最小阈值 (TMED 50)小于1 mg/kg。LY2228820 作用于患胶原性关节炎(CIA)大鼠模型,有效作用于足肿胀, 骨质糜烂, 和软骨破坏, 半数有效剂量最小阈值(TMED50)为 1.5 mg/kg。[1]
动物实验 Animal Models 脂多糖(LPS)-诱导的Balb/c小鼠
Dosages 0-20 mg/kg
Administration 口服处理,每天两次,持续14天
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02860780 Completed
Advanced Cancer|Metastatic Cancer|Colorectal Cancer|Non-small Cell Lung Cancer
Eli Lilly and Company
August 10 2016 Phase 1
NCT02364206 Completed
Adult Glioblastoma
Centre Jean Perrin|National Cancer Institute France|ARC Foundation for Cancer Research
June 8 2015 Phase 1|Phase 2
NCT02322853 Terminated
Postmenopausal|Metastatic Breast Cancer
Centre Francois Baclesse|National Cancer Institute France|ARC Foundation for Cancer Research
January 2015 Phase 2
NCT01393990 Completed
Advanced Cancer
Eli Lilly and Company
September 4 2008 Phase 1

化学信息&溶解度

分子量 612.74 分子式

C24H29FN6.2CH4O3S

CAS号 862507-23-1 SDF Download Ralimetinib (LY2228820) dimesylate SDF
Smiles CC(C)(C)CN1C2=C(C=CC(=N2)C3=C(N=C(N3)C(C)(C)C)C4=CC=C(C=C4)F)N=C1N.CS(=O)(=O)O.CS(=O)(=O)O
储存条件(自收到货起)

体外溶解度
批次:

Water : 100 mg/mL

Ethanol : 20 mg/mL

DMSO : 4 mg/mL ( 6.52 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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