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Ralimetinib dimesylate

产品编号 T6047 CAS 862507-23-1

别名: LY2228820 dimesylate, Ralimetinib, LY2228820, Ralimetinib Mesylate

Ralimetinib dimesylate (LY2228820 dimesylate) 是一种选择性，ATP 竞争性的 p38 MAPK α/β抑制剂，IC50分别为5.3 和 3.2 nM。

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Ralimetinib dimesylate Chemical Structure

Ralimetinib dimesylate, CAS 862507-23-1

规格	价格/CNY	货期
2 mg	￥ 445	现货
5 mg	￥ 751	现货
10 mg	￥ 1,272	现货
50 mg	￥ 2,850	现货
100 mg	￥ 4,230	现货
1 mL * 10 mM (in DMSO)	￥ 997	现货

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其他形式的 Ralimetinib dimesylate:

Ralimetinib
询价

选择批次

纯度: 99.38%

纯度: 98.59%

纯度: 98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ralimetinib dimesylate (LY2228820 dimesylate) is the dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities.
靶点活性	p38α:7 nM
体外活性	LY2228820 inhibits p38α, as well as the level of phosphoMAPKAPK-2 (pMK2) in RAW 264.7 cells, with IC50 values of 7 nM and 34.3 nM, respectively. Furthermore, LY2228820 inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC50 of 5.2 nM. [1] In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, LY2228820 (200 nM–800 nM) significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. LY2228820 (200 nM–400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but LY2228820 alone doesn't inhibit the growth of MM.1S cells. LY2228820 (200 nM–800 nM) also inhibits secretion of IL-6 and MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138+, CD138? or PB CD14+ cells. LY2228820 (400 nM–800 nM) also blocks osteoclastogenesis from CD14+ cells. [2]
体内活性	In LPS-induced mice, LY2228820 effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED50) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), LY2228820 displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED50)of 1.5 mg/kg. [1]
激酶实验	Inhibition of p38α: Inhibition of p38α is determined using recombinant human p38α in a standard filter binding protocol using ATP[γ-33P] and EGFR 21-mer peptide as substrate. Functional inhibition of TNFα in murine peritoneal macrophages is determined using LPS stimulation in the presence of LY2228820. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with LY2228820 and then stimulated with anisomycin. The level of p38α activity is detected using a phosphoMAPKAPK-2 (pMK2) (Thr 334) antibody which reacts with a residue specifically phosphorylated by p38α.
细胞实验	MTT assays and APO 2.7 staining are performed to assess cellular proliferation and induction of apoptosis, respectively. Viability is expressed as percent viable cells. Apoptosis in cells is evaluated by APO 2.7 staining. For detection of mitochondrial membrane protein 7A6 expressed in apoptotic cells, cells are incubated with APO 2.7 reagent for 20 min. Expression of APO 2.7 is determined using an EPICS XL flow cytometer.(Only for Reference)

别名	LY2228820 dimesylate, Ralimetinib, LY2228820, Ralimetinib Mesylate
分子量	612.74
分子式	C24H29FN6·2CH4O3S
CAS No.	862507-23-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 27.5 mg/mL (44.88 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.632 mL	8.1601 mL	16.3201 mL	40.8003 mL
	5 mM	0.3264 mL	1.632 mL	3.264 mL	8.1601 mL
	10 mM	0.1632 mL	0.816 mL	1.632 mL	4.08 mL
	20 mM	0.0816 mL	0.408 mL	0.816 mL	2.04 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Mader M, et al. Bioorg Med Chem Lett, 2008, 18(1), 179-183. 2. Ishitsuka K, et al. Br J Haematol, 2008, 141(5), 598-606. 3. Ishitsuka K, et al. Oncogene, 2005, 24(38), 5888-5896. 4. Dong W, Xie W, Liu Y, et al. Receptor tyrosine kinase inhibitors block proliferation of TGEV mainly through p38 mitogen-activated protein kinase pathways[J]. Antiviral Research. 2020, 173: 104651. 5. Chiang C, Zhang M, Wang D, et al. Therapeutic potential of targeting MKK3-p38 axis with Capsaicin for Nasopharyngeal Carcinoma[J]. Theranostics. 2020, 10(17): 7906.

文献引用

1. Chiang C, Zhang M, Wang D, et al. Therapeutic potential of targeting MKK3-p38 axis with Capsaicin for Nasopharyngeal Carcinoma. Theranostics. 2020, 10(17): 7906. 2. Dong W, Xie W, Liu Y, et al. Receptor tyrosine kinase inhibitors block proliferation of TGEV mainly through p38 mitogen-activated protein kinase pathways. Antiviral Research. 2020, 173: 104651

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ralimetinib dimesylate 862507-23-1 Apoptosis Autophagy MAPK p38 MAPK Ralimetinib Dimesylate LY 2228820 Dimesylate LY2228820 Dimesylate LY-2228820 Dimesylate LY 2228820 Inhibitor LY-2228820 LY2228820 dimesylate inhibit Ralimetinib LY2228820 Ralimetinib Mesylate inhibitor

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Ralimetinib dimesylate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords