- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
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Ralimetinib (LY2228820) dimesylate
Ralimetinib (LY2228820) dimesylate 是一種新型有效的p38 MAPK抑制劑，無細(xì)胞試驗(yàn)中IC50為7 nM，不改變p38 MAPK的活化。Phase 1/2。
Ralimetinib (LY2228820) dimesylate Chemical Structure
CAS: 862507-23-1
產(chǎn)品質(zhì)控
批次：
純度：
99.63%
99.63
Ralimetinib (LY2228820) dimesylate相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | p38α p38β | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Adezmapimod (SB203580) SB202190 Doramapimod (BIRB 796) PH-797804 VX-702 Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L Asiatic Acid TAK-715 Pamapimod Pexmetinib SD 0006 R1487 PD 169316 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 MAPK抑制劑庫 細(xì)胞周期化合物庫 TGF-beta/Smad信號(hào)通路庫 抗阿爾茨海默病化合物庫 | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Ralimetinib (LY2228820) dimesylate 是一種新型有效的p38 MAPK抑制劑，無細(xì)胞試驗(yàn)中IC50為7 nM，不改變p38 MAPK的活化。Phase 1/2。 | ||
|---|---|---|---|
| 特性 | LY2228820是新型有效的p38有絲分裂原活化蛋白激酶(MAPK)通路抑制劑。 | ||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | LY2228820作用于RAW 264.7細(xì)胞，抑制p38α,和磷酸MAPKAPK-2(pMK2)水平,IC50分別為7 nM 和 34.3 nM。而且, LY2228820作用于小鼠腹腔巨噬細(xì)胞，抑制脂多糖 (LPS)-誘導(dǎo)的TNFα形成, IC50為5.2 nM。[1] 200 nM-800 nM LY2228820作用于多發(fā)性骨髓瘤(MM)細(xì)胞, 包括INA6, RPMI-8226, U266, 和RPMI-Dox40,通過抑制HSP27磷酸化而顯著抑制p38MAPK信號(hào), HSP27是p38MAPK下游靶點(diǎn),不影響 HSP27表達(dá)水平。200 nM-400 nM LY2228820增強(qiáng)細(xì)胞毒性和凋亡, 但是LY2228820 單獨(dú)處理不會(huì)抑制MM.1S細(xì)胞生長。200 nM-800 nM LY2228820作用于長期骨髓基質(zhì)干細(xì)胞(LT-BMSCs)，骨髓單個(gè)核細(xì)胞(BMMNCs)，外周血（PB）CD138+，CD138-或外周血（PB）CD14+細(xì)胞，也抑制IL-6和MIP-1α分泌。400 nM-800 nM LY2228820也抑制CD14+ 細(xì)胞形成破骨細(xì)胞。[2] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 抑制p38α實(shí)驗(yàn) | |||
| 使用重組人p38α 在標(biāo)準(zhǔn)過濾器中使用ATP[γ-33P] 和EGFR 21肽底物測定抑制p38α的效果。在LY2228820存在時(shí)，使用LPS刺激，在小鼠腹腔巨噬細(xì)胞測定抑制TNFα效果。在使用LY2228820處理，然后用Anisomycin刺激的RAW 264.7細(xì)胞中測定p38α活性。使用磷酸MAPKAPK-2(pMK2)(Thr 334)抗體測定p38α活性水平。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | MM細(xì)胞,包括 INA6, RPMI-8226, U266,和RPMI-Dox40 | ||
| 濃度 | 200 nM-800 nM | |||
| 孵育時(shí)間 | 48小時(shí) | |||
| 方法 | 進(jìn)行MTT實(shí)驗(yàn)和APO 2.7 染色分別測定細(xì)胞增殖和凋亡誘導(dǎo)。測定活細(xì)胞百分?jǐn)?shù)作為可活力。通過APO 2.7染色測定凋亡。為了測定凋亡細(xì)胞中線粒體膜蛋白7A6的表達(dá)，用APO 2.7試劑處理細(xì)胞20分鐘。使用EPICS XL流式細(xì)胞儀測定APO 2.7的表達(dá)。 |
|||
| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27 p-S6K |
|
23335506 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | LY2228820 作用于LPS誘導(dǎo)的小鼠，有效抑制TNFα 形成，半數(shù)有效劑量最小閾值 (TMED 50)小于1 mg/kg。LY2228820 作用于患膠原性關(guān)節(jié)炎(CIA)大鼠模型,有效作用于足腫脹, 骨質(zhì)糜爛, 和軟骨破壞, 半數(shù)有效劑量最小閾值(TMED50)為 1.5 mg/kg。[1] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 脂多糖(LPS)-誘導(dǎo)的Balb/c小鼠 |
| Dosages | 0-20 mg/kg | |
| Administration | 口服處理，每天兩次，持續(xù)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 |
化學(xué)信息&溶解度
| 分子量 | 612.74 | 分子式 | C24H29FN6.2CH4O3S |
| CAS號(hào) | 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 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (163.2 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO) Water : 100 mg/mL (163.2 mM) Ethanol : 7 mg/mL (11.42 mM) |
摩爾濃度計(jì)算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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