Ralimetinib 2MsOH(LY2228820)

产品编号: DC8630
Ralimetinib 2MsOH(LY2228820)
结构式
862507-23-1
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中国地区超过5000个高品质化合物库存
应用领域
LY2228820 is a novel and potent p38MAPK inhibitor (the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively).
Cas No.: 862507-23-1
名称:
别名: Ralimetinib dimesylate; LY2228820 dimesylate; LY2228820 2MsOH; LY 2228820; LY-2228820
SMILES: CS(=O)(O)=O.CS(=O)(O)=O.FC1=CC=C(C2N=C(C(C)(C)C)NC=2C2=CC=C3C(N(C(=N3)N)CC(C)(C)C)=N2)C=C1
分子式: C26H37FN6O6S2
分子量: 612.74
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: LY2228820 is a novel and potent p38MAPK inhibitor (the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively).in vitro: 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. n 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. in vivo: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_3494_DC8630_862507-23-1
COA
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产品编号 产品名称 应用领域
DC8630 Ralimetinib 2MsOH(LY2228820) LY2228820 is a novel and potent p38MAPK inhibitor (the IC50 for p38αMAPK and p38βMAPK were 7 nM and 3 nM, respectively).