Ralimetinib (LY2228820)


Ralimetinib (LY2228820)化学構造


Ralimetinib (LY2228820) is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.

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JPY 28220.00
JPY 53120.00
JPY 161020.00


  • CD34 expression after 14 days of culture of CB CB CD34+ cells treated with the P38α inhibitor Ly2228820 or vehicle (DMSO; n=3). Error bars represent SEM.

    Blood 2012 119, 6255-8. Ralimetinib (LY2228820) purchased from Selleck.

    Cell cycle phase distributions were determined on U87EV and U87PTEN cell treated with B, +/- rapamycin and +/- LY2228820 as shown. Percent apoptotic cells as determined via annexin V staining is also shown below each graph. D were identical to B, except LN229MER-AKT and LN229EV cells induced with 4OHT were used.

    Mol Cancer Ther 2011 10, 2244-56. Ralimetinib (LY2228820) purchased from Selleck.

  • Cells were treated with 100-mU/mL bTSH with or without 1μM LY2228820. After 5 days, OPN expression (C) was determined by RT-qPCR. OPN secretion was determined by ELISA in cell culture medium. The bars represent the mean ± SEM of 3 experiments with at least 2 biological replicates.

    Endocrinology, 2016, 157(5):2173-81. Ralimetinib (LY2228820) purchased from Selleck.

    Relationship of JNK, p38 MAPK, and PI3K activation in TNF-α-induced signaling. Western blot analysis of the effect of another p38 MAPK inhibitor, LY2228820, on TNF-α signaling. HUVECs were pretreated with LY2228820 (10 umol/L) or wortmannin (1 umol/L) for 1 h, followed by stimulation with TNF-α (5 ng/mL) for 15 min (n=2).

    Acta Pharmacol Sin 2014 35, 339-50. Ralimetinib (LY2228820) purchased from Selleck.

  • Neuroscience, 2018, 374:61-69. Ralimetinib (LY2228820) purchased from Selleck.

    For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of LY2228820 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. Ralimetinib (LY2228820) purchased from Selleck.


p38 MAPK阻害剤の選択性比較


製品説明 Ralimetinib (LY2228820) is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
p38α [1]
(Cell-free assay)
7 nM

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]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 M4HmbGtqdmG|ZTDhd5NigQ>? NEX3Omh,QDByIH7N NHLsdVhFVVOR MorjbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 MVGxPFM6PzN2NR?=
U266 M4\lR2tqdmG|ZTDhd5NigQ>? NF;EOmR,QDByIH7N M3XZbWROW09? MVXpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MV2xPFM6PzN2NR?=
MM.1S NYq1RmlYU2mwYYPlJIF{e2G7 NXy0W3BkhjhyMDDuUS=> NWLmSGx5TE2VTx?= NVzI[2dEcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 MmDaNVg{QTd|NEW=
RPMI-Dox40 M4n0V2tqdmG|ZTDhd5NigQ>? NVq5UmszhjhyMDDuUS=> M2nFNWROW09? NIe1[WhqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= M13HelE5Ozl5M{S1
RPMI-LR5 NEHmSnFMcW6jc3WgZZN{[Xl? NHPyc5V,QDByIH7N MlfiSG1UVw>? MlvObY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M3y2PVE5Ozl5M{S1
INA-6 MULLbY5ie2ViYYPzZZk> MVj+PFAxKG6P NU\mcIRbTE2VTx?= MYDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MWexPFM6PzN2NR?=
RPMI-8226 M3T3VGN6fG:6aXPpeJkh[XO|YYm= NV\YbldNhjFyMECgcm0> M4jETWROW09? M3\4co5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NV\2V3BSOTh|OUezOFU>
U266 NWTsXZU6S3m2b4jpZ4l1gSCjc4PhfS=> MlLWglExODBibl2= MmTXSG1UVw>? M1ixSo5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> MWWxPFM6PzN2NR?=
MM.1S M1L6TmN6fG:6aXPpeJkh[XO|YYm= MkDYglExODBibl2= M4m1bGROW09? NV3ZOYlldm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 MmXqNVg{QTd|NEW=
RPMI-Dox40 NXTMW|c6S3m2b4jpZ4l1gSCjc4PhfS=> Mof4glExODBibl2= NGjJd45FVVOR NU\tR2NNdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 MXyxPFM6PzN2NR?=
RPMI-LR5 NHLjU4tEgXSxeHnjbZR6KGG|c3H5 M4\MRp4yODByIH7N Mlj0SG1UVw>? NV;sO4Rndm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 MXSxPFM6PzN2NR?=
INA-6 M1LLVmN6fG:6aXPpeJkh[XO|YYm= MmTQglExODBibl2= Mn7tSG1UVw>? NGnIbI5vdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> MkO1NVg{QTd|NEW=
CD14+ MVXGeY5kfGmxbjDhd5NigQ>? M1;L[545ODBibl2= NU\tN5p2TE2VTx?= MYnpcohq[mm2czDvd5Rmd2OuYYP0c4dmdmW|aYOg[pJwdSCFREG0JJBwe2m2aY\lJINmdGy| NXLqW3B2OTh|OUezOFU>
U-87-MG NIfTenRHfW6ldHnvckBie3OjeR?= MlPaNUDPxE1? Mn7XSG1UVw>? NYfQUYpkemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NUTGeXk3OjN|M{W1NFY>
MDA-MB-231 NIDPRWpHfW6ldHnvckBie3OjeR?= MmrzNUDPxE1? NYXlflNrTE2VTx?= M{LFZ5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M2\JNVI{OzN3NUC2
A-2780 NHn5[npHfW6ldHnvckBie3OjeR?= M3W4VlEh|ryP M1OyNWROW09? M3PHOZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MYqyN|M{PTVyNh?=
SK-OV-3 NIPRS3JHfW6ldHnvckBie3OjeR?= MoXFNUDPxE1? NH20bGVFVVOR MVzy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= M3nLSVI{OzN3NUC2
LXFA-629 M37LZWZ2dmO2aX;uJIF{e2G7 Mn72NUDPxE1? NFnsUmtFVVOR MUPy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NVnQeWV{OjN|M{W1NFY>
NCI-H1650 M3TacGZ2dmO2aX;uJIF{e2G7 MlywNUDPxE1? MVTEUXNQ M3K0WpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NVjueXZROjN|M{W1NFY>
PC-3 MUXGeY5kfGmxbjDhd5NigQ>? NIjWcFYyKM7:TR?= NIrPWIhFVVOR NGfBRm9z\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M1S0UFI{OzN3NUC2
RAW264.7 Mn2wSpVv[3Srb36gZZN{[Xl? NYrxNHBshjJyIN88US=> NFfUWIZFVVOR M1e0UolvcGmkaYTzJGFvcXOxbYnjbY4ue3SrbYXsZZRm\CCPS{KgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kA{PS5|IH7N NYPJcGR5OjR|NU[4NVQ>
mouse peritoneal macrophages MVzGeY5kfGmxbjDhd5NigQ>? NFHhfpl,OjBizszN NF7kc5hFVVOR NIDTOWhNWFNxSV\OMe6{6oDVc4TpcZVt[XSnZDDUUmYu|rFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhPi5|IH7N MmC4NlQ{PTZ6MUS=
A549 M2HFe2Z2dmO2aX;uJIF{e2G7 M2X6TZ4zOCEQvF2= NVjvR4JwTE2VTx?= MWrpcohq[mm2czDMVHMucW6mdXPl[EBEYEOOODDwdo9lfWO2aX;uJJdqfGhiSVO1NEBw\iBzNESuPUBvVQ>? M37NfFI1OzV4OEG0
MDA-231 NVK5eZZuTnWwY4Tpc44h[XO|YYm= NIDvSFF,OTBizszN NH3CPHp{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> NH\NSYIzPjRyN{i0Ny=>
MCF-7 MnnhSpVv[3Srb36gZZN{[Xl? NHjoPIR,OTBizszN M3LKb5N2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> MofLNlY1ODd6NEO=
MDA-435 NEDNNYFHfW6ldHnvckBie3OjeR?= MnroglExKM7:TR?= M1X5UZN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NWjROZNMOjZ2MEe4OFM>
PC3 M4LMUWZ2dmO2aX;uJIF{e2G7 NYTnSWFjhjFyIN88US=> MmTUSG1UVw>? MV3zeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MUOyOlkyOzZyOB?=


体内試験 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]


+ 展開

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.
細胞試験: [2, 3]
+ 展開
  • 細胞株: MM cells, including INA6, RPMI-8226, U266, and RPMI-Dox40
  • 濃度: 200 nM–800 nM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
+ 展開
  • 動物モデル: Lipopolysaccharide (LPS)-induced Balb/c mice
  • 製剤: Dissolved in 1% CMC/0.25% Tween 80 in water
  • 投薬量: 0–20 mg/kg
  • 投与方法: Oral bid dosing for 14 days

溶解度 (25°C)

体外 Water 100 mg/mL (163.2 mM) warming
DMSO 4 mg/mL warmed (6.52 mM)
Ethanol 3 mg/mL (4.89 mM)
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 612.74


CAS No. 862507-23-1
in solvent
別名 N/A





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02364206 Active not recruiting 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
NCT01663857 Completed Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Eli Lilly and Company July 2012 Phase 1|Phase 2
NCT01393990 Completed Advanced Cancer Eli Lilly and Company August 2008 Phase 1



Handling Instructions


  • * 必須

p38 MAPKシグナル伝達経路

p38 MAPK Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID