Ralimetinib (LY2228820)

製品コードS1494

Ralimetinib (LY2228820)化学構造

分子量(MW):612.74

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.

サイズ 価格(税別)  
JPY 28220.00
JPY 53120.00
JPY 161020.00

カスタマーフィードバック(6)

  • 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.

製品安全説明書

p38 MAPK阻害剤の選択性比較

生物活性

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.
ターゲット
p38α [1]
(Cell-free assay)
7 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 MXzLbY5ie2ViYYPzZZk> MmD2glgxOCCwTR?= NGnTdm9FVVOR M4DsS4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MXWxPFM6PzN2NR?=
U266 MWnLbY5ie2ViYYPzZZk> NXu5bnJChjhyMDDuUS=> NYHoZpl{TE2VTx?= NEnZO4xqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= M3;le|E5Ozl5M{S1
MM.1S M2DTcmtqdmG|ZTDhd5NigQ>? MXH+PFAxKG6P NYPMcoo1TE2VTx?= M{TiWolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MXexPFM6PzN2NR?=
RPMI-Dox40 NWK4Wo53U2mwYYPlJIF{e2G7 NIX0bWd,QDByIH7N MYTEUXNQ M2PyXIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= Mn3aNVg{QTd|NEW=
RPMI-LR5 NHntSZpMcW6jc3WgZZN{[Xl? M3y4d545ODBibl2= MYPEUXNQ NGDmV|JqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NIPHVY0yQDN7N{O0OS=>
INA-6 NFWxRnhMcW6jc3WgZZN{[Xl? MnHiglgxOCCwTR?= M37UOmROW09? MVzpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MnO4NVg{QTd|NEW=
RPMI-8226 MlLQR5l1d3irY3n0fUBie3OjeR?= NIfRbIZ,OTByMDDuUS=> NUPMeJJETE2VTx?= MoPVco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M1TQTVE5Ozl5M{S1
U266 MnrJR5l1d3irY3n0fUBie3OjeR?= NHfUeYZ,OTByMDDuUS=> NXnnV2hzTE2VTx?= NVztT2JXdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NEnoNIsyQDN7N{O0OS=>
MM.1S Mo\FR5l1d3irY3n0fUBie3OjeR?= NF7SeWF,OTByMDDuUS=> NY\ycYhCTE2VTx?= Mlq3co8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M1TvV|E5Ozl5M{S1
RPMI-Dox40 Mkf3R5l1d3irY3n0fUBie3OjeR?= MmSwglExODBibl2= M{TVXmROW09? M3y2UY5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NGP6T4gyQDN7N{O0OS=>
RPMI-LR5 MkLWR5l1d3irY3n0fUBie3OjeR?= M2TCUp4yODByIH7N NE\KW4hFVVOR NHfDRYxvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NIfocIkyQDN7N{O0OS=>
INA-6 NX32XVlGS3m2b4jpZ4l1gSCjc4PhfS=> NH[1eYZ,OTByMDDuUS=> NXPNcphJTE2VTx?= NGTxWnVvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NFXTeFkyQDN7N{O0OS=>
CD14+ M1fZfGZ2dmO2aX;uJIF{e2G7 Mnz4glgxOCCwTR?= M{XjSmROW09? NW\lUIY1cW6qaXLpeJMhd3O2ZX;jcIF{fG:pZX7ld4l{KG[{b32gR2QyPCCyb4PpeIl3\SClZXzsdy=> MVOxPFM6PzN2NR?=
U-87-MG MWfGeY5kfGmxbjDhd5NigQ>? MVWxJO69VQ>? NIf4N29FVVOR NHP1e21z\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MmrzNlM{OzV3ME[=
MDA-MB-231 M3\mU2Z2dmO2aX;uJIF{e2G7 MmC1NUDPxE1? MYDEUXNQ MWLy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= M1T4U|I{OzN3NUC2
A-2780 NVu2O2Z2TnWwY4Tpc44h[XO|YYm= NV:w[FZjOSEQvF2= M{LLOmROW09? MmfwdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MVqyN|M{PTVyNh?=
SK-OV-3 NHHlS2hHfW6ldHnvckBie3OjeR?= NEPj[IcyKM7:TR?= NEi4Z|FFVVOR NFuwU49z\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M4\SclI{OzN3NUC2
LXFA-629 NUfNS2lITnWwY4Tpc44h[XO|YYm= MknZNUDPxE1? NYTiWVVpTE2VTx?= MVHy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MnPhNlM{OzV3ME[=
NCI-H1650 NGfwcGtHfW6ldHnvckBie3OjeR?= NVrHfJREOSEQvF2= NWfGcJp6TE2VTx?= NWTTOWlvemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NVHS[5J[OjN|M{W1NFY>
PC-3 MX3GeY5kfGmxbjDhd5NigQ>? NES4ZYcyKM7:TR?= MUPEUXNQ MojmdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NWX0eGJWOjN|M{W1NFY>
RAW264.7 NYLWfZhlTnWwY4Tpc44h[XO|YYm= MYL+NlAh|ryP MYfEUXNQ NX\yXJhZcW6qaXLpeJMhSW6rc3;tfYNqdi2|dHnteYxifGWmIF3LNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDN3LkOgcm0> Ml\QNlQ{PTZ6MUS=
mouse peritoneal macrophages M17vcWZ2dmO2aX;uJIF{e2G7 MUH+NlAh|ryP NWTQTmlHTE2VTx?= NVnVfmd5VFCVL1nGUk3Pu+LCk4P0bY12dGG2ZXSgWG5HNc7zIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDZwMzDuUS=> MoPkNlQ{PTZ6MUS=
A549 NYT1WII1TnWwY4Tpc44h[XO|YYm= MoDmglIxKM7:TR?= M2HFNWROW09? NEDDUohqdmirYnn0d{BNWFNvaX7keYNm\CCFWFPMPEBxem:mdXP0bY9vKHerdHigTWM2OCCxZjCxOFQvQSCwTR?= NFPvWpczPDN3NkixOC=>
MDA-231 M{HkPGZ2dmO2aX;uJIF{e2G7 NELUU3d,OTBizszN NWDOSW9Je3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v MWmyOlQxPzh2Mx?=
MCF-7 MWjGeY5kfGmxbjDhd5NigQ>? MVH+NVAh|ryP NWHGUWxFe3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v NXraTHJOOjZ2MEe4OFM>
MDA-435 MXfGeY5kfGmxbjDhd5NigQ>? MYD+NVAh|ryP MXjzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= M3nOd|I3PDB5OESz
PC3 Mne0SpVv[3Srb36gZZN{[Xl? NETxc2x,OTBizszN NX7BbnJpTE2VTx?= MVPzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NXHtSVNTOjZ7MUO2NFg>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[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.
    (参考用のみ)
動物試験:[1]
+ 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
    (参考用のみ)

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):
Saline
混合させたのち直ちに使用することを推奨します。
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。

化学情報

分子量 612.74
化学式

C24H29FN6.2CH4O3S

CAS No. 862507-23-1
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

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

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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
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
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
NCT01663857 Completed Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Eli Lilly and Company July 2012 Phase 1|Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 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