Doramapimod (BIRB 796)

目录号:S1574

Doramapimod (BIRB 796) Chemical Structure

Molecular Weight(MW): 527.66

Doramapimod (BIRB 796)是一种泛p38 MAPK抑制剂,在无细胞试验中作用于p38α/β/γ/δ的IC50分别为38 nM,65 nM,200 nM 和520 nM,并且能够与p38α结合,在THP-1细胞中Kd为0.1 nM,比作用于JNK2选择性高330倍,对c-RAF,Fyn 和Lck具有较弱的抑制作用,对ERK-1,SYK,IKK2也有微弱抑制作用。

规格 价格 库存 购买数量  
RMB 2403.35 现货
RMB 1221.86 现货
RMB 2215.96 现货
RMB 3866.11 现货
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客户使用该产品的5个实验数据:

  • Lympho-myeloid potential assessed by FACS analysis of human CD19 (B-lymphoid cells) and CD33/CD15 (myeloid cells) in bone marrow of NSG recipient mice, 17 weeks after transplantation. Each plot represents an animal from the experiment presented in panel.

    Blood 2012 119(26), 6255-8. Doramapimod (BIRB 796) purchased from Selleck.

    A p38α/ERK crosstalk exists in CRC cells and tissues. Use of a structurally and functionally different p38α inhibitor (BIRB-796) confirms ERK1/2 phospho-activation. Using BIRB-796 for up to 72 h triggers MEK-ERK1/2 signaling in HT-29 cells.

    Cancer Lett 2012 324(1), 98-108. Doramapimod (BIRB 796) purchased from Selleck.

  • Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.

    Int J Cancer 2014 134(3), 575-86. Doramapimod (BIRB 796) purchased from Selleck.

    Inhibition of p38 MAPK activity prevents induction of autophagy by glucose. NIH 3T3 cells were incubated in KH medium without glucose in the presence of the p38 MAPK inhibitor BIRB796 (50 nM, middle panels). After 30 min, glucose (10 mM) and lysosomal inhibitors were added to the indicated samples and cells were further incubated for 2 h. Cell lysates were collected and processed for SDS/PAGE. LC3 levels were detected and actin served as a loading control. The values shown in the histograms represent means盨.D. from three independent experiments with the LC3-II levels normalized to actin and expressed as a percentage of the values of KH medium without glucose. *P<0.05. Glc, glucose; w/o, without.

    Biochem J 2014 449(2), 497-506. Doramapimod (BIRB 796) purchased from Selleck.

  • Doramapimod (BIRB 796) purchased from Selleck.

产品安全说明书

p38 MAPK抑制剂选择性比较

生物活性

产品描述 Doramapimod (BIRB 796)是一种泛p38 MAPK抑制剂,在无细胞试验中作用于p38α/β/γ/δ的IC50分别为38 nM,65 nM,200 nM 和520 nM,并且能够与p38α结合,在THP-1细胞中Kd为0.1 nM,比作用于JNK2选择性高330倍,对c-RAF,Fyn 和Lck具有较弱的抑制作用,对ERK-1,SYK,IKK2也有微弱抑制作用。
特性 BIRB 796是第一个进入三期临床试验的p38 MAPK抑制剂。
靶点
p38α [1]
(Cell-free assay)
p38α [7]
0.1 nM(Kd) 38 nM
体外研究

BIRB 796作用于ERK-1,SYK,IKK2β,ZAP-70,EGFR激酶,HER2,蛋白激酶 A(PKA),PKC,PKC-α,PKC-β(I和II)和PKC-γ没有明显抑制效果。BIRB 796通过在吗啉氧和p38α的ATP结合域间形成氢键,显著提高亲和力。BIRB 796是作用于人类p38 MAPK的最有效和分离最慢的抑制剂之一。[1] BIRB 796 有效抑制c-Raf-1和Jnk2α2,IC50分别为1.4和0.1 nM。[2] 高浓度BIRB796也抑制SAPK3/p38γ的活性和激活。BIRB796阻断压力诱导的框架蛋白SAP97磷酸化, SAP97是SAPK3/p38γ的底物。BIRB796作用于HEK293细胞,阻断JNK1/2激活和活性,而作用于Hela细胞,不抑制ERK1/ERK2激活和活性。而且, BIRB796与p38 MAPKs或JNK1/2的结合,降低上游激酶MKK6或MKK4磷酸化,而不增强去磷酸化。 [3] BIRB 796 作用于TNF-α和TGF-β1引起的BMSCs,下调IL-6和VEGF分泌。[4] BIRB-796有吡唑环 ,使亲脂的末端异丁基基团 与低选择性位点结合,甲苯基环与高选择性位点结合。BIRB-796也抑制B-Raf和Abl,IC50分别为83 nM 和14.6 μM。 [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXwSmRKSzVyPUCuN|Q4PjNizszN M4rYPHNCVkeURWK=
DU-145 NX60dYxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTNwOUO4NVEh|ryP NUjEUHdPW0GQR2LFVi=>
GOTO MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHYTWM2OD14LkO5NVYyKM7:TR?= NFLWdXpUSU6JUlXS
NCI-H358 NE[xV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTdwNUO4JO69VQ>? MUDTRW5IWkWU
IST-MES1 M2j4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC4WWNsUUN3ME23Mlk2PjN5IN88US=> M37LNXNCVkeURWK=
KP-N-YN MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P5W2lEPTB;OD6yNFE6KM7:TR?= MknmV2FPT1KHUh?=
T-24 M1LPN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HKXGlEPTB;OD60NFY4OyEQvF2= M2fhOXNCVkeURWK=
MPP-89 M3\LT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q5OWlEPTB;OD60OlI2OSEQvF2= NYnRO|d2W0GQR2LFVi=>
NCI-SNU-1 M2OzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmmzTWM2OD17LkC2O|M6KM7:TR?= MVHTRW5IWkWU
BFTC-905 M3TMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHsUJM5UUN3ME2xNE4yOjN|IN88US=> M2T0T3NCVkeURWK=
MS-1 NY\ZbYptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTFyLkiyN|Uh|ryP MnTOV2FPT1KHUh?=
NBsusSR NV;kWmw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHmwPIJKSzVyPUGwMlgzOzVizszN MYHTRW5IWkWU
BEN MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDhTWM2OD1zMz6xNlY1KM7:TR?= NIrMdJlUSU6JUlXS
HMV-II NITLUWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTF2LkKzNFkh|ryP MVPTRW5IWkWU
NCI-H1581 NHXzXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\nd3RKSzVyPUG3MlA1PDdizszN NWDuPHIyW0GQR2LFVi=>
ES8 NFL2b4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTF5LkG2O{DPxE1? Mo[3V2FPT1KHUh?=
LC-2-ad MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELZOGxKSzVyPUG3MlQ{PjZizszN MXrTRW5IWkWU
EW-13 NHWzdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3XTWM2OD1zNz65OVE3KM7:TR?= NHHH[|lUSU6JUlXS
AN3-CA Mnu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DZbmlEPTB;MUiuNUDPxE1? MlTNV2FPT1KHUh?=
DB NHftSmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz1TWM2OD1zOD63PVI{KM7:TR?= MY\TRW5IWkWU
SK-MEL-1 MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJyLkO2PFMh|ryP MXrTRW5IWkWU
CAPAN-1 Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv6[nlZUUN3ME2yNk4yQDh2IN88US=> MkXaV2FPT1KHUh?=
NCI-H2228 M4LMPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTJ|Lk[2Olgh|ryP NWT4OJNZW0GQR2LFVi=>
HOP-92 M1Kzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\NPJdNUUN3ME2yOE4{QDN6IN88US=> NFnpPYNUSU6JUlXS
KYSE-270 NUOxZ|Y6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJ2LkW1O|Mh|ryP M3zFV3NCVkeURWK=
HCC1806 M{j5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\CUnVKSzVyPUK0Mlc4QTlizszN M4K3R3NCVkeURWK=
HuO-3N1 NHHub5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3STWtKSzVyPUK1MlgyQDVizszN NV22N2JGW0GQR2LFVi=>
HOS MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XvXWlEPTB;MkWuPVI6OiEQvF2= NInoPGpUSU6JUlXS
KYSE-510 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\lW2JKSzVyPUK2MlE3OTJizszN NF7DTXFUSU6JUlXS
COLO-741 NFrtXHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7mTXpoUUN3ME2yOk4{OzJ7IN88US=> NIG4PWxUSU6JUlXS
H-EMC-SS NEPjZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz4TWM2OD1{Nj65NlQ2KM7:TR?= NV3WS2tJW0GQR2LFVi=>
HCC1937 NXjrV3VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Ltc2lEPTB;MkeuNlI{QCEQvF2= M174XXNCVkeURWK=
NCI-H2126 M2\0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O4V2lEPTB;MkeuN|k4PSEQvF2= M37YXHNCVkeURWK=
NCI-H1703 MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJ6LkC0NVMh|ryP M3i2OnNCVkeURWK=
U-2-OS MnHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfDTWM2OD1{OD61OVE2KM7:TR?= NF:4TnhUSU6JUlXS
DBTRG-05MG NV65ZZJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe3R4hKSzVyPUK4MlU3PTFizszN M1P1NXNCVkeURWK=
MHH-ES-1 NGr5fIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vwdGlEPTB;M{GuPVQyKM7:TR?= MnO1V2FPT1KHUh?=
HCC1419 M4H2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTN{LkGxNVkh|ryP M{jEbnNCVkeURWK=
HOP-62 M{TaOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfTOWNqUUN3ME2zNk4zPzBzIN88US=> MojFV2FPT1KHUh?=
AM-38 NIG4TYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnqyTWM2OD1|Mj65PVMyKM7:TR?= MkjhV2FPT1KHUh?=
NCI-H2009 NF;x[3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;wVmlEPTB;M{OuOFAxPyEQvF2= NFviT3NUSU6JUlXS
EM-2 NEjGTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW3TWM2OD1|Mz61OVEyKM7:TR?= M4jVeXNCVkeURWK=
SW1116 Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfuNGFKSzVyPUO0MlQ5OzhizszN NU\PVXV4W0GQR2LFVi=>
SK-N-AS NH3wT|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrWTWM2OD1|NT6wO|E1KM7:TR?= MX;TRW5IWkWU
ChaGo-K-1 NVnNT5JxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTN3Lk[wN|Ih|ryP MU\TRW5IWkWU
RT-112 NG[zd4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPwTWM2OD1|NT65PFc6KM7:TR?= M1jOPXNCVkeURWK=
HTC-C3 M17Rb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN4LkKzOVUh|ryP M2nP[XNCVkeURWK=
SK-NEP-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTmVmdKSzVyPUO2MlYyODZizszN M1npT3NCVkeURWK=
LB831-BLC NHvPU2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDuTWM2OD1|Nz62OVQyKM7:TR?= NULLbpZXW0GQR2LFVi=>
CTB-1 NYnUWmVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHFN25RUUN3ME2zPE41PTF{IN88US=> M4\mXnNCVkeURWK=
MOLT-4 NV;xd2hWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLCRmlbUUN3ME2zPE45OzlzIN88US=> M1LxXHNCVkeURWK=
SW756 MkjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH1bXJKSzVyPUSwMlk{QDVizszN NWD0bpMxW0GQR2LFVi=>
CAL-72 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDWSHdsUUN3ME20Nk4xOyEQvF2= NYXUdXZCW0GQR2LFVi=>
KNS-62 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmKyTWM2OD12Mj62Nlk3KM7:TR?= MYLTRW5IWkWU
KARPAS-299 NUjh[opvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTR|LkOyN|Mh|ryP MonmV2FPT1KHUh?=
HEL MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTR3LkS2OFYh|ryP MmrHV2FPT1KHUh?=
KP-4 M2Lzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPmOYkxUUN3ME20Ok44OzZzIN88US=> MUDTRW5IWkWU
NEC8 NULsW3RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\uV2hQUUN3ME20O{4yPjZzIN88US=> MnLkV2FPT1KHUh?=
G-402 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTR6LkewNVIh|ryP MXTTRW5IWkWU

... Click to View More Cell Line Experimental Data

体内研究 BIRB 796按30 mg/kg剂量作用于LPS刺激的鼠,抑制TNF-α达84%。作用于患胶原诱导的关节炎鼠显示高效性。[1] BIRB 796口服处理给鼠,具有好的药物动力学特征。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:

[2]

+ 展开
  • Animal Models: 患胶原诱导的关节炎雌性Balb/c鼠
  • Formulation: 70% PEG400(静脉注射)或100% PEG400(口服)
  • Dosages: 1 mg/kg(静脉注射)或10 mg/kg(口服)
  • Administration: 静脉注射或口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (189.51 mM)
Ethanol 100 mg/mL (189.51 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 527.66
化学式

C31H37N5O3

CAS号 285983-48-4
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02214888 Terminated Arthritis, Rheumatoid Boehringer Ingelheim May 2003 Phase 2
NCT02211885 Completed Healthy Boehringer Ingelheim October 2002 Phase 1
NCT02209753 Completed Psoriasis Boehringer Ingelheim June 2001 Phase 2
NCT02209805 Completed Healthy Boehringer Ingelheim January 2001 Phase 1

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操作手册

如果有其他问题,请给我们留言。

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p38 MAPK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID