Doramapimod (BIRB 796)

For research use only. Not for use in humans.

目录号:S1574 中文名称:达马莫德

Doramapimod (BIRB 796) Chemical Structure

CAS No. 285983-48-4

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  
10mM (1mL in DMSO) RMB 2403.35 现货
RMB 1221.86 现货
RMB 2215.96 现货
RMB 3866.11 现货
RMB 12039.3 现货
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客户使用Selleck生产的Doramapimod (BIRB 796)发表文献74篇:

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
JNK2 [1]
()
c-RAF [1]
()
Fyn [1]
()
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
HOP-92 NY\yT4dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVuyRYw3UUN3ME2yOE4{QDN6IN88US=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
NCI-H2228 M4rFdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLCXFZKSzVyPUKzMlY3PjhizszN M1O1WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
CAPAN-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkexTWM2OD1{Mj6xPFg1KM7:TR?= M{nIelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
SK-MEL-1 M4Lze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPITWM2OD1{MD6zOlg{KM7:TR?= NHnQUWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK|5USU6JRWK8M4E,
DB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF6Lke5NlMh|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
AN3-CA M{D1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TkS2lEPTB;MUiuNUDPxE1? NWPVRlc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
EW-13 NFjiRmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTF5Lkm1NVYh|ryP NYXBNmJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
LC-2-ad MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTF5LkSzOlYh|ryP NYPsZpoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
ES8 MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF5LkG2O{DPxE1? MoLzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
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HMV-II M17mS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF2LkKzNFkh|ryP MmHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
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MS-1 M2facmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFyLkiyN|Uh|ryP M{HENFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
BFTC-905 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWzTWM2OD1zMD6xNlM{KM7:TR?= NGqxeGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK|5USU6JRWK8M4E,
NCI-SNU-1 NU\Vd40xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvnUVFKSzVyPUmuNFY4OzlizszN NVz3VmZ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
MPP-89 NFewbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH36Tm1KSzVyPUiuOFYzPTFizszN NVPqepB4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
T-24 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q1UmlEPTB;OD60NFY4OyEQvF2= M1W1XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
KP-N-YN M{HoeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfBTWM2OD16LkKwNVkh|ryP NH7peGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK|5USU6JRWK8M4E,
IST-MES1 NFfmXmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XQeWlEPTB;Nz65OVY{PyEQvF2= NVTJ[4FGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
NCI-H358 MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz1[GVKSzVyPUeuOVM5KM7:TR?= NX\tXIpYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
GOTO M{LMdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTZwM{mxOlEh|ryP NIi2dWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK|5USU6JRWK8M4E,
DU-145 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnmW|FKSzVyPUOuPVM5OTFizszN M4H4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
EoL-1-cell M2DnZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTlOVFEUUN3ME2wMlM1PzZ|IN88US=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
KYSE-270 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[1RodKSzVyPUK0MlU2PzNizszN M3XxOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
HCC1806 MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvBT|RHUUN3ME2yOE44Pzl7IN88US=> MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
HuO-3N1 NUfzO2ZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfCTWM2OD1{NT64NVg2KM7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
HOS NEjKSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJ3LkmyPVIh|ryP NYTE[YVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
KYSE-510 MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ4LkG2NVIh|ryP M4PkVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
COLO-741 NFr0VlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDqSndKSzVyPUK2MlM{OjlizszN NX\nTFBpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB|Nk[3M{c,W0GQR1XSQE9iRg>?
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MHH-ES-1 NFXTPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTNzLkm0NUDPxE1? MkjDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
HCC1419 NEDjcJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDtVG9KSzVyPUOyMlEyOTlizszN M2fNV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
HOP-62 NYrD[ZE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN{LkK3NFEh|ryP MoHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38 ; 

PubMed: 23349819     


The inhibitory effect of phosphorylated p38 in KB, KBV200 (B) and in MCF-7, MCF-7/ADR (C) treated with BIRB796 at various concentrations after 24 h. 

mTOR / p-S6K / S6K / p-MK2 / MK2 / p-Hsp27 / Hsp27 ; 

PubMed: 26844273     


CRC cells were treated with 4 μM LY2228820, 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.

p-p38 / γ-H2AX ; 

PubMed: 27082306     


The expression of p-P38 was tested via protein gel blot after the cells were treated with BIRB796.

23349819 26844273 27082306
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]

- 合并
  • Animal Models: 患胶原诱导的关节炎雌性Balb/c鼠
  • 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(数据来自Selleck实验检测而非文献):
5% DMSO+40%PEG300+5%Tween80 +50%H2O
5mg/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
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID