Doramapimod (BIRB 796)

中文名称:达马莫德

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。

Doramapimod (BIRB 796) Chemical Structure

Doramapimod (BIRB 796) Chemical Structure

CAS: 285983-48-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) 794.43 现货
5mg 647.01 现货
50mg 3104.01 现货
200mg 7772.31 现货
1g 16134.3 现货
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Doramapimod (BIRB 796)相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
U937 Antiinflammatory assay 2 hrs Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control, IC50 = 0.015 μM. 26800309
whole blood cells Antiinflammatory assay 4 hrs Antiinflammatory activity in human whole blood cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by time-resolved fluorescence assay, IC50 = 0.6 μM. 22749282
KNS-62 Growth Inhibition Assay IC50=42.6296 μM SANGER
CAL-72 Growth Inhibition Assay IC50=42.03 μM SANGER
SW756 Growth Inhibition Assay IC50=40.9385 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=38.8391 μM SANGER
CTB-1 Growth Inhibition Assay IC50=38.4512 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=37.6541 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=36.6106 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=36.2355 μM SANGER
RT-112 Growth Inhibition Assay IC50=35.9879 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=35.6032 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=35.0714 μM SANGER
SW1116 Growth Inhibition Assay IC50=34.4838 μM SANGER
EM-2 Growth Inhibition Assay IC50=33.5511 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=33.4007 μM SANGER
AM-38 Growth Inhibition Assay IC50=32.9931 μM SANGER
HOP-62 Growth Inhibition Assay IC50=32.2701 μM SANGER
HCC1419 Growth Inhibition Assay IC50=32.1119 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=31.941 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=28.5651 μM SANGER
U-2-OS Growth Inhibition Assay IC50=28.5515 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=28.0413 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=27.3975 μM SANGER
HCC1937 Growth Inhibition Assay IC50=27.2238 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=26.9245 μM SANGER
COLO-741 Growth Inhibition Assay IC50=26.3329 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=26.1612 μM SANGER
HOS Growth Inhibition Assay IC50=25.9292 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=25.8185 μM SANGER
HCC1806 Growth Inhibition Assay IC50=24.7799 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=24.5573 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.34763 μM SANGER
DU-145 Growth Inhibition Assay IC50=3.93811 μM SANGER
GOTO Growth Inhibition Assay IC50=6.39161 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=7.538 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=7.95637 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=8.2019 μM SANGER
T-24 Growth Inhibition Assay IC50=8.40673 μM SANGER
MPP-89 Growth Inhibition Assay IC50=8.46251 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=9.06739 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=10.1233 μM SANGER
MS-1 Growth Inhibition Assay IC50=10.8235 μM SANGER
NBsusSR Growth Inhibition Assay IC50=10.8235 μM SANGER
BEN Growth Inhibition Assay IC50=13.1264 μM SANGER
HMV-II Growth Inhibition Assay IC50=14.2309 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=17.0447 μM SANGER
ES8 Growth Inhibition Assay IC50=17.167 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=17.4366 μM SANGER
EW-13 Growth Inhibition Assay IC50=17.9516 μM SANGER
AN3-CA Growth Inhibition Assay IC50=18.1 μM SANGER
DB Growth Inhibition Assay IC50=18.7923 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=20.3683 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=22.1884 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=23.6668 μM SANGER
HOP-92 Growth Inhibition Assay IC50=24.3838 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=43.3233 μM SANGER
HEL Growth Inhibition Assay IC50=45.4646 μM SANGER
KP-4 Growth Inhibition Assay IC50=46.7361 μM SANGER
NEC8 Growth Inhibition Assay IC50=47.1661 μM SANGER
G-402 Growth Inhibition Assay IC50=48.7012 μM SANGER
Sf21 Function assay Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells SPR analysis, Kd = 0.000123 μM. 28834431
THP1 Function assay Inhibition of LPS-induced TNFalpha production in human THP1 cells, IC50 = 0.013 μM. 18325768
THP1 Function assay Inhibition of LPS-induced TNFalpha production in human THP1 cells, IC50 = 0.018 μM. 19356929
THP1 Function assay Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells, EC50 = 0.018 μM. 12086485
THP Function assay Tested for inhibition of Tumor necrosis factor, alpha in THP cells, EC50 = 0.018 μM. 14561087
THP1 Function assay Inhibition of LPS-induced TNFalpha production in THP1 cells, IC50 = 0.018 μM. 17560108
THP1 Function assay Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50 = 0.018 μM. 18462940
HLF Function assay Inhibition of p38alpha phosphorylation in IL-1-alpha-stimulated HLF cells, IC50 = 0.047 μM. 18602262
HLF Function assay Inhibition of HSP27 phosphorylation in IL-1-alpha-stimulated HLF cells, IC50 = 0.058 μM. 18602262
HEK293F Function assay Inhibition of sodium arsenate activated N-terminal GST-tagged Brugia malayi MPK1 expressed in HEK293F cells using FAM-p38tide as substrate by IMAP assay, IC50 = 0.14 μM. 29541362
BL21(DE3) Function assay Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assay, IC50 = 0.25 μM. 19928858
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
点击查看更多细胞系数据

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(In Vitro)
体外研究活性

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]

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-p38 / γ-H2AX mTOR / p-S6K / S6K / p-MK2 / MK2 / p-Hsp27 / Hsp27 p-p38 / p38 27082306
体内研究(In Vivo)
体内研究活性

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]

动物实验 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02211885 Completed
Healthy
Boehringer Ingelheim
October 2002 Phase 1

化学信息&溶解度

分子量 527.66 分子式

C31H37N5O3

CAS号 285983-48-4 SDF Download Doramapimod (BIRB 796) SDF
Smiles CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (189.51 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 100 mg/mL (189.51 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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