|1-(3-(叔丁基)-1-(对甲苯基)-1H-吡唑-5-基)-3-(4-(2-吗啉乙氧基)萘-1-基)脲|CsnPharm

CAS No.: 285983-48-4

Doramapimod/达马莫德 Catalog No. CSN10856

Synonyms: BIRB 796;达马莫德

Doramapimod is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 p38 MAPKα

Kd:0.1nM
描述The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. The well reported isoforms of p38 MAPKs include p38α, p38β and others. Doramapimod, also termed BIRB 796, is a p38 MAPK inhibitor. The IC₅₀s of doramapimod against p38α determined by kinase assay at incubation time of 0 min, 30 min and 90 min were 0.08 μM, 0.07 μM and 0.038 μM, respectively, and the data of doramapimod against p38β were 0.38 μM, 0.215 μM and 0.065 μM, respectively at the same time points^[3]. The affinity of doramapimod for p38 MAPK was 0.1 nM, and the inhibitory IC₅₀ of it against TNFα in THP-1 cell culture was 18 nM^[4]. In multiple myeloma MM1S and U266 cells, 2h treatment by doramapimod at the concentration of 25 nM was sufficient to inhibit phosphorylation of p38 MAPK^[5]. In a mouse model of LPS-stimulated TNF-α synthesis, a 65% inhibition of TNF-α synthesis was observed when doramapimod was dosed orally at 10 mg/kg. In a 5 week model of established collagen-induced arthritis using B10.RIII mice, doramapimod produced a 63% inhibition of arthritis severity when dosed orally at 30 mg/kg qd^[6].
作用机制Doramapimod is a p38 MAPK inhibitor. Doramapimod indirectly competed with the binding of ATP, but prior to binding, the kinase underwent a reorganization of the activation loop exposing a critical binding domain and yielded a structure incompatible with ATP binding^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
AM-38	-	Growth Inhibition Assay	-	IC50=32.9931 μM	SANGRER
AN3-CA	-	Growth Inhibition Assay	-	IC50=18.1 μM	SANGRER
BEN	-	Growth Inhibition Assay	-	IC50=13.1264 μM	SANGRER

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临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT02208856 Healthy Phase 1 Completed - -
NCT02211170 Healthy Phase 1 Completed - -
NCT02209831 Healthy Phase 1 Completed - -
更多

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02208856	Healthy	Phase 1	Completed	-	-
NCT02211170	Healthy	Phase 1	Completed	-	-
NCT02209831	Healthy	Phase 1	Completed	-	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8952 mL
- 9.4758 mL
- 18.9517 mL
- 5 mM
- 0.3790 mL
- 1.8952 mL
- 3.7903 mL
- 10 mM
- 0.1895 mL
- 0.9476 mL
- 1.8952 mL

技术信息

CAS号

285983-48-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H37N5O3

运输

蓝冰

分子量

527.66

别名

BIRB 796;达马莫德

溶解度

DMSO	98.0 mg/mL (185.7 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (189.5 mM)

动物实验配方

5% DMSO+40%PEG300+5%Tween80 +50%water

5 mg/mL

大规格询价

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

AM-38	-	Growth Inhibition Assay	-	IC50=32.9931 μM	SANGRER
AN3-CA	-	Growth Inhibition Assay	-	IC50=18.1 μM	SANGRER
BEN	-	Growth Inhibition Assay	-	IC50=13.1264 μM	SANGRER
BFTC-905	-	Growth Inhibition Assay	-	IC50=10.1233 μM	SANGRER
CAL-72	-	Growth Inhibition Assay	-	IC50=42.03 μM	SANGRER
CAPAN-1	-	Growth Inhibition Assay	-	IC50=22.1884 μM	SANGRER
ChaGo-K-1	-	Growth Inhibition Assay	-	IC50=35.6032 μM	SANGRER
COLO-741	-	Growth Inhibition Assay	-	IC50=26.3329 μM	SANGRER
CTB-1	-	Growth Inhibition Assay	-	IC50=38.4512 μM	SANGRER
DB	-	Growth Inhibition Assay	-	IC50=18.7923 μM	SANGRER
DBTRG-05MG	-	Growth Inhibition Assay	-	IC50=28.5651 μM	SANGRER
DU-145	-	Growth Inhibition Assay	-	IC50=3.93811 μM	SANGRER
EM-2	-	Growth Inhibition Assay	-	IC50=33.5511 μM	SANGRER
EoL-1-cell	-	Growth Inhibition Assay	-	IC50=0.34763 μM	SANGRER
ES8	-	Growth Inhibition Assay	-	IC50=17.167 μM	SANGRER
EW-13	-	Growth Inhibition Assay	-	IC50=17.9516 μM	SANGRER
G-402	-	Growth Inhibition Assay	-	IC50=48.7012 μM	SANGRER
GOTO	-	Growth Inhibition Assay	-	IC50=6.39161 μM	SANGRER
HCC1419	-	Growth Inhibition Assay	-	IC50=32.1119 μM	SANGRER
HCC1806	-	Growth Inhibition Assay	-	IC50=24.7799 μM	SANGRER
HCC1937	-	Growth Inhibition Assay	-	IC50=27.2238 μM	SANGRER
HEL	-	Growth Inhibition Assay	-	IC50=45.4646 μM	SANGRER
H-EMC-SS	-	Growth Inhibition Assay	-	IC50=26.9245 μM	SANGRER
HMV-II	-	Growth Inhibition Assay	-	IC50=14.2309 μM	SANGRER
HOP-62	-	Growth Inhibition Assay	-	IC50=32.2701 μM	SANGRER
HOP-92	-	Growth Inhibition Assay	-	IC50=24.3838 μM	SANGRER
HOS	-	Growth Inhibition Assay	-	IC50=25.9292 μM	SANGRER
HTC-C3	-	Growth Inhibition Assay	-	IC50=36.2355 μM	SANGRER
HuO-3N1	-	Growth Inhibition Assay	-	IC50=25.8185 μM	SANGRER
IST-MES1	-	Growth Inhibition Assay	-	IC50=7.95637 μM	SANGRER
KARPAS-299	-	Growth Inhibition Assay	-	IC50=43.3233 μM	SANGRER
KNS-62	-	Growth Inhibition Assay	-	IC50=42.6296 μM	SANGRER
KP-4	-	Growth Inhibition Assay	-	IC50=46.7361 μM	SANGRER
KP-N-YN	-	Growth Inhibition Assay	-	IC50=8.2019 μM	SANGRER
KYSE-270	-	Growth Inhibition Assay	-	IC50=24.5573 μM	SANGRER
KYSE-510	-	Growth Inhibition Assay	-	IC50=26.1612 μM	SANGRER
LB831-BLC	-	Growth Inhibition Assay	-	IC50=37.6541 μM	SANGRER
LC-2-ad	-	Growth Inhibition Assay	-	IC50=17.4366 μM	SANGRER
MHH-ES-1	-	Growth Inhibition Assay	-	IC50=31.941 μM	SANGRER
MOLT-4	-	Growth Inhibition Assay	-	IC50=38.8391 μM	SANGRER
MPP-89	-	Growth Inhibition Assay	-	IC50=8.46251 μM	SANGRER
MS-1	-	Growth Inhibition Assay	-	IC50=10.8235 μM	SANGRER
NBsusSR	-	Growth Inhibition Assay	-	IC50=10.8235 μM	SANGRER
NCI-H1581	-	Growth Inhibition Assay	-	IC50=17.0447 μM	SANGRER
NCI-H1703	-	Growth Inhibition Assay	-	IC50=28.0413 μM	SANGRER
NCI-H2009	-	Growth Inhibition Assay	-	IC50=33.4007 μM	SANGRER
NCI-H2126	-	Growth Inhibition Assay	-	IC50=27.3975 μM	SANGRER
NCI-H2228	-	Growth Inhibition Assay	-	IC50=23.6668 μM	SANGRER
NCI-H358	-	Growth Inhibition Assay	-	IC50=7.538 μM	SANGRER
NCI-SNU-1	-	Growth Inhibition Assay	-	IC50=9.06739 μM	SANGRER
NEC8	-	Growth Inhibition Assay	-	IC50=47.1661 μM	SANGRER
RT-112	-	Growth Inhibition Assay	-	IC50=35.9879 μM	SANGRER
SK-MEL-1	-	Growth Inhibition Assay	-	IC50=20.3683 μM	SANGRER
SK-N-AS	-	Growth Inhibition Assay	-	IC50=35.0714 μM	SANGRER
SK-NEP-1	-	Growth Inhibition Assay	-	IC50=36.6106 μM	SANGRER
SW1116	-	Growth Inhibition Assay	-	IC50=34.4838 μM	SANGRER
SW756	-	Growth Inhibition Assay	-	IC50=40.9385 μM	SANGRER
T-24	-	Growth Inhibition Assay	-	IC50=8.40673 μM	SANGRER
U-2-OS	-	Growth Inhibition Assay	-	IC50=28.5515 μM	SANGRER

Doramapimod/达马莫德 Catalog No. CSN10856

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