285983-48-4
Chemical Structure
Doramapimod
Synonym(s): BIRB 796
- CAS No.: 285983-48-4
- Formula:C31H37N5O3
- Molecular Weight:527.66
IUPAC Name: 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea
InChIKey: MVCOAUNKQVWQHZ-UHFFFAOYSA-N
SMILES: O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3
Biological Activity: Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM[1][2].
| Cat. No. | 상품명 | Purity | 제품 설명 | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Doramapimod | 99.89% | Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Doramapimod (Standard) | ≥98% | Doramapimod (Standard) is the analytical standard of Doramapimod. This product is intended for research and analytical applications. Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Doramapimod (GMP) | Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
-
Similarity Score 0.99
HY-10320ADoramapimod hydrochloride -
Similarity Score 0.79
HY-18874p38-α MAPK-IN-1 -
Similarity Score 0.70
HY-120595JNJ-49095397 -
Similarity Score 0.60
HY-18312PF-4618433 -
Similarity Score 0.59
HY-401485Pyk2-IN-2 -
Similarity Score 0.58
HY-18882p38α-IN-11 -
Similarity Score 0.58
HY-14716CCT239065 -
Similarity Score 0.57
HY-120823PF-05381941 -
Similarity Score 0.57
HY-16782Pexmetinib -
Explore the MedChemAI to find more analogs
References
- [1]. Dietrich J, et al. The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors. Bioorg Med Chem. 2010 Aug 1;18(15):5738-48 [Content Brief]
- [2]. Cicenas J, et al. JNK, p38, ERK, and SGK1 Inhibitors in Cancer. Cancers (Basel). 2017 Dec 21;10(1). pii: E1. [Content Brief]
