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Mivebresib

Names

[ CAS No. ]:
1445993-26-9

[ Name ]:
Mivebresib

[Synonym ]:
N-[4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide
N-[4-(2,4-Difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid
N-[4-(2,4-Difluorophénoxy)-3-(6-méthyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phényl]éthanesulfonamide
Ethanesulfonamide, N-[4-(2,4-difluorophenoxy)-3-(6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]-
Mivebresib
ABBV-075

Biological Activity

[Description]:

Mivebresib is a potent and orally available bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
Research Areas >> Cancer

[Target]

IC50: 1.5 nM (BET)[1]


[In Vitro]

Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins[1].

[References]

[1]. EJ Faivre et al. Abstract 4694: ABBV-075, a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo


[Related Small Molecules]

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
608.9±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H19F2N3O4S

[ Molecular Weight ]:
459.466

[ Flash Point ]:
322.0±34.3 °C

[ Exact Mass ]:
459.106445

[ LogP ]:
3.91

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.647

[ Storage condition ]:
-20℃

Related Compounds