Mivebresib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mivebresib (ABBV-075) 是一种有效的口服 BET bromodomain 抑制剂，对 BRD2、BRD3、BRD4 和 BRDT 的 Ki 值分别为 1.0、12.2、1.5 和 2.2 nM。

Mivebresib (ABBV-075) is a potent and orally available BET bromodomain inhibitor with Ki of 1.0, 12.2, 1.5, and 2.2 nM for BRD2, BRD3, BRD4 and BRDT, respectively; displays 54-fold selectivity over EP300, has potential weak activity against SMARCA4 (70% inhibition at 1 uM), Kd >1 uM for 18 other bromodomains; exhibits inhibition of c-Myc expression and displacing BRD4 from the Myc promoter; dose-dependently inhibits IL-6 concentration in a murine model of LPS-induced endotoxic shock, shows vivo antitumor efficacy in a Kasumi-1 AML mouse xenograft model.Breast Cancer Phase 1 Clinical(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.

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.

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ABBV-075 | ABBV075

Chromatin/Epigenetic

Bromodomain

BET

Cancer

Breast Cancer

1445993-26-9

459.4658

C22H19F2N3O4S

>98% (HPLC)

DMSO: ≥ 37 mg/mL

CCS(=O)(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)=O

Ethanesulfonamide, N-[4-(2,4-difluorophenoxy)-3-(6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years