ABBV-744

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

ABBV-744 (ABBV744) 是一种有效的 BDII 选择性 BET 溴结构域抑制剂。

ABBV-744 (ABBV744) is a potent, BDII-selective BET bromodomain inhibitor, ABBV-744 is a potent, selective inhibitor of the AR transcription activity; induces tumor growth inhibition in LNCaP and MDA-Pca-2b xenograft models.Prostate Cancer Phase 1 Clinical.

Western Blot Analysis Cell Line:LNCaP cells Concentration:90 nM Incubation Time:0~24 hours Result:Downregulated the expression of KLK2 and MYC genes.Cell Cycle Analysis Cell Line:LNCaP cells Concentration:90 nM Incubation Time:0~72 hours Result:Induced cell cycle arrest in G1 followed by senescence.

Animal Model:Mice Dosage:4.7 mg/kg (Pharmacokinetic Analysis)Administration:Oral gavage; 28 days Result:Caused a delay in tumor growth and displayed equivalent or better antitumor activity compared with ABBV-075.Animal Model:Sprague-Dawley rats Dosage:30 mg/kg (Pharmacokinetic Analysis) Administration:14 days Result:Produced significant antitumor activity.

ABBV744

Chromatin/Epigenetic

Bromodomain

BET bromodomain

Cancer

Prostate Cancer

2138861-99-9

491.563

C28H30FN3O4

>98% (HPLC)

DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(C(N1)=CC(C(C2=CC(C(C)(O)C)=CC=C2OC3=C(C)C=C(F)C=C3C)=CN4C)=C1C4=O)NCC

1H-Pyrrolo[2,3-c]pyridine-2-carboxamide, N-ethyl-4-[2-(4-fluoro-2,6-dimethylphenoxy)-5-(1-hydroxy-1-methylethyl)phenyl]-6,7-dihydro-6-methyl-7-oxo-

(-20℃)

With Ice Pack

≥ 2 years