aladdin 阿拉丁 A414297 阿罗布塞(GS-5829) 1637771-14-2 98%

中文名：阿罗布塞(GS-5829)

英文名：Alobresib

纯度：≥98%

货号：A414297

Cas号：1637771-14-2

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK , AKT , ERK1/2 , and MYC . Alobresib (GS-5829) also inhibits NF-κB signaling.

Targets

BET ; BLK ; Akt ; ERK1/2 ; MYC 33297,

In vitro

In-vitro experiments demonstrates high sensitivity of USC cell-lines to the exposure to GS-5829 causing a dose-dependent decrease in the phosphorylated levels of c-Myc and a dose-dependent increase in caspase activation (apoptosis). GS-5829 inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. IκBα modulation indicates that GS-5829 also inhibits NF-κB signaling. GS-5829-induced apoptosis results from an imbalance between positive (BIM) and negative regulators (BCL-XL) of the intrinsic apoptosis pathway.

In vivo

GS-5829 has impressive activity against USC primary tumors as well as USC xenografts. Assessment of c-Myc expression in tumors exposed to the GS-5829 demonstrates down-regulation of both total and phospho c-Myc proteins. GS-5829 demonstrates excellent bioavailability after oral administration and is significantly more effective than JQ1 at the doses used in comparative experiments in vivo against USC xenografts. Clinical studies with GS-5829 in USC patients harboring disease resistant to standard salvage chemotherapy are warranted.

Cell Research(from reference)

Cell lines：PBMC, MEC-1 

Concentrations：100 nM, 200 nM, 400 nM, 800 nM 

Incubation Time：72 h, 24 h 

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