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Alobresib

Chemical Structure : Alobresib

CAS No.: 1637771-14-2

Alobresib (GS5829, GS-5829)

货号: PC-38148Not For Human Use, Lab Use Only.

GS-5829 (GS5829, Alobresib) is a novel potent, selective BET inhibitor.

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10 mg ¥1980 In stock
50 mg ¥4980 In stock
100 mg ¥7980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GS-5829 (GS5829, Alobresib) is a novel potent, selective BET inhibitor.
GS-5829 dose-dependently induced apoptosis of CLL cells, 400 nM GS-5829 reduced the percentage of viable cells from 94.8% to 64.4%.
In XTT viability/proliferation assay, GS-5829 demonstrated more potency against MEC-1 CLL cells compared to JQ1 with IC50 of 46.4 nM.
GS-5829 inhibited CLL cell proliferation and induced leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC.
GS-5829 also inhibited NF-κB signaling. GS-5829 significantly reduced c-Myc protein expression in ARK2 xenograft tumor samples, impaired USC-ARK2 xenograft tumor growth in vivo.

物理化学性质&存储条件

分子量 437.5
分子式 C26H23N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-cyclopropyl-5-(3,5-dimethyl-4-isoxazolyl)-α,α-di-2-pyridinyl-1H-benzimidazole-7-methanol

参考文献

1. Bonazzoli E, et al. Clin Cancer Res. 2018 Oct 1;24(19):4845-4853.

2. Kim E, et al. Leukemia. 2020 Jun;34(6):1588-1598.

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