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Chemical Structure : Alobresib
CAS No.: 1637771-14-2
Catalog No.: PC-38148Not For Human Use, Lab Use Only.
GS-5829 (GS5829, Alobresib) is a novel potent, selective BET inhibitor.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 50 mg | $498 | In stock | |
| 100 mg | $798 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 437.5 | |
| Formula | C26H23N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-cyclopropyl-5-(3,5-dimethyl-4-isoxazolyl)-α,α-di-2-pyridinyl-1H-benzimidazole-7-methanol |
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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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