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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-ABBV-744
ABBV-744

Chemical Structure : ABBV-744

CAS No.: 2138861-99-9

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ABBV-744 (ABBV744)

货号: PC-35172Not For Human Use, Lab Use Only.

ABBV-744 (ABBV744) is a highly potent and selective inhibitor of the BD2 domain of BET family proteins with IC50 of 4-18 nM for BD2 of BRD2, BRD3, BRD4 and BRDT.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 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

ABBV-744 (ABBV744) is a highly potent and selective inhibitor of the BD2 domain of BET family proteins with IC50 of 4-18 nM for BD2 of BRD2, BRD3, BRD4 and BRDT.
ABBV-744 displayed >250-fold differential binding preference for BDII over BDI and excellent drug-like properties.
ABBV-744 inhibited SARS-CoV-2 replication in Syrian hamsters, potently blocked endogenous ACE2 expression and SARS-CoV-2 infection of human cells, highlighting the potential of BRD2 as a novel therapeutic target for COVID-19.
ABBV-744 displayed significant antiproliferative activities largely although not exclusively in cancer cell lines derived from acute myeloid leukemia and androgen receptor positive prostate cancer.
ABBV-744 demonstrated antitumor efficacy in acute myeloid leukemia xenograft models with an improved therapeutic index compared with the pan-BET inhibitor ABBV-075. enhanced the antitumor efficacy of BCL-2 inhibitor, venetoclax.

物理化学性质&存储条件

分子量 491.563
分子式 C28H30FN3O4
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

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-

参考文献

1. Faivre EJ, et al. Nature. 2020 Feb;578(7794):306-310.
2. Sheppard GS, et al. J Med Chem. 2020 May 28;63(10):5585-5623.
3. Fakhar Z, et al. Sci Rep. 2021 Jan 8;11(1):234.

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