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首页-抗体药物偶连体和PROTACs-PROTAC-A1874
A1874

Chemical Structure : A1874

CAS No.: 2064292-12-0

A1874 (A-1874)

货号: PC-35762Not For Human Use, Lab Use Only.

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).

规格 价格 库存 数量
1 mg ¥1980 In stock
5 mg ¥4880 In stock
10 mg Get quote
25 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).
A1874 is more effective in inhibiting proliferation of many cancer cell lines with wild type p53 than was a corresponding VHL-utilizing PROTAC with similar potency and efficacy to degrade BRD4.
A1874 demonstrates synergistic antiproliferative effect via simultaneous degradation of BRD4 and stabilization of p53.

物理化学性质&存储条件

分子量 1173.597
分子式 C58H62Cl3F2N9O7S
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

(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-N-(4-((1-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2-oxo-6,9,12-trioxa-3-azatetradecan-14-yl)carbamoyl)-2-methoxyphenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamide

参考文献

1. Hines J, et al. Cancer Res. 2018 Nov 1. pii: canres.2918.2018.

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