PROTAC BRD3/BRD4-L degrader-2 

PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with K_i values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer^[1].

Ki: 16.91 nM (BRD3 BD1); 2.8 nM (BRD3 BD2) ^[1].
IC50: 7.46 nM (MV4-11 cells); 85.4 nM (MM.1 S cells) ^[1].

PROTAC BRD3/BRD4-L degrader-2 (Compound 28) 对 BRD3 BD1 和 BRD3 BD2 具有结合亲和力，K_i 值分别为 16.91 和 2.8 nM^[1]。
PROTAC BRD3/BRD4-L degrader-2 在 MV4-11 和 MM.1 S 细胞系中具有细胞活性，IC₅₀ 值分别为 7.46 和 85.4 nM^[1].
PROTAC BRD3/BRD4-L degrader-2 (30 nM; 1, 3, 6, 8, 24 h) 以时间依赖性方式选择性降解 BRD3 和 BRD4-L ^[1].
PROTAC BRD3/BRD4-L degrader-2 (1, 3, 10, 30, 100, 300 nM; 24 h) 在 MM.1 S 细胞中具有抗肿瘤活性，并以剂量依赖性方式诱导 G1 期细胞周期停滞^[1] 。

PROTAC BRD3/BRD4-L degrader-2(compound 28) (oral, i.v.; 3 mg/kg) 口服生物利用度差，静脉内给药时表现出良好的全身暴露^[1]。
PROTAC BRD3/BRD4-L degrader-2 (i.v.; 3 mg/kg) 在 MM.1 S 小鼠异种移植模型中具有抗肿瘤功效^[1]。
PROTAC BRD3/BRD4-L degrader-2 (i.v.; 1, 5 mg/kg; signal dose) 促进体内 BRD3 和 BRD4-L 的选择性降解，并表现出强大的抗肿瘤活性^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

742.31

C₄₃H₄₄ClN₇O₃

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yan Z, et al. Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines. Eur J Med Chem. 2023;254:115381.  [Content Brief]