PROTAC BRD3/BRD4-L degrader-2

CAS: F: C43H44ClN7O3 W: 742.31

PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3and BRD4-L with Ki values of

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Bioactivity	PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki 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].
Target	Ki: 16.91 nM (BRD3 BD1); 2.8 nM (BRD3 BD2) .IC50: 7.46 nM (MV4-11 cells); 85.4 nM (MM.1 S cells) .
Invitro	PROTAC BRD3/BRD4-L degrader-2 (Compound 28) 对 BRD3 BD1 和 BRD3 BD2 具有结合亲和力，Ki 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] 。 Western Blot Analysis[1] Cell Line:
In Vivo	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]。 Animal Model:
Name	PROTAC BRD3/BRD4-L degrader-2
Formula	C43H44ClN7O3
Molar Mass	742.31
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.