计算溶液所需的质量、体积或浓度。
概述
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC 50 of 2.6 nM for BRD4 . BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities ( K d values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity
In Vitro
BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest. BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels. BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6. BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC 50 >20 μM). BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ∼1500-fold selectivity for BRD4(1) over EP300 (IC 50 =3857 nM). BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC 50 values of 2.4, 4.8, 17.6 and 15.1 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: MV-4-11 cells Concentration: 31.25, 62.5, 125 nM Incubation Time: 24 hours Result: Led to more pronounced G1-phase cell cycle arrest. Western Blot AnalysisCell Line: MV-4-11 cells Concentration: 31.25, 62.5, 125, 250, 500 nM Incubation Time: 6 or 24 hours Result: Induced dose-dependent inhibition on c-Myc expression and upregulation of p21 levels. RT-PCRCell Line: MV-4-11 cells Concentration: 31.25, 62.5, 125 nM Incubation Time: 6 hours Result: Robustly reduced the expressions of c-Myc, BCL-2, and CDK6.
In Vivo
BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg . BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T 1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min•kg, and a V ss of 1464 and 782 mL/kg for rats and mouse, respectively . BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T 1/2 of 3.6 hours, a C max of 159 ng/mL and an AUC of 884 ng•h/mL for rats . BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T 1/2 of 1.3 hours, a C max of 399 ng/mL and an AUC of 1710 ng•h/mL for mouse . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: An MV4-11 mouse xenograft model Dosage: 6.25, 12.5 mg/kg Administration: PO; daily ; for 28 days Result: Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg. Animal Model: Male SD rats Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a T 1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a V ss of 1464 mL/kg.
Form:Solid
IC50& Target:BRD4 2.6 nM (IC 50 ) BRD2(2) 1.3 nM (Kd) BRD3(2) 1.0 nM (Kd) BRD4(1) 3.0 nM (Kd) BRD4(2) 1.6 nM (Kd) BRDT(2) 2.1 nM (Kd)
规格
别名
BET 溴结构域抑制剂 1
规格或纯度
≥99%
英文名称
BET bromodomain inhibitor 1
生化机理
BET 溴基团抑制剂 1 是一种口服活性、选择性溴基团和末端外（BET）溴基团抑制剂，对 BRD4 的 IC 50 为 2.6 nM。BET 溴基团抑制剂 1 与 BRD2(2)、BRD3(2)、BRD4(1)、BRD4(2) 和 BRDT(2) 具有高亲和力。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
459.47
高级数据
化学和物理性质
溶解性
DMSO : 62.5 mg/mL (136.03 mM; ultrasonic and warming and heat to 60°C)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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