BET bromodomain inhibitor 1 T39998
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
2 mg | 2411226-02-1 | ¥2,120.00 | 询底价 |
Product Introduction
Bioactivity
英文名: BET bromodomain inhibitor 1
描述: BET bromodomain inhibitor 1 is an orally active, selective inhibitor of bromodomain and extra-terminal (BET) proteins. It specifically inhibits BRD4 with an IC50 of 2.6 nM. Additionally, BET bromodomain inhibitor 1 demonstrates high affinities towards BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, and 2.1 nM, respectively. This compound exhibits anti-cancer activity.
体外活性: BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest[1]. 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[1]. BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6[1]. BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC 50 >20 μM)[1]. 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)[1]. 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[1]. Cell Cycle Analysis[1]Cell 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 Analysis[1]Cell 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-PCR[1]Cell 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.
体内活性: 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[1]. 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[1]. 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[1]. 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[1]. Animal Model: An MV4-11 mouse xenograft model[1]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[1]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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: BET bromodomain inhibitor 1
BET bromodomain inhibitor 1 T39998信息由TargetMol中国为您提供,如您想了解更多关于BET bromodomain inhibitor 1 T39998报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途