化合物Birabresib T6032

Product Introduction
Bioactivity


英文名: Birabresib

描述: Birabresib (MK-8628) 是一种 BRD2/3/4抑制剂，IC50值为 92 到 112 nM 之间，具有潜在的抗肿瘤活性。

细胞实验: Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay.(Only for Reference)

激酶实验: TR-FRET Assay [1]: To assess binding of OTX015 to BRD2, BRD3, and BRD4, BRD-expressing CHO cell lysate (from CHO cells transfected with expression plasmids for Flag-tagged BRD2, BRD3, or BRD4 or vector alone), europium-conjugated anti-Flag antibody, XL-665-conjugated streptavidin, and biotinylated OTX015 are incubated at room temperature for 0.2 to 2 h. Fluorescence is measured by TR-FRET using an EnVision 2103 Multilabel Reader and EC50 for binding is calculated by nonlinear regression using PRISM version 5.02.

体外活性: OTX015 inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. [1] OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. [2]

体内活性: OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 9.8 mg/mL (20 mM)
DMSO : 49.2 mg/mL (100 mM)


关键字: Epigenetic Reader Domain | OTX 015 | Inhibitor | Birabresib | OTX015 | MK8628 | MK 8628 | MK 8628/Birabresib | inhibit

相关产品: BMS-986158 | BRD4 Inhibitor-20 | SMD-3040 | Histone Acetyltransferase Inhibitor II | Eleven-Nineteen-Leukemia Protein IN-3 | 3',6-Disinapoylsucrose | GNE-207 | 2-methyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-4-one | LP99 | UNC926

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Target-Focused Phenotypic Screening Library | Preclinical Compound Library | Reprogramming Compound Library