BI-9564
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
作用于BRD9和BRD7 bromodomains,IC50分别为75 nM和3.4 μM。
BI-9564是一种BRD9/7特异性抑制剂。
BRD7和BRD9是bromodomain家族蛋白的两个重要成员。 BRD7和BRD9都参与染色质重塑。
体外:通过基于片段的筛选和结构导向设计,BI-9564被鉴定为BRD9/7特异性抑制剂。研究发现,BI-9564结合BRD9的亲和力高于对BRD7的亲和力,并且对BET家族蛋白呈阴性。此外,已证实BI-9564对CECR2具有体外而非细胞中的脱靶选择性[1]。
体内:在动物研究中,每天两次口服剂量给药BomTac:NMRIFoxn1nu小鼠,并测量血浆中BI-9564的浓度。获得BI-9564的剂量依赖性AUC,与EOL-1细胞EC50水平相比,暴露水平更高。此外,当在第5天开始用180 mg / kg的BI-9564进行口服治疗并且在第18天和19天中断每天给药时,与对照组相比,在第18天发现肿瘤生长的显著降低,导致中值肿瘤生长抑制值为52%[1]。
临床试验:到目前为止,BI-9564仍处于临床前研究阶段。
参考文献:
[1] Martin LJ et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem.2016 May 26;59(10):4462-75.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 353.41 |
Cas No. | 1883429-22-8 |
Formula | C20H23N3O3 |
Solubility | ≥8.82 mg/mL in DMSO with ultrasonic,≥8.32 mg/mL in EtOH with ultrasonic,insoluble in H2O |
Chemical Name | 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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