BI-7273
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,IC50分别为19和117 nM。
BI-7273是一种BRD9 bromodomain抑制剂。
BRD9是SWI / SNF亚基,在白血病生长中具有关键作用,并且已经显示BRD9 bromodomain(BD)对于急性骨髓性白血病细胞的增殖具有关键作用。
体外:先前的研究证明,BI-7273模拟BRD9的遗传扰动。 BI-7273还可以靶向BRD7 BD,一种在SWI / SNF重塑复合物亚型中发现的与BRD9共享高序列同源性的BD蛋白。此外,BI-7273能够与BRD9中Asn100的羰基形成额外的正相互作用。此外,在生物化学Alpha测定中,即使浓度达到100μM,BI-7273对BET家族BD仍未显示出可测量的活性[1]。
体内:为了探究BI-7273作为体内化学探针的潜力,以20和180 mg / kg两个剂量口服给药雌性BomTac:NMRIFoxn1nu小鼠,并测量血浆中BI-7273随时间的浓度。结果显示,观察到BI-7273剂量依赖性但非线性的AUC,与使用EOL-1细胞的增殖测定中测定的BI-7273的EC50水平相比,获得更高水平的暴露[1]。
临床试验:到目前为止,BI-7273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 solid |
Storage | Store at -20°C |
M.Wt | 353.41 |
Cas No. | 1883429-21-7 |
Formula | C20H23N3O3 |
Solubility | ≥35.3 mg/mL in DMSO with gentle warming; ≥1.99 mg/mL in EtOH with ultrasonic; ≥8.74 mg/mL in H2O |
Chemical Name | 4-(4-((dimethylamino)methyl)-3,5-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(OC)=C2)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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