AZD 5153
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.
Target: BRD4
IC50: 5 nM
AZD5153 is a potent, selective, and orally available inhibitor of the bromodomain and extraterminal (BET) protein BRD4, with the IC50 value of 5 nM. AZD5153 could simultaneously ligate two bromodomains in BRD4, and exert antitumor activity in multiple xenograft tumor models [1].
In Vitro: A quantitative immuno-fluorescent assay in U2OS cells revealed that AZD5153 could significantly disrupt BRD4 foci, with the IC50 value of 1.7 nM. Besides, AZD5153 could inhibit the proliferation of AML, MM, and DLBCL cell lines, with the majority of cell lines having a GI50 value < 25 nM. Furthermore, 200 nM AZD5153 could significantly decrease the level of mTOR pathway associated proteins in sensitive hematologic cancer cell lines (MOLP8, MV-4-11, OCILY19) [1].
In Vivo: In AML, MM, and DLBCL xenografted tumor mouse models, oral administration of AZD5153 at the dose of 1, 2.5, and 5mg/kg could inhibit tumor growth in a dose dependent manner [1].
Clinical trial: no data available.
Reference:
[1] Rhyasen G W, Hattersley M M, Yao Y, et al. AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies[J]. Molecular Cancer Therapeutics, 2016, 15(11): 2563-2574.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 479.6 |
| Cas No. | 1869912-39-9 |
| Formula | C25H33N7O3 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | (3R)-4-[2-[4-[1-(3-methoxy-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-2-piperazinone |
| SDF | Download SDF |
| Canonical SMILES | COC1=NN=C2N1N=C(N3CCC(C4=CC=C(OCCN5[C@H](C)C(N(C)CC5)=O)C=C4)CC3)C=C2 |
| 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。 |
化学结构
