Axon 2699
CAS [1693731-40-6]
MF C32H32N4O5MW 552.62
Highly potent, orally bioavailable inhibitor of the HSF1 stress pathway. CCT251236 displayed the desired balance of in vitro properties, while maintaining excellent cellular activity for inhibition of HSF1-mediated HSP72 induction (IC50 value of 19 nM). Moreover, CCT251236 displayed efficacy in a human ovarian carcinoma xenograft model. Promising chemical probe to investigate the role of HSF1 pathway inhibition and pirin binding in vitro and in vivo.
KEYWORDS: CCT251236 | supplier | HSF1 inhibitor | CCT 251236 | CCT-251236 | CAS [1693731-40-6] | DNA-RNA | HSF1 | Inhibitor | Transcription Factors | HSP72 | Pirin
MD Cheeseman et al. Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen. J Med Chem. 2017 Jan 12;60(1):180-201. |
N-(5-(2,3-Dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)-2-(2-(pyrrolidin-1-yl)ethoxy)quinoline-6-carboxamide
[1693731-40-6]
Axon Medchem的业务之一,是独有的Axon Ligands配体库,在世界范围内,被认为是药物研发的标准。这其中,针对850余种生物靶标(包括细胞信号、基因转录、凋亡、细胞周期调控、CNS等),Axon Medchem拥有多达2000余种小分子抑制剂或调节剂。除了配体库,Axon Medchem还是欧洲著名的CRO公司,主要针对生物活性分子和药物类似分子展开合成及协议开发工作,在过去的10年中,Axon Medchem已经发现了多种潜在药物分子,并在生物医药界享有一定的声誉。