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Submit ReviewETP 45658 is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively). Inhibits proliferation of multiple cancer cell lines in vitro and reduces Akt phosphorylation levels in vivo.
分子量 | 311.34 |
公式 | C16H17N5O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1198357-79-7 |
PubChem ID | 25229608 |
InChI Key | BJVRNXSHJLDZJR-UHFFFAOYSA-N |
Smiles | CN2C1=NC(C3=CC(O)=CC=C3)=NC(N4CCOCC4)=C1C=N2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Link et al (2009) Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J.Biol.Chem. 284 28392 PMID: 19690175
Hill et al (2014) A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes. Breast Cancer Res. 16 482 PMID: 25488803
关键词: ETP 45658, ETP 45658 supplier, ETP45658, PI3-K, kinases, inhibitors, inhibits, dna-pk, mtor, PI3Ka, PI3Kalpha, PI3Kd, PI3Kdelta, PI3Kb, PI3Kbeta, PI3Kg, PI3Kgamma, PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ, PI, 3-Kinase, mTOR, DNA-dependent, Protein, Kinase, 4702, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ETP 45658 的部分引用包括:
Maswadeh et al (2015) Coadministration of dox. and etop. loaded in camel milk phospholipids liposomes showed increased antitumor activity in a murine model. PLoS One 10 2847 PMID: 25926730
Small et al (2022) Phenotypic screening for small molecules that protect beta -cells from glucolipotoxicity. ACS Chem.Biol. 17 1131 PMID: 35439415
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