| Identification | Back Directory | [Name]
4H-1-Benzopyran-4-one, 8-[(2R)-1-(3,5-difluorophenyl)-2-pyrrolidinyl]-2-(4-morpholinyl)-6-(4-morpholinylcarbonyl)- | [CAS]
1403458-28-5 | [Synonyms]
4H-1-Benzopyran-4-one, 8-[(2R)-1-(3,5-difluorophenyl)-2-pyrrolidinyl]-2-(4-morpholinyl)-6-(4-morpholinylcarbonyl)- | [Molecular Formula]
C28H29F2N3O5 | [MOL File]
1403458-28-5.mol | [Molecular Weight]
525.54 |
| Hazard Information | Back Directory | [Uses]
PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively)[1]. | [in vivo]
PI3K-IN-2 shows profound pharmacodynamic modulation of AKT phosphorylation in PTEN-deficient PC3 prostate tumour bearing mice after oral administration and gave significant inhibition of tumour growth in the same xenograft model[1]. | [IC 50]
PI3Kα: 13 nM (IC50); PI3Kβ: 7.1 nM (IC50); PI3Kδ: 190 nM (IC50); PI3Kγ: 8.6 nM (IC50) | [References]
[1] Barlaam B, et al. Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954. DOI:10.1016/j.bmcl.2017.03.027 |
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