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1259522-94-5

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1259522-94-5 Structure

1259522-94-5 Structure
IdentificationBack Directory
[Name]

AM-0687
[CAS]

1259522-94-5
[Synonyms]

AM-0687
4-Quinolinecarboxamide, 2-[(1S)-1-[(6-amino-5-cyano-4-pyrimidinyl)amino]ethyl]-6-fluoro-N-methyl-3-(2-pyridinyl)-
[Molecular Formula]

C23H19FN8O
[MOL File]

1259522-94-5.mol
[Molecular Weight]

442.45
Chemical PropertiesBack Directory
[Boiling point ]

721.0±60.0 °C(Predicted)
[density ]

1.43±0.1 g/cm3(Predicted)
[pka]

12.15±0.46(Predicted)
Hazard InformationBack Directory
[Uses]

AM-0687 is a selective inhibitor for PI3Kδ with an IC50 of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC50=0.8 nM) and the phosphorylation of AKT (IC50=0.7 nM), and exhibits anti-inflammatory efficacy[1].
[IC 50]

PI3Kδ: 2.9 nM (IC50); PI3Kβ: 2840 nM (IC50); PI3Kγ: 3530 nM (IC50); PI3Kα: 17600 nM (IC50)
[References]

[1] Gonzalez-Lopez de Turiso F, et al. Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430). J Med Chem. 2016 Aug 11;59(15):7252-67. DOI:10.1021/acs.jmedchem.6b00827
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