Crystallization (Comment) | Organism |
---|---|
structure activity relationship study of inhibitor 2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole, i.e. ZSTK474, with catalytic subunit gamma isoform, PDB entry 2CHX | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole | lead compound for structure-activity study | Homo sapiens | |
6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole | inhibitory against all three class Ia PI 3-kinase enzymes, i.e. p110alpha, p110beta, and p110delta, and also displays significant potency against two mutant forms of the p110alpha isoform, H1047R and E545K. In an in vivo U87MG human glioblastoma tumor xenograftmodel in Rag1-/- mice, and at a dose of 50mg/kg given by intraperitoneal injection it dramatically reduces cancer growth by 81% compared to untreated controls | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P48736 | catalytic subunit gamma isoform | - |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000022 | - |
isoform p110alpha, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole | |
0.00000038 | - |
isoform p110delta, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole | |
0.0000014 | - |
isoform p110beta, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole |