Information BI-847325 is an orally bioavailable, and selective dualMEK/Aurora kinaseinhibitor withIC50of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1. Targets Aurora B (Xenopus laevis) ; MEK2 ; Aurora C (Human) ; Aurora A (Human) ; MEK1 3 nM; 4 nM; 15 nM; 25 nM; 25 nM In vitro BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression. In vivo In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights. Cell Research(from reference) Cell lines：M229, M229R, A375, A375R, WM793, WM793R, 1205Lu, 1205LuR, M249, M249R, WM164, WM164R, WM39 and RPMI17951 cells Concentrations：30 μM Incubation Time：72 h
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BI-847325
CAS number：1207293-36-4 molecular formula：C29H28N4O2
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| Chinese alias | - | ||
| English alias | NSC799360 | NSC-799360 | (Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide | 2-Propynamide, 3-((3Z)-3-(((4-((dimethylamino)methyl)phenyl)amino)phenylmethylene)-2,3-dihydro-2-oxo-1H-indol-6-yl)-N-ethy | ||
| CAS number | 1207293-36-4 | molecular formula | C29H28N4O2 |
| molecular weight | 464.56 g/mol | Exact mass | 10mM in DMSO |
| PSA | 80.700 Ų | logp | 4.041 |
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