Molecular Formula | C29H28N4O2 |
Molar Mass | 464.56 |
Solubility | DMSO: ≥36 mg/mL |
Storage Condition | -20℃ |
In vitro study | BI-847325 showed growth inhibition in BRAF mutant and vemurafenib resistant melanoma cells with an IC50 in the range of 0.3 nM-2 μm and prevented colony formation in six BRAF mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression. |
In vivo study | In mice loaded with 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) caused significant tumor regression without significant change in body weight. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.153 ml | 10.763 ml | 21.526 ml |
5 mM | 0.431 ml | 2.153 ml | 4.305 ml |
10 mM | 0.215 ml | 1.076 ml | 2.153 ml |
5 mM | 0.043 ml | 0.215 ml | 0.431 ml |
biological activity | BI-847325 is an oral selective dual MEK/Aurora kinase inhibitor with biological activity. the IC50 for Xenopus Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2 are 3 nM,25 nM,15 nM respectively, 25 nM, and 4 nM. Phase 1. |
target | TargetValue Aurora B (Xenopus laevis) 3 nM MEK2 4 nM Aurora C (Human) 15 nM Aurora A (Human) 25 nM MEK1 25 nM |
Target | Value |
Aurora B (Xenopus laevis) | 3 nM |
MEK2 | 4 nM |
Aurora C (Human) | 15 nM |
Aurora A (Human) | 25 nM |
MEK1 | 25 nM |
in vitro study | BI-847325 showed growth inhibition on BRAF mutant and vemurafenib resistant melanoma cells, with IC50 ranging from 0.3 nM-2 μM and preventing colony formation in 6 BRAF mutant melanoma cell lines. BI-847325 also induce apoptosis by reducing Mcl-1 expression. |
in vivo study | in mice loaded with 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) caused significant tumor degeneration without significant weight change. |