product name BI-847325
Description: BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 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. BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C.
References: Mol Cancer Ther. 2015 Jun;14(6):1354-64.
464.56
Formula
C29H28N4O2
CAS No.
1207293-36-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 19 mg/mL (40.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl: 30 mg/mL
Synonyms
BI 847325; BI847325.
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393556
| In Vitro |
In vitro activity: 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 Kinase Assay: BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 15 and 4 nM for human AK-C and MEK2, respectively. Cell Assay: Cells (M229, M229R, A375, A375R, WM793, WM793R, 1205Lu, 1205LuR, M249, M249R, WM164, WM164R, WM39 and RPMI17951 cells) are plated at a density of 2.5 × 103 cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturers protocol. |
|---|---|
| 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 |
| Animal model | Mice bearing 1205Lu and 1205LuR xenografts |
| Formulation & Dosage | Dissolved in 2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl; 70 mg/kg; Oral gavage |
| References | Mol Cancer Ther. 2015 Jun;14(6):1354-64. |
Related Posts
product name BI-847325
Description: BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 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. BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C.
References: Mol Cancer Ther. 2015 Jun;14(6):1354-64.
464.56
Formula
C29H28N4O2
CAS No.
1207293-36-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 19 mg/mL (40.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl: 30 mg/mL
Synonyms
BI 847325; BI847325.
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393556
| In Vitro |
In vitro activity: 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 Kinase Assay: BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 15 and 4 nM for human AK-C and MEK2, respectively. Cell Assay: Cells (M229, M229R, A375, A375R, WM793, WM793R, 1205Lu, 1205LuR, M249, M249R, WM164, WM164R, WM39 and RPMI17951 cells) are plated at a density of 2.5 × 103 cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturers protocol. |
|---|---|
| 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 |
| Animal model | Mice bearing 1205Lu and 1205LuR xenografts |
| Formulation & Dosage | Dissolved in 2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl; 70 mg/kg; Oral gavage |
| References | Mol Cancer Ther. 2015 Jun;14(6):1354-64. |