Home MAPK MEK inhibitor - Aurora Kinase inhibitor BI-847325 For research use only.

BI-847325

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. Phase 1.

BI-847325 Chemical Structure

BI-847325 Chemical Structure

CAS No. 1207293-36-4

Purity & Quality Control

Batch: S784301 DMSO]19 mg/mL]false]Ethanol]1 mg/mL]false]Water]Insoluble]false Purity: 99.64%
99.64

BI-847325 Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Biological Activity

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. Phase 1.
Targets
Aurora B (Xenopus laevis) [1] MEK2 [1] Aurora C (Human) [1] Aurora A (Human) [1] MEK1 [1]
3 nM 4 nM 15 nM 25 nM 25 nM
In vitro
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. [1]
Cell Research 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
Method 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 manufacturer's protocol.
In Vivo
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. [1]
Animal Research Animal Models Mice bearing 1205Lu and 1205LuR xenografts
Dosages 70 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 464.56 Formula

C29H28N4O2
CAS No. 1207293-36-4 SDF Download BI-847325 SDF
Smiles CCNC(=O)C#CC1=CC2=C(C=C1)C(=C(N2)O)C(=NC3=CC=C(C=C3)CN(C)C)C4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 19 mg/mL ( (40.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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