BI-847325
- Product Name
- BI-847325
- CAS No.
- 1207293-36-4
- Chemical Name
- BI-847325
- Synonyms
- BI-847325;BI 847325;BI847325;BI-847325;BI 847325;BI847325;BI-847325, 98%, an ATP competitive dual inhibitor of MEK and aurora kinases (AK);3-[3-[[4-(dimethylaminomethyl)anilino]-phenylmethylidene]-2-oxo-1H-indol-6-yl]-N-ethylprop-2-ynamide;3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide;(Z)-3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide;3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide;2-Propynamide, 3-[3-[[[4-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-;BI 847325,inhibit,Apoptosis,MEK,MAPKK,MAP2K,Inhibitor,Aurora Kinase,Mitogen-activated protein kinase kinase,BI847325,BI-847325
- CBNumber
- CB12743902
- Molecular Formula
- C29H28N4O2
- Formula Weight
- 464.56
- MOL File
- 1207293-36-4.mol
BI-847325 Property
- storage temp.
- Store at -20°C
- solubility
- ≥24.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
- form
- crystalline solid
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 18301
- Product name
- BI-847325
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 18301
- Product name
- BI-847325
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $171
- Updated
- 2024/03/01
- Product number
- B591715
- Product name
- BI-847325
- Packaging
- 100mg
- Price
- $1240
- Updated
- 2021/12/16
- Product number
- B6014
- Product name
- BI-847325
- Packaging
- 5mg
- Price
- $173
- Updated
- 2021/12/16
- Product number
- 3237EM
- Product name
- 3-[3-[N-[4-[(Dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide
- Packaging
- 1mg
- Price
- $179
- Updated
- 2021/12/16
BI-847325 Chemical Properties,Usage,Production
Description
BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC50 values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively. It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim. At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.
Uses
BI-847325 is a novel ATP-competitive MEK and Aurora kinase inhibitor. It can inhibit the growth of BRAF resistant melanoma cells through suppression of Mcl-1 and MEK expression in human melanoma cell lines and mouse xenograft model. The efficacy of BI-847325 was studied in patients with refractory solid tumors.
References
[1]. sini p, gürtler u, zahn sk, et al. pharmacological characterization of bi 847325, a dual inhibitor of mek and aurora kinases. cancer research, 2012, 72(8 supplement): 1919-1919.
[2]. hideshima t, chauhan d, richardson p, et al. nf-κb as a therapeutic target in multiple myeloma. journal of biological chemistry, 2002, 277(19): 16639-16647.
[3]. rommel c, clarke ba, zimmermann s, et al. differentiation stage-specific inhibition of the raf-mek-erk pathway by akt. science, 1999, 286(5445): 1738-1741..