ChemicalBook > CAS DataBase List > BI-847325

BI-847325

Product Name: BI-847325
CAS No.: 1207293-36-4
Chemical Name: BI-847325
Synonyms: BI-847325;BI 847325;BI847325;BI-847325, 10 mM in DMSO;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-
CBNumber: CB12743902
Molecular Formula: C29H28N4O2
Formula Weight: 464.56
MOL File: 1207293-36-4.mol

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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
color: Light yellow to yellow

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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.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 18301
Product name: BI-847325
Purity: ≥98%
Packaging: 1mg
Price: $73
Updated: 2024/03/01

Cayman Chemical

Product number: 18301
Product name: BI-847325
Purity: ≥98%
Packaging: 5mg
Price: $171
Updated: 2024/03/01

TRC

Product number: B591715
Product name: BI-847325
Packaging: 100mg
Price: $1240
Updated: 2021/12/16

ApexBio Technology

Product number: B6014
Product name: BI-847325
Packaging: 5mg
Price: $173
Updated: 2021/12/16

AK Scientific

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

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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.

in vivo

Daily oral administration of BI 847325 at 10 mg/kg shows efficacy in both BRAF- and KRAS-mutant xenograft models. BI 847325 administered once weekly at 70 mg/kg inhibits both MEK and AK in KRAS-mutant tumors^[1].

IC 50

MEK2: 4 nM (IC₅₀); Aurora C: 15 nM (IC₅₀)

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..

BI-847325 Preparation Products And Raw materials

Raw materials

Preparation Products

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1207293-36-4, BI-847325Related Search:

BI-847325

3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide

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

BI 847325;BI847325

BI-847325;BI 847325;BI847325

(Z)-3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide

2-Propynamide, 3-[3-[[[4-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-

3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide

BI 847325,inhibit,Apoptosis,MEK,MAPKK,MAP2K,Inhibitor,Aurora Kinase,Mitogen-activated protein kinase kinase,BI847325,BI-847325

BI-847325, 10 mM in DMSO

1207293-36-4

APIs