1207293-36-4

Basic information

• Product Name: BI-847325
• Synonyms: 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)
• CAS NO: 1207293-36-4
• Molecular Formula: C29H28N4O2
• Molecular Weight: 464.55822
• EINECS: -0
• Mol File: 1207293-36-4.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Solubility: ≥24.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
• CAS DataBase Reference: BI-847325(CAS DataBase Reference)
• NIST Chemistry Reference: BI-847325(1207293-36-4)
• EPA Substance Registry System: BI-847325(1207293-36-4)

Safety Data

• Hazardous Substances Data: 1207293-36-4(Hazardous Substances Data)

Usage

Description

BI-847325 is a selective dual MEK/Aurora kinase inhibitor with potent activity against various kinases, including X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2. It has demonstrated the ability to inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines by suppressing the expression of Mcl-1 and MEK while increasing the expression of the pro-apoptotic protein Bim. BI-847325 has been studied for its efficacy in patients with refractory solid tumors.

Uses

Used in Oncology:
BI-847325 is used as an anticancer agent for the treatment of melanoma, particularly in cases where the tumor cells have become resistant to standard treatments. It works by inhibiting the growth of BRAF resistant melanoma cells through the suppression of Mcl-1 and MEK expression in human melanoma cell lines and mouse xenograft models. At a dosage of 70 mg/kg, BI-847325 has been shown to induce apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.
Additionally, the compound has been investigated for its potential use in treating patients with refractory solid tumors, indicating its possible broader application in oncology beyond melanoma treatment.

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..

Relevant articles and documents

NEW COMPOUNDS

The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use