1094614-85-3

Basic information

• Product Name: BIX 02189
• Synonyms: BIX 02189;3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide;(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide;3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide BIX 02189;BIX 02189, >=98%;(Z)-3-(((3-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6;BIX-02189(Random Configuration)
• CAS NO: 1094614-85-3
• Molecular Formula: C27H28N4O2
• Molecular Weight: 440.53682
• Product Categories: MAPK;Inhibitors
• Mol File: 1094614-85-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.230
• Storage Temp.: -20°C Freezer, Under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly)
• CAS DataBase Reference: BIX 02189(CAS DataBase Reference)
• NIST Chemistry Reference: BIX 02189(1094614-85-3)
• EPA Substance Registry System: BIX 02189(1094614-85-3)

Safety Data

• Hazardous Substances Data: 1094614-85-3(Hazardous Substances Data)

Usage

Description

BIX 02189 is a MEK inhibitor that prevents cell proliferation and induces apoptosis. It is a promising pharmaceutical candidate for the treatment of cancers and proliferative cell diseases.

Uses

Used in Cancer Treatment:
BIX 02189 is used as an anticancer agent for its ability to inhibit cell proliferation and induce apoptosis in cancer cells. It can be applied towards treatments of various types of cancers.
Used in Lung Cancer Metastasis Prevention:
BIX 02189 is used as a preventive agent for lung cancer metastasis by directly targeting the TGF-β type I receptor, inhibiting TGF-β1-induced lung cancer cell metastasis.
Used in Proliferative Cell Disease Treatment:
BIX 02189 is used as a therapeutic agent for the treatment of proliferative cell diseases due to its ability to prevent cell proliferation and induce apoptosis.

Biological Activity

bix 02189 is a selective inhibitor of mek5 with ic50 value of 1.5 nm 1.bix 02189 belongs to the indolinone kinase inhibitor series. it selectively inhibited the catalytic activity of mek5 but not other closely related kinases such as mek1, mek2, erk2 and jnk2. bix 02189 also inhibited erk5 with ic50 value of 59 nm. in hela cells, treatment of bix 02189 inhibited the phosphorylation of erk5 but not erk1/2. besides that, bix 02189 prevented the transcription of the downstream substrate mef2c in hela and hek293 cells. moreover, in a three-dimensional lymphangiogenic sprouting assay, bix 02189 resulted in an inhibition of lymphangiogenic sprouting with a minimal effective concentration of 1 μm 1,2.

references

1. tatake r j, o’neill m m, kennedy c a, et al. identification of pharmacological inhibitors of the mek5/erk5 pathway. biochemical and biophysical research communications, 2008, 377(1): 120-125.2. schulz m m p, reisen f, zgraggen s, et al. phenotype-based high-content chemical library screening identifies statins as inhibitors of in vivo lymphangiogenesis. proceedings of the national academy of sciences, 2012, 109(40): e2665-e2674.