ZM 336372 (c-Raf inhibitor）

Biological Activity

ZM 336372 is a potent, selective, and ATP-competitive inhibitor of c-Raf kinase (Raf-1, IC₅₀ = 70 nM) that shows 10-fold selectivity over B-Raf, a 30-fold selectivity over SAPK2/p38 (IC₅₀= 2 μM) but with no inhibition against 17 other protein kinases even at 50 nM. ZM 336372 displays a paradoxical response of >100-fold Raf-1 activation without triggering any activation of MKK1 or p42 MAPK/ERK2 in whole cell cultures ^[1]. ZM 336372 results in progressive phosphorylation of Raf-1 pathway mediators, significant reduction of chromogranin A, and decreased expression of neuroendocrine transcription factor, hASH1. ZM 336372 displays the capability to suppress cell proliferation and induce cell cycle inhibitors in carcinoid tumor cells ^[2]. ZM336372, as a Raf-1 activator, may be a potential drug for both therapeutic and palliative treatment for neuroendocrine tumors (NETs) ^[3-5] as well as hepatocellular carcinoma, with similar characteristics with that of NETs ^[6].

Chemical Properties

Cas No.: 208260-29-1	M. Wt.: 389.45
Formula: C23H23N3O3	Purity: >98% by HPLC
Synonym: ZM336372,ZM-336372
Chemical Name: 3-(dimethylamino)-N-[3-[(4-hydroxybenzoyl)-amino]-4-methylphenyl]benzamide
Appearance: White solid
Solubility: Soluble in DMSO (to 100 mM)
Storage：Store solid at -20 ºC for the stability up to two years

Application Concentration (Just for reference)

The appropriate working concentration of ZM 336372 depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.