923032-37-5

Basic information

• Product Name: RDEA119
• Synonyms: RDEA119;BAY-869766;RefaMetinib;RDEA-119 (BAY-869766);BAY 8697661;RefaMetinib/BAY 8697661;N-[3,4-Difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropanesulfonamide;(S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
• CAS NO: 923032-37-5
• Molecular Formula: C19H20F3IN2O5S
• Molecular Weight: 572.3371796
• Product Categories: Inhibitors
• Mol File: 923032-37-5.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 566.9±60.0 °C(Predicted)
• Appearance: /
• Density: 1.82±0.1 g/cm3(Predicted)
• Solubility: insoluble in H2O; ≥151.8 mg/mL in DMSO; ≥90.2 mg/mL in EtOH
• PKA: 15.54±0.20(Predicted)
• CAS DataBase Reference: RDEA119(CAS DataBase Reference)
• NIST Chemistry Reference: RDEA119(923032-37-5)
• EPA Substance Registry System: RDEA119(923032-37-5)

Safety Data

• Hazardous Substances Data: 923032-37-5(Hazardous Substances Data)

Usage

Description

RDEA119, also known as Refametinib and Bay 86-9766, is a potent, ATP non-competitive, and highly selective inhibitor of MEK1 and MEK2. It is an oral TKI that targets both ALK and ROS1 with high affinity and good CNS penetration.
Used in Pharmaceutical Industry:
RDEA119 is used as a potent MEK inhibitor for the treatment of various cancers. Its high selectivity and affinity for MEK1 and MEK2 make it a promising candidate for targeted cancer therapy.
Used in Cancer Research:
RDEA119 is used as a research tool for studying the role of MEK1 and MEK2 in cancer cell growth and proliferation. Its potent inhibitory effects on these proteins can provide valuable insights into the development of novel cancer therapies.
Used in Drug Development:
RDEA119 is used in the development of new drugs targeting the MEK pathway. Its high selectivity and potency make it a valuable compound for designing and testing new therapeutic agents for cancer treatment.

Clinical Use

Lorlatinib is the sole third-generation ALK inhibitor at this time; it is approved for ALK-positive NSCLC patients who progressed on at least two ALK inhibitors with one being crizotinib or who progressed on alectinib or ceritinib if either is used in the frontline setting.

references

[1] iverson c, larson g, lai c, et al. rdea119/bay 869766: a potent, selective, allosteric inhibitor of mek1/2 for the treatment of cancer. cancer research, 2009, 69(17): 6839-6847.

Upstream product

• 923032-74-0 3,4-difluoro-N₂-(2-fluoro-4-iodo-phenyl)-6-methoxy-benzene-1,2-diamine 
• 1262760-00-8 (S)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonyl chloride 
• 1335100-23-6 butyl 1-[(2S)-3-{[tert-butyl(dimethyl)silyl]oxy}-2-hydroxypropyl]cyclopropanesulfonate 
• 1335100-27-0 butyl 1-[(2R)-oxiran-2-ylmethyl]cyclopropanesulfonate 
• 1335100-29-2 butyl 1-[(2S)-2,3-dihydroxypropyl]cyclopropanesulfonate 
• 1335100-31-6 butyl 1-{[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}cyclopropanesulfonate 
• 1415503-36-4 1-{[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}cyclopropanesulfonyl bromide 
• 1415503-37-5 1-{[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}cyclopropanesulfonyl bromide 
• 1262760-35-9 (R)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropanethiol 
• 1262760-33-7 sodium (R)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonate 
• 1262760-31-5 1,2-bis(1-(((R)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropyl)disulfane 
• 1262760-10-0 (R)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonamide 
• 1262759-99-8 (R)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonyl chloride 
• 1262760-09-7 (R)-4-((1-iodocyclopropyl)methyl)-2,2-dimethyl-1,3-dioxolane 

Relevant articles and documents

BIOMARKERS FOR DETERMINING EFFECTIVE RESPONSE OF TREATMENTS OF HEPATOCELLULAR CARCINOMA (HCC) PATIENTS

This invention is directed to the use of one or more biomarkers defined as KRAS or NRAS gene for predicting the pharmaceutical efficacy or clinical response of MEK protein kinase inhibitor and/or Sorafenib or Regorafenib to be administred to a Hepatocellu

PREPARATION OF (R)- AND (S)-N-(3, 4-DIFLUORO-2-(2-FLUORO-4-IODOPHENYLAMINO)--6-METHOXYPHENYL) -1- (2, 3-DIHYDROXYPROPYL)CYCLOPROPANE-1-SULFONAMIDE AND PROTECTED DERIVATIVES THEREOF

The present invention relates to the preparation of (R)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydr

N-(ARYLAMINO)-SULFONAMIDE INHIBITORS OF MEK

This invention concerns N-(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.