937366-57-9

Basic information

• Product Name: 3-(2,5-dichloropyriMidin-4-yl)-1H-indole
• Synonyms: 3-(2,5-dichloropyriMidin-4-yl)-1H-indole
• CAS NO: 937366-57-9
• Molecular Formula: C₁₂H₇Cl₂N₃
• Molecular Weight: 264.11008
• Mol File: 937366-57-9.mol
• Article Data: 14

Chemical Properties

• Appearance: /
• Storage Temp.: Sealed in dry,Store in freezer, under -20°C
• CAS DataBase Reference: 3-(2,5-dichloropyriMidin-4-yl)-1H-indole(CAS DataBase Reference)
• NIST Chemistry Reference: 3-(2,5-dichloropyriMidin-4-yl)-1H-indole(937366-57-9)
• EPA Substance Registry System: 3-(2,5-dichloropyriMidin-4-yl)-1H-indole(937366-57-9)

Safety Data

• Hazardous Substances Data: 937366-57-9(Hazardous Substances Data)

Usage

Uses

3-(2,5-Dichloropyrimidin-4-yl)-1H-indole is used in the preparation 2-(2,4,5-substituted -anilino)pyrimidine derivatives as EGFR modulators useful for the prevention or treatment of a number of different cancers, in particular non-small cell lung cancer.

Upstream product

• 120-72-9 indole 
• 5750-76-5 2,4,5-trichloropyrimidine 
• 882562-40-5 3-(2,5-dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole 
• 937366-54-6 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole 
• 129271-98-3 1-(phenylsulfonyl)-1H-indol-3-ylboronic acid 

Downstream Products

• 1356962-34-9 5-Chloro-4-(1H-indol-3-yl)-N-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidin-2-amine 
• 1356962-20-3 AZD3436 

Relevant articles and documents

Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7

CDK7 has emerged as an exciting target in oncology due to its roles in two important processes that are misregulated in cancer cells: cell cycle and transcription. This report describes the discovery of SY-5609, a highly potent (sub-nM CDK7 Kd) and selective, orally available inhibitor of CDK7 that entered the clinic in 2020 (ClinicalTrials.gov Identifier: NCT04247126). Structure-based design was leveraged to obtain high selectivity (>4000-times the closest off target) and slow off-rate binding kinetics desirable for potent cellular activity. Finally, incorporation of a phosphine oxide as an atypical hydrogen bond acceptor helped provide the required potency and metabolic stability. The development candidate SY-5609 displays potent inhibition of CDK7 in cells and demonstrates strong efficacy in mouse xenograft models when dosed as low as 2 mg/kg.

CDK inhibitor based on organic arsine as well as preparation method and application of CDK inhibitor

The invention provides a CDK inhibitor based on organic arsine as well as a preparation method and application of the CDK inhibitor. Specifically, the invention providese compounds of Formula I, or stereoisomers or tautomers thereof, or pharmaceutically acceptable salts, hydrates or solvates thereof; and the invention also discloses a preparation method and application thereof. Definitions of allgroups in the formula are shown in the specification.

Pyrimidine amine compound, and preparation method and application thereof

The invention discloses a polycyclic compound, and a preparation method and an application thereof. The invention provides the polycyclic compound represented by formula I, or a pharmaceutically acceptable salt thereof. The compound has a relatively good inhibition effect on CDK7.