909712-01-2

Basic information

• Product Name: (5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone
• CAS NO: 909712-01-2
• Molecular Weight: 284.156
• Mol File: 909712-01-2.mol
• Article Data: 8

Chemical Properties

• CAS DataBase Reference: (5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone(CAS DataBase Reference)
• NIST Chemistry Reference: (5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone(909712-01-2)
• EPA Substance Registry System: (5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone(909712-01-2)

Safety Data

• Hazardous Substances Data: 909712-01-2(Hazardous Substances Data)

Usage

General Description

(5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone is a chemical compound with the molecular formula C12H15BrN4O. It is a combination of a bromopyridine group and a methylpiperazine group attached to a methanone functional group. (5-bromopyridin-2-yl)(4-methylpiperazin-1-yl)methanone has potential applications in medicinal chemistry and drug development, as both the bromopyridine and methylpiperazine groups are commonly found in pharmaceuticals and have been associated with various biological activities. The presence of the methanone functional group also indicates potential reactivity and compatibility with different biological systems. Overall, this compound is a versatile building block for the synthesis of novel bioactive molecules and has potential in drug discovery and development.

Upstream product

• 109-01-3 1-methyl-piperazine 
• 30766-11-1 5-bromoisonicotinic acid 
• 137178-88-2 5-bromopyridine-2-carbonyl chloride 

Relevant articles and documents

Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT

Herein, we report two promising compounds 30 and 36 possessing nanomolar FLT3 inhibitory activities (IC50 = 1.5-7.2 nM), high selectivity over c-KIT (>1000-fold), and excellent anti-AML activity (MV4-11 IC50 = 0.8-3.2 nM). Furthermore, these two compounds efficiently inhibited the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y. Oral administration of 30 and 36 at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5% and 95.1%, respectively. Importantly, 36 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W. No clear myelosuppression was observed in the treated group of 36 in the MPO strain of zebrafish, even at 10 μM. In summary, our data demonstrated that 36 may represent a promising candidate for the treatment of FLT3 mutant AML.

1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES

The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.

Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.