Tag: M.W=200-250

Lee, Heajin; Landgraf, Ralf; Wilson, James N. published the artcile< Synthesis and photophysical properties of a fluorescent cyanoquinoline probe for profiling ERBB2 kinase inhibitor response>, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid, the main research area is cyanoquinoline fluorescent probe preparation ERBB2 kinase inhibitor; EGFR; ERBB; Fluorescent probe; Kinase inhibitor; Receptor tyrosine kinase.

A fluorescent probe targeting the ERBB2 receptor tyrosine was designed, synthesized and evaluated as reporter of ERBB2 dynamics in overexpressing BT474, i.e. Her2(+), cells. Two cyanoquinoline (CQ) probes modeled after type-I (CQ1, I) or active state and type-II (CQ2, II) or inactive state inhibitors were designed and synthesized with extended π systems that impart binding-induced, turn-on fluorescence. Solution spectroscopy revealed that I exhibited attractive photophys. properties and displayed turn-on emission in the presence of purified, soluble ERBB2 kinase domain, while II was found to be non-emissive, likely due to quenching via a photoinduced electron transfer mechanism. Live cell imaging with I revealed that this probe targeted an intracellular population of ERBB2, which increased following treatment with type-I inhibitors, gefinitib and canertinib, but showed no response to type-II inhibitors. I thus provides a novel means of imaging the dynamic response of ERBB2(+) cells to kinase inhibitors.

Bioorganic & Medicinal Chemistrypublished new progress about Density functional theory. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Lu, Xi; Wang, Xiao-Xu; Gong, Tian-Jun; Pi, Jing-Jing; He, Shi-Jiang; Fu, Yao published the artcile< Nickel-catalyzed allylic defluorinative alkylation of trifluoromethyl alkenes with reductive decarboxylation of redox-active esters>, Name: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid, the main research area is functionalized geminal difluoroalkene preparation; haloalkene redox active ester defluorinative reductive coupling nickel catalyst.

An efficient method was developed for the synthesis of functionalized gem-difluoroalkenes I [R = c-hexyl, 4-BrC6H4(CH2)2, 4-CNC6H4O(CH2)2C(Me)2, etc.; Ar = 3,4-(OMe)2C6H3, 4-PhC6H4, 2-naphthyl, etc.] via nickel-catalyzed defluorinative reductive cross-coupling of trifluoromethyl alkenes with redox-active esters. The present reaction involved C(sp3)-F bond cleavage and C(sp3)-C(sp3) bond formation under very mild reaction conditions, while tolerating many sensitive functional groups and requiring minimal substrate protection. Therefore, this method provided an efficient and convenient approach for late-stage modification of biol. interesting mols.

Chemical Sciencepublished new progress about Carboxylic esters Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Name: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Cheng, Chuanjie; Sun, Jianwei; Xing, Lixin; Xu, Jimin; Wang, Xinyan; Hu, Yuefei published the artcile< Highly Chemoselective Pd-C Catalytic Hydrodechlorination Leading to the Highly Efficient N-Debenzylation of Benzylamines>, Product Details of C9H19ClN2O2, the main research area is benzylamine debenzylation synergistic trichloroethane chemoselective hydrodechlorination palladium catalyst; amine hydrochloride preparation.

In the presence of 1,1,2-trichloroethane, a novel procedure for the Pd-C catalytic N-debenzylation of benzylamines was established. The method proceeded in a synergistic catalytic system and directly gave the products as crystalline amine hydrochlorides in practically quant. yields.

Journal of Organic Chemistrypublished new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent) (benzylic). 76535-74-5 belongs to class piperazines, and the molecular formula is C9H19ClN2O2, Product Details of C9H19ClN2O2.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Lee, Heajin; Liu, Wenjun; Brown, Adrienne S.; Landgraf, Ralf; Wilson, James N. published the artcile< Fluorescent Kinase Probes Enabling Identification and Dynamic Imaging of HER2(+) Cells>, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid, the main research area is fluorescent kinase probe imaging HER2 cancer.

The human epidermal growth factor receptor, EGFR/ERBB/HER, family of receptor tyrosine kinases is central to many signaling pathways and a validated chemotherapy target in multiple cancers. While EGFR/ERBB-targeted therapies, including monoclonal antibodies, e.g., trastuzumab, and small mol. kinase inhibitors, such as lapatinib, have been developed, rapid identification and classification of cancer cells is key to identifying the best treatment regime. The authors report ERBB2 (also HER2) targeting kinase probes that exhibit a “”turn-on”” emission response upon binding. These live cell compatible probes differentiate ERBB2(+) cells from low-level, ERBB2(-) cells by targeting the intracellular ATP-binding pocket of ERBB2 with therapeutic inhibitor-like specificity. Beyond kinase expression levels, probe signal is linked to the phosphotyrosine-correlated activation state of the ERBB2 population. Addnl., the rapid signaling capability of the probes can report changes in activation state in live cells providing a unique type of complementary information to immunohistochem. assays of receptor kinase populations.

Analytical Chemistry (Washington, DC, United States)published new progress about Confocal laser scanning microscopy. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics