Month: November 2022

On December 31, 2011, Hu, Le-Le; Chen, Chen; Huang, Tao; Cai, Yu-Dong; Chou, Kuo-Chen published an article.COA of Formula: C17H21ClFN3O4 The title of the article was Predicting biological functions of compounds based on chemical-chemical interactions. And the article contained the following:

Given a compound, how can we effectively predict its biol. function. It is a fundamentally important problem because the information thus obtained may benefit the understanding of many basic biol. processes and provide useful clues for drug design. In this study, based on the information of chem.-chem. interactions, a novel method was developed that can be used to identify which of the following eleven metabolic pathway classes a query compound may be involved with: (1) Carbohydrate Metabolism, (2) Energy Metabolism, (3) Lipid Metabolism, (4) Nucleotide Metabolism, (5) Amino Acid Metabolism, (6) Metabolism of Other Amino Acids, (7) Glycan Biosynthesis and Metabolism, (8) Metabolism of Cofactors and Vitamins, (9) Metabolism of Terpenoids and Polyketides, (10) Biosynthesis of Other Secondary Metabolites, (11) Xenobiotics Biodegradation and Metabolism It was observed that the overall success rate obtained by the method via the 5-fold cross-validation test on a benchmark dataset consisting of 3,137 compounds was 77.97%, which is much higher than 10.45%, the corresponding success rate obtained by the random guesses. Besides, to deal with the situation that some compounds may be involved with more than one metabolic pathway class, the method presented here is featured by the capacity able to provide a series of potential metabolic pathway classes ranked according to the descending order of their likelihood for each of the query compounds concerned. Furthermore, our method was also applied to predict 5,549 compounds whose metabolic pathway classes are unknown. Interestingly, the results thus obtained are quite consistent with the deductions from the reports by other investigators. It is anticipated that, with the continuous increase of the chem.-chem. interaction data, the current method will be further enhanced in its power and accuracy, so as to become a useful complementary vehicle in annotating uncharacterized compounds for their biol. functions. A dissertation. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).COA of Formula: C17H21ClFN3O4

The Article related to carbohydrate energy lipid biol function, metabolic pathway chem interaction, Pharmacology: Methods and other aspects.COA of Formula: C17H21ClFN3O4

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

Claudiani, Simone; Apperley, Jane F.; Szydlo, Richard; Khan, Afzal; Nesr, George; Hayden, Chloe; J. Innes, Andrew; Dominy, Kathy; Foskett, Pierre; Foroni, Letizia; Khorashad, Jamshid; Milojkovic, Dragana published an article in 2021, the title of the article was TKI dose reduction can effectively maintain major molecular remission in patients with chronic myeloid leukaemia.Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile And the article contains the following content:

A review. Targeted therapy for chronic myeloid leukemia (CML) has allowed for a near-normal patient life-expectancy; however, quality of life and aggravation of existing co-morbidities have posed new treatment challenges. In clin. practice, TKI dose reduction occurs frequently, often on multiple occasions, because of intolerance. We conducted a retrospective ‘real-world practice’ review of 246 patients receiving lower than standard dose (LD) TKI after the achievement o major mol. response (MR3), because of intolerable adverse events. In 274 of 298 cases of dose reduction (91·9%), MR3 was maintained at median follow-up of 27·3 mo. One patient progressed to blast crisis while on LD TKI. Two patients developed two new ABL kinase domain mutations (T315I and V299L), of whom one had achieved deep mol. response on an alternative LD TKI at last follow-up. Seventy-six patients eventually discontinued LD TKI and the two-year treatment-free remission (TFR) rate in these patients was 74·1%. The majority of patients with CML in at least MR3 appear to be safely managed with LD TKI, although three of 246 patients had new events (progression and new mutation), indicating that this approach requires vigilance. TKI LD does not prevent the achievement of TFR in this patient population. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to review tyrosine kinase inhibitor dose patient chronic myeloid leukemia, cml, tfr, tki, dose-reduction, low dose, Pharmacology: Reviews and other aspects.Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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

Breccia, Massimo; Colafigli, Gioia; Scalzulli, Emilia; Martelli, Maurizio published an article in 2021, the title of the article was Asciminib an investigational agent for the treatment of chronic myeloid leukemia.COA of Formula: C26H29Cl2N5O3 And the article contains the following content:

A review. Tyrosine kinase inhibitors (TKIs) have drastically changed the outcome of chronic myeloid leukemia (CML) patients. However, a subset of patients experienced resistance and/or intolerance and need to switch to other agents. Resistance to second-generation TKIs used in first-line treatment is less of an issue when compared to imatinib in first line. New drugs that are able to improve efficacy, without long-term off-target effects are needed. Allosteric inhibitors such as asciminib (ABL001) were created to overcome resistance and off-target toxicity.: In this review, we report the mechanism of action, pharmacokinetic data, and the clin. trial results of asciminib tested in chronic phase CML patients.: Asciminib, the first example of allosteric inhibition, could be a promising approach as third-line therapy and in the subset of patients with T315I mutation that, for coexistent comorbidities, cannot receive other drugs. Future results will probably help to move the drug to earlier lines of treatment. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).COA of Formula: C26H29Cl2N5O3

The Article related to review asciminib chronic myeloid leukemia investigational agent, chronic myeloid leukemia, allosteric inhibition, asciminib, tyrosine kinase inhibitors, Pharmacology: Reviews and other aspects.COA of Formula: C26H29Cl2N5O3

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

On May 1, 2021, Verougstraete, Nick; Stove, Veronique; Verstraete, Alain G.; Stove, Christophe published an article.Recommanded Product: 380843-75-4 The title of the article was Quantification of eight hematological tyrosine kinase inhibitors in both plasma and whole blood by a validated LC-MS/MS method. And the article contained the following:

Therapeutic drug monitoring (TDM) of tyrosine kinase inhibitors (TKIs) in cancer therapy offers the potential to improve treatment efficacy while minimizing toxicity. Therefore, a high-throughput, sensitive LC-MS/MS method was developed and validated, to be used for personalized treatment of hematol. malignancies. The assay allows the simultaneous quantification in plasma (EDTA and heparin) and whole blood of eight TKIs, including bosutinib, dasatinib, gilteritinib, ibrutinib, imatinib, midostaurin, nilotinib and ponatinib, which are used in the treatment of chronic and acute myeloid leukemia (CML, AML) and chronic lymphocytic leukemia (CLL). The procedure involves simple protein precipitation of 50μL of sample, a 4-min chromatog. separation by applying gradient elution on a standard reverse phase column, and tandem mass spectrometric detection. The method was successfully validated based on international guidelines in terms of calibration curves, precision (within-run CV 0.74-16.4%; between-run CV 1.65-17.8%), accuracy (within-run bias 0.07-19.8%; between-run bias 0.05 to -17.6%), carry-over (max 19.4%, for ponatinib), selectivity, matrix-effects, recovery (ranging from 61 to 128%), stability (only issues observed for ibrutinib) and dilution integrity. Furthermore, the accuracy of the method was demonstrated by analyzing external quality controls, with a maximum bias of -11.3%. Assay applicability was demonstrated by analyzing authentic plasma and whole blood samples in order to derive blood-plasma ratios and the variation thereof. The latter are important to allow possible blood-plasma conversion when envisaging possible future implementation of TDM via dried blood microsampling. The presented method can be applied in clin. practice for performing TDM of TKIs in plasma and whole blood samples. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Recommanded Product: 380843-75-4

The Article related to hematol plasma blood tyrosine kinase inhibitors lc ms, chronic myeloid leukemia, lc-ms/ms, therapeutic drug monitoring (tdm), tyrosine kinase inhibitors, Pharmacology: Methods and other aspects.Recommanded Product: 380843-75-4

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

On January 14, 2020, Gambacorti-Passerini, Carlo; Coutre, Philipp le; Piazza, Rocco published an article.SDS of cas: 380843-75-4 The title of the article was The role of bosutinib in the treatment of chronic myeloid leukemia. And the article contained the following:

A review. The availability of several BCR-ABL1 tyrosine kinase inhibitor (TKI) options means physicians and patients can select the most appropriate treatment for a patient with chronic myeloid leukemia (CML). BCR-ABL TKI selection as a first- or later-line therapy is dependent on a number of clin. factors. Regular monitoring of patients, patient education, dose optimization and management of treatment-emergent adverse events are key aspects of long-term chronic myeloid leukemia management and contribute to improved clin. outcomes, quality of life, patient adherence and healthcare costs. This review provides an overview of the BCR-ABL1 TKI bosutinib, its pharmacol. and clin. trials; discusses the impact of comorbidities and concomitant medications on bosutinib treatment selection; and suggests strategies for managing adverse events and dose optimization during bosutinib treatment. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).SDS of cas: 380843-75-4

The Article related to review tyrosine kinase inhibitor bosutinib chronic myeloid leukemia pharmacol, bosutinib, chronic myeloid leukemia, first-line, later-line, treatment selection, Pharmacology: Reviews and other aspects.SDS of cas: 380843-75-4

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

On January 15, 2020, Mukai, Yuji; Yoshida, Tatsunari; Kondo, Takeshi; Inotsume, Nobuo; Toda, Takaki published an article.Product Details of 380843-75-4 The title of the article was Novel high-performance liquid chromatography-tandem mass spectrometry method for simultaneous quantification of BCR-ABL and Bruton’s tyrosine kinase inhibitors and their three active metabolites in human plasma. And the article contained the following:

Therapeutic drug monitoring is important in patients taking BCR-ABL and Bruton’s tyrosine kinase inhibitors (TKIs). Some TKI active metabolites with long elimination half-lives, such as dihydrodiol ibrutinib (DHI), N-desmethyl imatinib (N-DI), and N-desmethyl ponatinib (N-DP), have been characterized, indicating that these active metabolites should be monitored along with the parent compounds However, there are currently no methods for the simultaneous quantification of BCR-ABL and Bruton’s TKIs and their three active metabolites. The present study aimed to develop and validate a method for the simultaneous quantification of nine pharmacol. active compounds (bosutinib, dasatinib, DHI, ibrutinib, imatinib, N-DI, N-DP, nilotinib, and ponatinib) using high-performance liquid chromatog.-tandem mass spectrometry. A 150-μL sample of plasma was analyzed after purification with supported liquid extraction The method has a run time of 7 min and was successfully validated over the following calibration ranges: 0.25-75 ng/mL for N-DP, 0.5-150 ng/mL for dasatinib and ponatinib, 10-3000 ng/mL for imatinib and nilotinib, and 1-300 ng/mL for the other analytes. Stability of the analytes after short- and long-term storage in the presence of plasma matrix was examined, and all analytes were found to be stable under all tested conditions. The recovery was ≥83%, and the relative standard deviation of internal-standard normalized matrix effects ranged from 3.9 to 13.9%. Dilution integrity up to 4-fold was ensured. The applicability of the method for all analytes was demonstrated using patient samples. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Product Details of 380843-75-4

The Article related to hplc ms determination bcrabl bruton’s kinase inhibitor metabolite plasma, lc-ms/ms, plasma concentration, therapeutic drug monitoring, tyrosine kinase inhibitor, Pharmacology: Methods and other aspects.Product Details of 380843-75-4

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

On May 31, 2020, Casavecchia, Grazia; Galderisi, Maurizio; Novo, Giuseppina; Gravina, Matteo; Santoro, Ciro; Agricola, Eustachio; Capalbo, Silvana; Zicchino, Stefano; Cameli, Matteo; De Gennaro, Luisa; Righini, Francesca Maria; Monte, Ines; Tocchetti, Carlo Gabriele; Brunetti, Natale Daniele; Cadeddu, Cristian; Mercuro, Giuseppe published an article.Quality Control of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile The title of the article was Early diagnosis, clinical management, and follow-up of cardiovascular events with ponatinib. And the article contained the following:

A review. Abstract: Chronic myeloid leukemia (CML) is a myeloproliferative disorder characterized by neoplastic transformation of pluripotent cells due to a typical cytogenetic and mol. mutation known as Philadelphia (Ph) chromosome. In 2001, the introduction of the tyrosine kinasis inhibitor (TKI) imatinib as a therapeutic strategy for CML with PH chromosome mutation represented an important step towards treatment of these patients, and nowadays, this drug represents the gold therapeutic standard in this clin. setting. A second generation of TKIs (dasatinib, nilotinib, and bosutinib) showed an effective action in all patients with mutations resistant to imatinib. Ponatinib is a third-generation TKI and is the only inhibitor with activity against T3151 mutation. The impact of ponatinib on cardiovascular events was first evaluated in the PACE trial. We therefore report and discuss most relevant evidence currently available on cardiovascular events associated with the use of ponatinib. Though many exams can be used for diagnosis and follow-up of this kind of cardiotoxicity, echocardiog. seems to have a pivotal role thanks to its feasibility, availability, and low cost. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Quality Control of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to review chronic myeloid leukemia cardiovascular event diagnosis ponatinib, cardio-oncology, chronic myeloid leukemia, ponatinib, review, tyrosine kinase inhibitors, Pharmacology: Reviews and other aspects.Quality Control of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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

Yuzbasioglu, Mebrure Burcak; Eskazan, Ahmet Emre published an article in 2021, the title of the article was Bosutinib – related pleural effusion in patients with chronic myeloid leukemia.HPLC of Formula: 380843-75-4 And the article contains the following content:

A review. Tyrosine kinase inhibitors (TKIs) are the mainstay of the current management of chronic myeloid leukemia (CML). Dasatinib is a 2GTKI, which is utilized in CML treatment both in the upfront and salvage settings Lymphocytosis pleural effusion. Bosutinib is another potent 2GTKI, which can also be used in the first- and subsequent-lines in patients with CML [20]. It is a dual Src/Abl TKI, and it exhibits minimal inhibitory activity against c-KIT or PDGFR [21]. Diarrhea is the most common AE of bosutinib therapy. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).HPLC of Formula: 380843-75-4

The Article related to review dasatinib bosutinib anticancer agent chronic myeloid leukemia, adverse event, bosutinib, chronic myeloid leukemia, pleural effusion, tyrosine kinase inhibitor, Pharmacology: Reviews and other aspects.HPLC of Formula: 380843-75-4

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

On February 28, 2021, Li, Huan-Ting; Zhu, Xiaoyong published an article.Electric Literature of 380843-75-4 The title of the article was Quinoline-based Compounds with Potential Activity against Drug-resistant Cancers. And the article contained the following:

A review. Drug resistance is the major cause of the failure of cancer chemotherapy, so one of the most important features in developing effective cancer therapeutic strategies is to overcome drug resistance. Quinoline moiety has become one of the most privileged structural motifs in anticancer agent discovery since its derivatives possess potent activity against various cancers including drug-resistant cancers. Several quinoline-based compounds which are represented by Anlotinib, Bosutinib, Lenvatinib, and Neratinib have already been applied in clin. practice to fight against cancers, so quinoline-based compounds are potential anticancer agents. The present short review article provides an overview of the recent advances of quinoline-based compounds with potential activity against drug-resistant cancers. The structure-activity relationship and mechanisms of action are also discussed. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Electric Literature of 380843-75-4

The Article related to review quinoline potential activity against drug resistant cancer, anticancer, cancers, drug resistance, mechanisms of action, quinoline, structure-activity relationship, Pharmacology: Reviews and other aspects.Electric Literature of 380843-75-4

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

On March 31, 1996, Rispal, Patric; Grellet, Jean; Celerier, Christophe; Breilh, Dominique; Dorian, Martine; Pellegrin, Jean Luc; Saux, Marie Claude; Leng, Bernard published an article.Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the article was Comparative uptake of sparfloxacin and ciprofloxacin into human THP 1 monocytic cells: evidence for an organic anion transport. And the article contained the following:

The uptake of sparfloxacin (CAS 11542-93-9) by human monocytes was studied by comparison with ciprofloxacin (CAS 86393-32-0). The human monocytic THP 1 cells were incubated with the antibiotics for 2 h. Entry of antimicrobials into the cells was determined by means of a velocity gradient centrifugation technique and HPLC assay. Antibiotic uptake was expressed as the ratio of the intracellular to the extracellular drug concentration (IC/EC). Quinolones enter readily in monocytic cells but sparfloxacin is taken up more rapidly than ciprofloxacin. At steady-state the IC/EC ratio of sparfloxacin (9.07) is higher than IC-EC of ciprofloxacin (4.29). Characterization of quinolone uptake suggests that these drugs penetrate throughout the THP 1 membrane by passive diffusion. However, the results of the present study indicate that addnl. mechanisms may contribute to intracellular accumulation of ciprofloxacin and sparfloxacin but does not modify IC/EC of sparfloxacin. It can be concluded that human monocyte-like cells have functional organic anion transporters and that this way of secretion is quinolone selective. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to sparfloxacin ciprofloxacin monocyte organic anion transport, Pharmacology: Drug Metabolism and other aspects.Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

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