Category: piperazines

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 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 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

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

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