Tag: 500-600

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

On October 1, 2020, Weatherald, Jason; Bondeelle, Louise; Chaumais, Marie-Camille; Guignabert, Christophe; Savale, Laurent; Jais, Xavier; Sitbon, Olivier; Rousselot, Philippe; Humbert, Marc; Bergeron, Anne; Montani, David published an article.Synthetic Route of 380843-75-4 The title of the article was Pulmonary complications of Bcr-Abl tyrosine kinase inhibitors. And the article contained the following:

A review. Tyrosine kinase inhibitors (TKIs) targeting the Bcr-Abl oncoprotein revolutionised the treatment of chronic myelogenous leukemia. Following the success of imatinib, second- and third-generation mols. were developed. Different profiles of kinase inhibition and off-target effects vary between TKIs, which leads to a broad spectrum of potential toxicities. Pulmonary complications are most frequently observed with dasatinib but all other Bcr-Abl TKIs have been implicated. Pleural effusions are the most frequent pulmonary complication of TKIs, usually associated with dasatinib and bosutinib. Pulmonary arterial hypertension is an uncommon but serious complication of dasatinib, which is often reversible upon discontinuation. Bosutinib and ponatinib have also been associated with pulmonary arterial hypertension, while imatinib has not. Rarely, interstitial lung disease has been associated with TKIs, predominantly with imatinib. Mechanistically, dasatinib affects maintenance of normal pulmonary endothelial integrity by generating mitochondrial oxidative stress, inducing endothelial apoptosis and impairing vascular permeability in a dose-dependent manner. The mechanisms underlying other TKI-related complications are largely unknown. Awareness and early diagnosis of the pulmonary complications of Bcr-Abl TKIs is essential given their seriousness, potential reversibility, and impact on future treatment options for the underlying chronic myelogenous leukemia. 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).Synthetic Route of 380843-75-4

The Article related to review bcr abl anticancer agent myelogenous leukemia, Pharmacology: Reviews and other aspects.Synthetic Route of 380843-75-4

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

On June 30, 2021, Wall, Thomas P.; Crowley, Peter D.; Buggy, Donal J. published an article.Recommanded Product: 380843-75-4 The title of the article was The effect of lidocaine and bosutinib on 4T1 murine breast cancer cell behaviour In Vitro. And the article contained the following:

Systemic lidocaine has recently emerged as a promising agent possessing numerous potentially anti-neoplastic effects. In vitro studies suggest that lidocaine may prevent metastasis by acting on the tyrosine kinase enzyme Src. I.v. lidocaine has been reported to reduce pulmonary metastasis in vivo in a murine breast cancer model, however the beneficial effect is abolished by the Src inhibitor bosutinib. In this study we examined whether lidocaine and/or bosutinib affects 4TI breast cancer cell activity in vitro and whether any drug interactions similar to that seen in murine models occur. 4TI murine breast cancer cells were exposed to lidocaine and/or bosutinib. Cell viability after / h ofexposure was measured using the 3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (G) assay. Cell migration after 24 h ofexposure was measured using the Oris migration assay. Lidocaine and bosutinib alone or combined inhibited 4TI cell viability and migration, but only at supratherapeutic concentrations Bosutinib did not modulate lidocaine’s effect on viability or migration at any concentration tested. Although lidocaine may inhibit 4T1 metastasis in vivo, a direct effect on 4TI cells is not detectable in vitro at non-toxic concentrations and unlike murine model testing, no unusual interaction with bosutinib was detected. Lidocaine’s anti-metastatic properties are likely to be complex and multifactorial and difficult to replicate outside ofa biol. host. 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 lidocaine bosutinib human murine breast cancer cell behavior, lidocaine, src, bosutinib, cancer, local anesthetics, metastasis, Pharmacology: Drug Metabolism and other aspects.Recommanded Product: 380843-75-4

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

Cohen, Jonathan; Palumbo, Alison; Wing, Jason; Heinrich, Michael C. published an article in 2020, the title of the article was Case series of chronic myeloid leukemia patients who maintained deep molecular response (DMR) with very low-dose ponatinib: experience in discontinuing low-dose ponatinib and treatment-free remission (TFR) outcomes.Reference of 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:

Chronic myeloid leukemia (CML) is a myeloproliferative disease caused by the BCR-ABL1 fusion protein resulting from chromosomal translocation, most classically the 9;22 translocation. Tyrosine kinase inhibitors (TKIs) have been the standard of care since the FDA approval of imatinib in 2001. TKIs used to treat CML include nilotinib, dasatinib, bosutinib, and ponatinib. Using modern TKI-based therapy, the annual mortality and 10-yr survival rates for chronic phase CML are currently 1-2% and 80-90%, resp. Select patients receiving TKI-based therapies that have maintained a deep mol. response (DMR) may discontinue TKI therapy, with trial of treatment-free remission (TFR). This case series supports that TFR may be successfully achieved in patients receiving ponatinib. 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).Reference of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to ponatinib treatment free remission chronic myeloid leukemia mol response, Pharmacology: Drug Metabolism and other aspects.Reference 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

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

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