Tag: 500-600

Vener, Claudia; Banzi, Rita; Ambrogi, Federico; Ferrero, Annalisa; Saglio, Giuseppe; Pravettoni, Gabriella; Sant, Milena published an article in 2020, the title of the article was First-line imatinib vs second- and third-generation TKIs for chronic-phase CML: a systematic review and meta-analysis.Product Details of 380843-75-4 And the article contains the following content:

Meta-anal. of. Imatinib, the first tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia (CML), improves overall survival (OS), but the introduction of newer TKIs requires the definition of the optimal first-line TKI for newly diagnosed Philadelphia chromosome-pos. (Ph+) chronic-phase CML. This systematic review of randomized controlled trials compares the efficacy and safety of imatinib vs second-generation (dasatinib, nilotinib, bosutinib) and third-generation TKIs (ponatinib) in adults with newly diagnosed Ph+ CP CML, concentrating on OS, progression-free survival, and hematol. and nonhematol. adverse events. The quality of the evidence was assessed using the Grading of Recommendations, Assessment, Development and Evaluation method. Two RCTs (imatinib vs nilotinib and imatinib vs dasatinib) found no difference in 5-yr OS or PFS. Second- and third-generation TKIs improved 3-mo major mol. responses (relative risk, 4.28; 95% confidence interval [RR], and other efficacy outcomes, decreased accelerated/blastic-phase transformations, but were associated with more cases of thrombocytopenia cardiovascular events and pancreatic and hepatic effects. GRADE showed that the certainty of the evidence ranged from high to moderate. This study shows that, in comparison with imatinib, second- and third-generation TKIs improve clin. responses, but the safer toxicity profile of imatinib may make it a better option for patients with comorbidities. 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 meta analysis chronic myeloid leukemia tki imatinib dasatinib ponatinib, Placeholder for records without volume info and other aspects.Product Details of 380843-75-4

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Piperazines – an overview | ScienceDirect Topics

Jabbour, Elias; Kantarjian, Hagop published an article in 2020, the title of the article was Chronic myeloid leukemia: 2020 update on diagnosis, therapy and monitoring.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:

A review. Disease overview : Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm with an incidence of 1-2 cases per 100 000 adults. It accounts for approx. 15% of newly diagnosed cases of leukemia in adults. Diagnosis : CML is characterized by a balanced genetic translocation, t(9;22)(q34;q11.2), involving a fusion of the Abelson gene (ABL1) from chromosome 9q34 with the breakpoint cluster region (BCR) gene on chromosome 22q11.2. This rearrangement is known as the Philadelphia chromosome. The mol. consequence of this translocation is the generation of a BCR-ABL1 fusion oncogene, which in turn translates into a BCR-ABL oncoprotein. Frontline therapy : Four tyrosine kinase inhibitors (TKIs), imatinib, nilotinib, dasatinib, and bosutinib are approved by the United States Food and Drug Administration for first-line treatment of newly diagnosed CML in chronic phase (CML-CP). Clin. trials with second generation TKIs reported significantly deeper and faster responses, but they had no impact on survival prolongation, likely because of the existence of highly effective salvage therapies for patients who have a cytogenetic relapse with frontline TKI. Salvage Therapy : For CML post failure on frontline therapy, second-line options include second and third generation TKIs. Although potent and selective, these exhibit unique pharmacol. profiles and response patterns relative to different patient and disease characteristics, such as patients′ comorbidities, disease stage, and BCR-ABL1 mutational status. Patients who develop the T315I “gatekeeper” mutation display resistance to all currently available TKIs except ponatinib. Allogeneic stem cell transplantation remains an important therapeutic option for patients with CML-CP who have failed at least 2 TKIs, and for all patients in advanced phase disease. Even among older patients who have a cytogenetic relapse post failure on all TKIs, they can maintain long-term survival if they continue on a daily most effective/less toxic TKI, with or without the addition of non-TKI anti-CML agents (hydroxyurea, omacetaxine, azacitidine, decitabine, cytarabine, busulfan, others). 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 review imatinib dasatinib anticancer agent chronic myeloid leukemia, Placeholder for records without volume info 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 April 30, 2020, Hochhaus, A.; Baccarani, M.; Silver, R. T.; Schiffer, C.; Apperley, J. F.; Cervantes, F.; Clark, R. E.; Cortes, J. E.; Deininger, M. W.; Guilhot, F.; Hjorth-Hansen, H.; Hughes, T. P.; Janssen, J. J. W. M.; Kantarjian, H. M.; Kim, D. W.; Larson, R. A.; Lipton, J. H.; Mahon, F. X.; Mayer, J.; Nicolini, F.; Niederwieser, D.; Pane, F.; Radich, J. P.; Rea, D.; Richter, J.; Rosti, G.; Rousselot, P.; Saglio, G.; Saussele, S.; Soverini, S.; Steegmann, J. L.; Turkina, A.; Zaritskey, A.; Hehlmann, R. published an article.Name: 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 European LeukemiaNet 2020 recommendations for treating chronic myeloid leukemia. And the article contained the following:

A review. Abstract: The therapeutic landscape of chronic myeloid leukemia (CML) has profoundly changed over the past 7 years. Most patients with chronic phase (CP) now have a normal life expectancy. Another goal is achieving a stable deep mol. response (DMR) and discontinuing medication for treatment-free remission (TFR). The European LeukemiaNet convened an expert panel to critically evaluate and update the evidence to achieve these goals since its previous recommendations. First-line treatment is a tyrosine kinase inhibitor (TKI; imatinib brand or generic, dasatinib, nilotinib, and bosutinib are available first-line). Generic imatinib is the cost-effective initial treatment in CP. Various contraindications and side-effects of all TKIs should be considered. Patient risk status at diagnosis should be assessed with the new EUTOS long-term survival (ELTS)-score. Monitoring of response should be done by quant. polymerase chain reaction whenever possible. A change of treatment is recommended when intolerance cannot be ameliorated or when mol. milestones are not reached. Greater than 10% BCR-ABL1 at 3 mo indicates treatment failure when confirmed. Allogeneic transplantation continues to be a therapeutic option particularly for advanced phase CML. TKI treatment should be withheld during pregnancy. Treatment discontinuation may be considered in patients with durable DMR with the goal of achieving TFR. 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 imatinib dasatinib anticancer agent chronic myeloid leukemia, Placeholder for records without volume info 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 November 1, 2021, Temps, Carolin; Lietha, Daniel; Webb, Emily R.; Li, Xue-Feng; Dawson, John C.; Muir, Morwenna; Macleod, Kenneth G.; Valero, Teresa; Munro, Alison F.; Contreras-Montoya, Rafael; Luque-Ortega, Juan R.; Fraser, Craig; Beetham, Henry; Schoenherr, Christina; Lopalco, Maria; Arends, Mark J.; Frame, Margaret C.; Qian, Bin-Zhi; Brunton, Valerie G.; Carragher, Neil O.; Unciti-Broceta, Asier published an article.Application of 380843-75-4 The title of the article was A conformation selective mode of inhibiting SRC improves drug efficacy and tolerability. And the article contained the following:

Despite the approval of several multikinase inhibitors that target SRC and the overwhelming evidence of the role of SRC in the progression and resistance mechanisms of many solid malignancies, inhibition of its kinase activity has thus far failed to improve patient outcomes. Here we report the small mol. eCF506 locks SRC in its native inactive conformation, thereby inhibiting both enzymic and scaffolding functions that prevent phosphorylation and complex formation with its partner FAK. This mechanism of action resulted in highly potent and selective pathway inhibition in culture and in vivo. Treatment with eCF506 resulted in increased antitumor efficacy and tolerability in syngeneic murine cancer models, demonstrating significant therapeutic advantages over existing SRC/ABL inhibitors. Therefore, this mode of inhibiting SRC could lead to improved treatment of SRC-associated disorders. 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).Application of 380843-75-4

The Article related to breast cancer src conformation lymphocyte ecf506 antiproliferative, Placeholder for records without volume info and other aspects.Application of 380843-75-4

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

On November 25, 2021, Schiffer, Charles A. published an article.Recommanded Product: 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 Asciminib for CML: same target, new arrow. And the article contained the following:

The outlook for patients with chronic phase chronic myelogenous leukemia (CML) has improved dramatically since the development in the late 1990s of oral tyrosine kinase inhibitors (TKIs) targeting the ATP binding site of the BCR-ABL1 oncoprotein. Here, the authors address the management of patients in chronic phase previously treated with ≥ 2 TKIs in a randomized trial comparing asciminib and bosutinib, which is approved for use in this patient population. Ascinimib (previously known as ABL001) is a small mol. which binds to the myristoyl pocket located at a different site on the BCR-ABL1 protein, producing a conformational change that inhibits downstream signaling. 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: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to asciminib bosutinib anticancer agent chronic myelogenous leukemia, Placeholder for records without volume info and other aspects.Recommanded Product: 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

Fu, Yuna; Wang, Jianhua; Wang, Yan; Sun, Heng published an article in 2022, the title of the article was Investigating the Effect of Tyrosine Kinase Inhibitors on the Interaction between Human Serum Albumin by Atomic Force Microscopy.Category: piperazines And the article contains the following content:

It is important for elucidating the regulation mechanism of life activities, as well as for the prevention, diagnosis, and drug design of diseases, to study protein-protein interactions (PPIs). Here, we investigated the interactions of human serum albumin (HSA) in the presence of tyrosine kinase inhibitors (TKIs: imatinib, nilotinib, dasatinib, bosutinib, and ponatinib) using at. force microscopy (AFM). The distribution of rupture events including the specific interaction force Fi and the non-specific interaction force F0 between HSA pairs was analyzed. Based on the force measurements, Fi and F0 between HSA pairs in the control experiment were calculated to be 47 ± 1.5 and 116.1 ± 1.3 pN. However, Fi was significantly decreased in TKIs, while F0 was slightly decreased. By measuring the rupture forces at various loading rates and according to the Bell equation, the kinetic parameters of the complexes were investigated in greater detail. Mol. docking was used as a complementary means by which to explore the force of this effect. The whole measurements indicated that TKIs influenced PPIs in a variety of ways, among which hydrogen bonding and hydrophobic interactions were the most important. In conclusion, these outcomes give us a better insight into the mechanisms of PPIs when there are exogenous compounds present as well as in different liquid environments. 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).Category: piperazines

The Article related to tyrosine kinase inhibitor serum albumin atomic force microscopy, atomic force microscopy, human serum albumin, protein–protein interactions, tyrosine kinase inhibitors, Placeholder for records without volume info and other aspects.Category: piperazines

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

Kazim, Noor; Yen, Andrew published an article in 2021, the title of the article was Evidence of off-target effects of bosutinib that promote retinoic acid-induced differentiation of non-APL AML cells.Safety 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:

In the present study, we determined the effects of the Src family kinase (SFK) inhibitor, Bosutinib, and the engineered loss of the Lyn SFK on all-trans retinoic acid-induced leukemic cell differentiation. Retinoic acid (RA) is an embryonic morphogen and dietary factor that demonstrates chemotherapeutic efficacy in inducing differentiation of a non-APL AML cell model, the HL-60 human myeloblastic (FAB-M2) leukemia cell line, via activation of a novel signalsome containing an ensemble of signaling mols. that drive differentiation. Bosutinib is an inhibitor of SFKs used to treat myeloid leukemias where prominent high expression of SFKs, in particular Lyn, has been observed Using either Bosutinib or loss of Lyn expression due to shRNA promoted RA-induced phenotypic differentiation, G0 arrest, and respiratory burst (functional differentiation) of HL-60 cells. Signaling events putatively seminal to RA-induced differentiation, the expression of Fgr, Cbl, Slp-76 and Vav, and the phosphorylation of c-Raf (pS259), Vav (p-tyr), and Slp76 (p-tyr) were not inhibited by Bosutinib or loss of Lyn. Nor was RA-induced upregulation of p-tyr phosphorylation of p47phox, a member of the NADPH complex that produces ROS, a putative phosphorylation dependent signaling regulator. Surprisingly, Bosutinib still works in the absence of Lyn to enhance RA-induced differentiation and neither compromised RA-induced expression, nor phosphorylation of signaling mols. that drive differentiation. These findings suggested there is a novel, off-target, Lyn-independent effect of Bosutinib that is of therapeutic significance to differentiation 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).Safety of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to bosutinib retinoic acid phosphorylation, acute myeloid leukemia (aml), lyn, bosutinib, cell differentiation, retinoic acid (ra), src family kinase (sfk) inhibitor, Placeholder for records without volume info and other aspects.Safety 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 December 31, 2021, Smith, Stephanie M.; Sabnis, Himalee S.; Lewis, Rebecca Williamson; Effinger, Karen E.; Bergsagel, John; Patterson, Briana; Mertens, Ann; Sakamoto, Kathleen M.; Schapira, Lidia; Castellino, Sharon M. published an article.SDS of cas: 380843-75-4 The title of the article was Patterns of surveillance for late effects of BCR-ABL tyrosine kinase inhibitors in survivors of pediatric Philadelphia chromosome positive leukemias. And the article contained the following:

Targeted anticancer therapies such as BCR-ABL tyrosine kinase inhibitors (TKIs) have improved outcomes for chronic myeloid leukemia (CML) and Philadelphia chromosome-pos. acute lymphoblastic leukemia (Ph + ALL). However, little is known about long-term risks of TKIs in children. Exposure-based survivorship guidelines do not include TKIs, thus surveillance practices may be variable. We retrospectively examined surveillance for cardiac and endocrine late effects in children receiving TKIs for Ph + leukemias, diagnosed at < 21 years between 2000 and 2018. Frequency of echocardiogram (ECHO), ECG (ECG), TSH (TSH), dual-energy x-ray absorptiometry (DXA), and bone age testing were abstracted. Descriptive statistics were stratified by leukemia type. 66 Patients (CML n = 44; Ph + ALL n = 22) met inclusion criteria. Among patients with CML, ≥1 evaluation was done: ECHO (50.0%), ECG (48.8%), TSH (43.9%), DXA (2.6%), bone age (7.4%). Among patients with Ph + ALL, ≥1 evaluation was done: ECHO (86.4%), ECG (68.2%), TSH (59.1%), DXA (63.6%), bone age (44.4%). Over a median 6.3 and 5.7 years of observation, resp., 2% of patients with CML and 57% with Ph + ALL attended a survivorship clinic. Despite common exposure to TKIs in survivors of Ph + leukemias, patterns of surveillance for late effects differed in CML and Ph + ALL, with the latter receiving more surveillance likely due to concomitant chemotherapy exposures. Targeted therapies such as TKIs are revolutionizing cancer treatment, but surveillance for late effects and referral to survivorship clinics are variable despite the chronicity of exposure. Evidence based guidelines and longer follow-up are needed. 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 tyrosine kinase inhibitor pediatric philadelphia chromosome leukemia, bcr-abl leukemia, cml, late-effects, ph + all, surveillance, tyrosine kinase inhibitors, Placeholder for records without volume info and other aspects.SDS of cas: 380843-75-4

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

On February 29, 2020, Okano, Hideyuki; Yasuda, Daisuke; Fujimori, Koki; Morimoto, Satoru; Takahashi, Shinichi 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 Ropinirole, a New ALS Drug Candidate Developed Using iPSCs. And the article contained the following:

A review. Induced pluripotent stem cells (iPSCs) are increasingly used in the study of disease mechanisms and the development of effective disease-modifying therapies for neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS). Recently, three candidate anti-ALS drugs-ropinirole (ROPI), retigabine, and bosutinib-have been identified in iPSC-based drug screens and are now being evaluated in clin. trials for safety and effectiveness. We review the preclin. data, clin. research design, and rationale for ROPI as an anti-ALS drug candidate compared with those of the other two drugs. We also discuss the use of iPSCs for understanding and monitoring treatment response as well as for new insights into the development of new drugs and therapeutic interventions for major neurodegenerative diseases. 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 ropinirole als drug candidate ipscs review, amyotrophic lateral sclerosis, disease modeling, drug repositioning, induced pluripotent stem cells, ropinirole, Placeholder for records without volume info 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

Saussele, Susanne; Kohlbrenner, Katharina; Vogelmann, Tobias; Schubert, Tino published an article in 2022, the title of the article was Incidence, Prevalence, and Real-World Treatment Patterns in Chronic Myeloid Leukemia: Results from a Population-Representative German Claims Data Analysis.COA of Formula: C26H29Cl2N5O3 And the article contains the following content:

Real-world data on usage of 1st-, 2nd-, and 3rd-generation tyrosine kinase inhibitor (TKI) in chronic myeloid leukemia (CML) are scarce. This study therefore aimed to analyze the use of different TKIs used in 1st- and 2nd-line treatment and the frequency of TKI switches in CML. This observational study was based on the InGef research database, an anonymized representative claims dataset in Germany (n = 4 million). An incidence and prevalence patient CML cohort was followed for 5 and 3 years. Analyses regarding incidence, prevalence, and therapy distribution were performed descriptively. 151 Patients were included in the incidence and 636 patients in the prevalence cohort. This resulted in an incidence of 1.8 (95% confidence interval [CI]: 1.34-2.20) and a prevalence of 14.9 (95% CI: 13.70-16.03) per 100,000 inhabitants. For the incidence cohort, data on 1st-line therapy were available for 124 patients and distributed across imatinib (N = 52), nilotinib (N = 44), dasatinib (N = 12), chemotherapies as hydroxycarbamide (N = 11), and ponatinib/bosutinib (N = 5). Twenty-six percent of patients switched TKI therapy at least once in 3 years. In the prevalence cohort, 423 patients (66.5%) had claims on existing or newly emerged cardiovascular diseases (CDs). No significant differences (p = 0.32) between TKIs in patients with CD were found. Every fourth patient switched TKI therapy within the first 3 years after treatment initiation. Switches were more likely when hints of disease progression or intolerability were observable in the database. 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 human disease progression chronic myeloid leukemia, chronic myeloid leukemia, chronic myeloid leukemia, claims data analysis, real-world evidence, tki, Placeholder for records without volume info and other aspects.COA of Formula: C26H29Cl2N5O3

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