Jouan, Elodie et al. published their research in European Journal of Drug Metabolism and Pharmacokinetics in 2021 | CAS: 1211441-98-3

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Product Details of 1211441-98-3

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors was written by Jouan, Elodie;Moreau, Amelie;Bruyere, Arnaud;Alim, Karima;Denizot, Claire;Parmentier, Yannick;Fardel, Olivier. And the article was included in European Journal of Drug Metabolism and Pharmacokinetics in 2021.Product Details of 1211441-98-3 This article mentions the following:

Equilibrative nucleoside transporter (ENT) 1 is a widely-expressed drug transporter, handling nucleoside analogs as well as endogenous nucleosides. ENT1 has been postulated to be inhibited by some marketed tyrosine kinase inhibitors (TKIs). To obtain insights into this point, the interactions of 24 TKIs with ENT1 activity have been analyzed. Inhibition of ENT1 activity was investigated in vitro through quantifying the decrease of [3H]-uridine uptake caused by TKIs in HAP1 ENT2-knockout cells, exhibiting selective ENT1 expression. TKI effects towards ENT1-mediated transport were addnl. characterized in terms of their in vivo relevance and of their relationship to TKI mol. descriptors. Putative transport of the TKI lorlatinib by ENT1/ENT2 was analyzed by LC-MS/MS. Of 24 TKIs, 12 of them, each used at 10μM, were found to behave as moderate or strong inhibitors of ENT1, i.e., they decreased ENT1 activity by at least 35%. This inhibition was concentration-dependent for at least the strongest ones (IC50 less than 10μM) and was correlated with some mol. descriptors, especially with atom-type E-state indexes. Lorlatinib was notably a potent in vitro inhibitor of ENT1/ENT2 (IC50 values around 1.0-2.5μM) and was predicted to inhibit these nucleoside transporters at relevant clin. concentrations, without, however, being a substrate for them. Our data unambiguously add ENT1 to the list of drug transporters inhibited by TKIs, especially by lorlatinib. This point likely merits attention in terms of possible drug-drug interactions, notably for nucleoside analogs, whose ENT1-mediated uptake into their target cells may be hampered by co-administrated TKIs such as lorlatinib. In the experiment, the researchers used many compounds, for example, 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3Product Details of 1211441-98-3).

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Product Details of 1211441-98-3

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

 

Amigo, Morgan et al. published their research in Journal of the American Academy of Dermatology in 2022 | CAS: 571190-30-2

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C24H29N7O2

Presentation and management of diverse cutaneous reactions after cyclin-dependent kinase 4/6 inhibitor use was written by Amigo, Morgan;Hoffman, Kalyn;Chung, Catherine;Lustberg, Maryam;Wesolowski, Robert;VanDeusen, Jeffrey;Stover, Daniel;Suarez, Gabriel Tinoco;Cherian, Mathew;Kaffenberger, Benjamin;Dulmage, Brittany. And the article was included in Journal of the American Academy of Dermatology in 2022.Synthetic Route of C24H29N7O2 This article mentions the following:

It discusses on presentation and management of diverse cutaneous reactions after cyclin-dependent kinase 4/6 inhibitor use. Inpatient data from 2016-2020 was used to identify 9 patients with hormone receptor breast cancer and patient with liposarcoma who had received treatment with CDK 4/6i and experienced the development of cutaneous reactions. Palbociclib was the initial CDK4/6i used in 9 of the 10 cases and abemaciclib the initial agent in. The average time between drug initiation and the report of a cutaneous reaction was 6.8 mo, with a range of 21 days to 13 mo. The morphol. of the reactions included morbilliform eruptions with mucosal erosions, inflamed actinic keratoses (AKs), psoriasiform dermatitis with or without pustulosis, pustular dermatoses, and palmoplantar dermatitis. The agents used to treat these adverse cutaneous reactions represent commonly prescribed therapeutics in the field of dermatol., except for methylprednisolone, and have low adverse effect profiles. Understanding the potential morphol. and distribution of CDK4/6i-induced cutaneous reactions allows for faster recognition, accurate diagnosis, and appropriate therapeutic management to continue oncol. therapies, leading to more favorable outcomes. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2Synthetic Route of C24H29N7O2).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C24H29N7O2

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

 

Kodama, Susumu et al. published their research in Journal of Toxicological Sciences in 2021 | CAS: 2192-20-3

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.HPLC of Formula: 2192-20-3

Association between in vitro nuclear receptor-activating profiles of chemical compounds and their in vivo hepatotoxicity in rats was written by Kodama, Susumu;Yoshii, Nao;Ota, Akihiro;Takeshita, Jun-ichi;Yoshinari, Kouichi;Ono, Atsushi. And the article was included in Journal of Toxicological Sciences in 2021.HPLC of Formula: 2192-20-3 This article mentions the following:

The liver plays critical roles to maintain homeostasis of living organisms and is also a major target organ of chem. toxicity. Meanwhile, nuclear receptors (NRs) are known to regulate major liver functions and also as a critical target for hepatotoxic compounds In this study, we established mammalian one-hybrid assay systems for five rat-derived NRs, namely PXR, PPARα, LXRα, FXR and RXRα, and evaluated a total of 326 compounds for their NR-activating profiles. Then, we assessed the association between their NR-activating profile and hepatotoxic endpoints in repeated-dose toxicity data of male rats from Hazard Evaluation Support System. In the in vitro cell-based assays, 68, 38, 20, 17 and 17 compounds were identified as positives for PXR, PPARα, LXRα, FXR and RXRα, resp. The association analyses demonstrated that the PXR-pos. compounds showed high frequency of endpoints related to liver hypertrophy, such as centrilobular hepatocellular hypertrophy, suggesting that PXR activation is involved in chem.-induced liver hypertrophy in rats. It is intriguing to note that the PXR-pos. compounds also showed statistically significant associations with both prolonged activated partial thromboplastin time and prolonged prothrombin time, suggesting a possible involvement of PXR in the regulation of blood clotting factors. Collectively, our approach may be useful for discovering new functions of NRs as well as understanding the complex mechanism for hepatotoxicity caused by chem. compounds In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3HPLC of Formula: 2192-20-3).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.HPLC of Formula: 2192-20-3

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

 

Lasut-Szyszka, Barbara et al. published their research in International Journal of Molecular Sciences in 2021 | CAS: 548472-68-0

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.SDS of cas: 548472-68-0

Transcriptome Analysis of Cells Exposed to Actinomycin D and Nutlin-3a Reveals New Candidate p53-Target Genes and Indicates That CHIR-98014 Is an Important Inhibitor of p53 Activity was written by Lasut-Szyszka, Barbara;Malachowska, Beata;Gdowicz-Klosok, Agnieszka;Krzesniak, Malgorzata;Glowala-Kosinska, Magdalena;Zajkowicz, Artur;Rusin, Marek. And the article was included in International Journal of Molecular Sciences in 2021.SDS of cas: 548472-68-0 This article mentions the following:

Co-treatment with actinomycin D and nutlin-3a (A + N) strongly activates p53. Previously we reported that CHIR-98014 (GSK-3 kinase inhibitor), acting in cells exposed to A + N, prevents activation of TREM2-an innate immunity and p53-regulated gene associated with Alzheimer′s disease. In order to find novel candidate p53-target genes and genes regulated by CHIR-98014, we performed RNA-Seq of control A549 cells and the cells exposed to A + N, A + N with CHIR-98014 or to CHIR-98014. We validated the data for selected genes using RT-PCR and/or Western blotting. Using CRISPR/Cas9 technol. we generated p53-deficient cells. These tools enabled us to identify dozens of candidate p53-regulated genes. We confirmed that p53 participates in upregulation of BLNK, APOE and IRF1. BLNK assists in activation of immune cells, APOE codes for apolipoprotein associated with Alzheimer′s disease and IRF1 is activated by interferon gamma and regulates expression of antiviral genes. CHIR-98014 prevented or inhibited the upregulation of a fraction of genes stimulated by A + N. Downregulation of GSK-3 did not mimic the activity of CHIR-98014. Our data generate the hypothesis, that an unidentified kinase inhibited by CHIR-98014, participates in modification of p53 and enables it to activate a subset of its target genes, e.g., the ones associated with innate immunity. In the experiment, the researchers used many compounds, for example, 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0SDS of cas: 548472-68-0).

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.SDS of cas: 548472-68-0

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

 

Laszlovszky, Istvan et al. published their research in Neuropsychopharmacologia Hungarica : a Magyar Pszichofarmakologiai Egyesulet lapja in 2019 | CAS: 839712-12-8

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Recommanded Product: 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea

[Cariprazine, a new type – dopamine D₃ receptor preferring – partial agonist atypical antipsychotic for the treatment of schizophrenia and the primary negative symptoms]. was written by Laszlovszky, Istvan;Kiss, Bela;Barabassy, Agota;Kapas, Margit;Nemeth, Gyorgy. And the article was included in Neuropsychopharmacologia Hungarica : a Magyar Pszichofarmakologiai Egyesulet lapja in 2019.Recommanded Product: 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea This article mentions the following:

Dopamine D₂ receptor partial agonists represent a new generation of atypical antipsychotics. Cariprazine, which has received centralized market authorization from the European Medicines Agency in 2017 for the treatment of adult patients with schizophrenia (including those with predominant negative symptoms of schizophrenia) differs from the other two partial agonist antipsychotics aripiprazole and brexpiprazole due to its unique features. Cariprazine is a dopamine D₃ preferring D₃/D₂ partial agonist with very similar dopamine receptor subtype selectivity as dopamine. It has proven efficacy in the treatment of positive and negative symptoms of schizophrenia, as well as for relapse prevention. Further phase-3 clinical studies proved the efficacy of cariprazine in the acute treatment of manic or mixed episodes associated with bipolar I disorder, as well as in bipolar depression. For the adjunctive treatment of major depressive disorder, phase 3 studies are in progress. In the experiment, the researchers used many compounds, for example, 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8Recommanded Product: 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Recommanded Product: 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea

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

 

Verschaeve, L. et al. published their research in Environmental and Molecular Mutagenesis in 1999 | CAS: 74852-62-3

4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Reference of 74852-62-3

VITOTOX bacterial genotoxicity and toxicity test for the rapid screening of chemicals was written by Verschaeve, L.;Van Gompel, J.;Thilemans, L.;Regniers, L.;Vanparys, P.;Van der Lelie, D.. And the article was included in Environmental and Molecular Mutagenesis in 1999.Reference of 74852-62-3 This article mentions the following:

The VITOTOX test is a new bacterial genotoxicity test that was previously shown to be very rapid and sensitive. Initially only one Salmonella typhimurium strain (TA104 recN2-4) was used in the test. In this paper the authors introduce a second strain (TA104pr1) that can be used as an internal control to further enhance the reliability of the test. The authors demonstrate the usefulness of this pr1 strain in genotoxicity and toxicity testing. The authors also report on the results of a study where the VITOTOX test was performed on newly synthesized pharmaceutical compounds, or intermediate products in the synthesis of drug candidates. The authors demonstrate that the test gives identical results when performed independently in two different laboratories and that it correlates well with either the Ames test or SOS chromotest. In the experiment, the researchers used many compounds, for example, 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3Reference of 74852-62-3).

4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline (cas: 74852-62-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Reference of 74852-62-3

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

 

Tang, Lloyd Wei Tat et al. published their research in Drug Metabolism & Disposition in 2022 | CAS: 872511-34-7

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Formula: C26H31Cl2N7O3

Metabolic activation of the acrylamide michael acceptor warhead in futibatinib to an epoxide intermediate engenders covalent inactivation of CYP3A was written by Tang, Lloyd Wei Tat;Fu, Jiaxin;Koh, Siew Kwan;Wu, Guoyi;Zhou, Lei;Chan, Eric Chun Yong. And the article was included in Drug Metabolism & Disposition in 2022.Formula: C26H31Cl2N7O3 This article mentions the following:

Futibatinib (FUT) is a potent inhibitor of fibroblast growth factor receptor (FGFR) 1-4 that is currently under clin. investigation for intrahepatic cholangiocarcinoma. Unlike its predecessors, FUT possesses an acrylamide warhead, which enables it to bind covalently to a free cysteine residue in the FGFR kinase domain. However, it remains uninterrogated if this electrophilic α,β-unsaturated carbonyl scaffold could also directly or indirectly engender offtarget covalent binding to nucleophilic centers on other cellular proteins. Here, we discovered that FUT inactivated both CYP3A isoforms with inactivator concentration at half-maximum inactivation rate constant, maximum inactivation rate constant, and partition ratios of 12.5 and 51.4 μM, 0.25 and 0.06 min-1, and ~52 and ~58 for CYP3A4 and CYP3A5, resp. Along with its time-, concentration-, and cofactor-dependent inhibitory profiles, FUT also exhibited several cardinal features that were consistent with mechanism-based inactivation. Moreover, the nature of inactivation was unlikely to be pseudo-irreversible and instead arose from the covalent modification of the cytochrome P 450 apoprotein and/or its heme moiety due to the lack of substantial enzyme activity recovery following dialysis and chem. oxidation, as well as the absence of the diagnostic Soret peak in spectral analyses. Finally, utilizing glutathione (GSH) trapping and high-resolution mass spectrometry, we illuminated that while the acrylamide moiety in FUT could nonenzymically conjugate to GSH via Michael addition, it was not implicated in the covalent inactivation of CYP3A. Rather, we surmised that it likely stemmed from the metabolic activation of its acrylamide covalent warhead to a highly electrophilic epoxide intermediate that could covalently modify CYP3A and culminate in its catalytic inactivation. SIGNIFICANCE STATEMENT In this study, we reported for the first time the inactivation of CYP3A by futibatinib (FUT). Furthermore, using FUT as an exemplary targeted covalent inhibitor, our study revealed the propensity for its acrylamide Michael acceptor moiety to be metabolically activated to a highly electrophilic epoxide. Due to the growing resurgence of covalent inhibitors and the well-established toxicol. ramifications associated with epoxides, we advocate that closer scrutiny be adopted when profiling the reactive metabolites of compounds possessing an α,β-unsaturated carbonyl scaffold. In the experiment, the researchers used many compounds, for example, 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7Formula: C26H31Cl2N7O3).

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Formula: C26H31Cl2N7O3

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

 

Park, Song Yi et al. published their research in Breast Cancer Research and Treatment in 2022 | CAS: 571190-30-2

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Reference of 571190-30-2

Prognostic role of tumor subtype and germline BRCA mutation in advanced breast cancer patients treated with palbociclib plus endocrine therapy was written by Park, Song Yi;Suh, Koung Jin;Lee, Dae-Won;Ryu, Han Suk;Kim, Miso;Kim, Se Hyun;Lee, Kyung-Hun;Kim, Tae-Yong;Kim, Jee Hyun;Park, In Ae;Im, Seock-Ah. And the article was included in Breast Cancer Research and Treatment in 2022.Reference of 571190-30-2 This article mentions the following:

Abstract: Purpose: Palbociclib is a cyclin-dependent kinase 4 and 6 inhibitor which shows promising effect in hormone receptor-pos. breast cancer. The purpose of this study is to evaluate the real-world efficacy and toxicity of palbociclib plus endocrine therapy. Methods: This is a retrospective study performed in two tertiary referral hospitals in Korea. Advanced breast cancer patients who were treated with 1st-line palbociclib plus endocrine therapy were enrolled. Results: A total of 216 patients were included between August 2016 and May 2019. Median age was 56 (29-89) years old and 75 patients (34.7%) were premenopausal. Median progression-free survival (PFS) was 33.0 mo [95% confidence interval (CI) 24.7 to 41.3] and objective response rate was 59.3%. Luminal B patients had shorter PFS (33.0 mo vs. Not reached, p = 0.019) and tendency of lower ORR (58.3 vs. 62.0%, p = 0.19) compared to luminal A patients. Multivariate anal. revealed luminal B (adjusted hazard ratio 1.90, p = 0.038) and germline BRCA mutation (adjusted hazard ratio 5.57, p = 0.002) as an independent poor prognostic factor for PFS. The most common grade 3 or 4 adverse event was neutropenia (86.7%). Conclusion: The efficacy and toxicity of palbociclib in the real world were comparable to those of clin. trials. In addition, palbociclib with endocrine therapy was an effective treatment option for young patients. Luminal B and germline BRCA mutation were associated with inferior outcome. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2Reference of 571190-30-2).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Reference of 571190-30-2

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

 

Han, Bo et al. published their research in FEBS Open Bio in 2020 | CAS: 548472-68-0

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Electric Literature of C30H30Cl2N4O4

Combined use of irinotecan and p53 activator enhances growth inhibition of mesothelioma cells was written by Han, Bo;Lee-Okada, Hyeon-Cheol;Ishimine, Momoko;Orita, Hajime;Nishikawa, Keiko;Takagaki, Tetsuya;Kajino, Kazunori;Yokomizo, Takehiko;Hino, Okio;Kobayashi, Toshiyuki. And the article was included in FEBS Open Bio in 2020.Electric Literature of C30H30Cl2N4O4 This article mentions the following:

Malignant mesothelioma (MM) is an aggressive malignant neoplasm which rapidly invades pleural tissues and has a poor prognosis. Here, we explore enhancement of the effect of irinotecan [camptothecin-11 (CPT-11)] by the p53-dependent induction of carboxylesterase 2 (CES2), a CPT-11-activating enzyme, in MM. The level of CES2 mRNA was greatly increased on treatment with nutlin-3a. A combination of CPT-11 and nutlin-3a inhibited the growth of MM cells more effectively than either drug alone. Knocking down CES2 in MM cells reduced the effect of the drug combination, and its forced expression in MESO4 cells enhanced the growth inhibitory activity of CPT-11 in the absence of nutlin-3a. Enhancement of the growth inhibitory activity of CPT-11 by nutlin-3a suggests a possible new combinatorial MM chemotherapy regimen. In the experiment, the researchers used many compounds, for example, 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0Electric Literature of C30H30Cl2N4O4).

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Electric Literature of C30H30Cl2N4O4

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

 

Tkaczynski, Tadeusz et al. published their research in Acta Poloniae Pharmaceutica in 1958 | CAS: 142-64-3

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.COA of Formula: C4H12Cl2N2

Synthesis of ethyleneamines. III. Pyrolysis of N,N’-bis(2-hydroxyethyl)ethylenediamine hydrochloride was written by Tkaczynski, Tadeusz. And the article was included in Acta Poloniae Pharmaceutica in 1958.COA of Formula: C4H12Cl2N2 This article mentions the following:

N,N’-Bis(2-hydroxyethyl)ethylenediamine – HCl heated 2.5 hrs. at 260° yielded piperazine-HCl (I). A similar process carried out at 200° gave I and N-piperazineëthanol-HCl (II). II on similar heating at 260° was converted into I. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3COA of Formula: C4H12Cl2N2).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.COA of Formula: C4H12Cl2N2

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