Category: 763111-47-3

Chemistry is traditionally divided into organic and inorganic chemistry. COA of Formula: C20H19FN4O2, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 763111-47-3

Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule

Poly (ADP-ribose) polymerase-1 (PARP1) is a major member of the PARP superfamily that is involved in DNA damage signalling and other important cellular processes. Here we report the development of a small molecule targeting PARP1 based on the PROTAC strategy. In the MDA-MB-231 cell line, the representative compound 3 can induce significant PARP1 cleavage and programmed cell death.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N834 – PubChem

Related Products of 763111-47-3, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 763111-47-3, 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, introducing its new discovery.

PHTHALAZINONE DERIVATIVE

4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 763111-47-3. In my other articles, you can also check out more blogs about 763111-47-3

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N807 – PubChem

763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, belongs to phthalazine compound, is a common compound. Computed Properties of C20H19FN4O2In an article, once mentioned the new application about 763111-47-3.

SILANOL BASED THERAPEUTIC PAYLOADS

Described herein in part are silanol based therapeutic payloads comprising a silanol terminus, a divalent spacer moiety, and a drug moiety capable of effecting a target cell or tissue.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N816 – PubChem

Synthetic Route of 763111-47-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, molecular formula is C20H19FN4O2. In a Patent£¬once mentioned of 763111-47-3

A method for preparing aurar handkerchief Nepal (by machine translation)

The invention discloses a method for preparing aurar handkerchief Nepal, comprising the following steps: 4 – (4-fluoro-3 – (piperazine-1-carbonyl) benzyl) naphthyridin -1 (2-hydrogen)-ketone, condensation agent, cyclopropanecarboxylic acid, alkali in a polar organic solvent in, for 0 C -120 C reaction 2-8 hours later, by adding water, precipitated solid, filtering, washing, drying, obtain aurar handkerchief Nepal. This invention adopts the cyclopropanecarboxylic formic acid as the raw material, mild reaction conditions, safety of operation is good, and there is no need to adopt the dichloromethane, the organic solvent, separating the purification step is simple and convenient, the high-yield preparation aurar handkerchief Nepal, the highest can reach 92% the above-mentioned; at the same time, the raw materials of this invention is easy to obtain, the method is simple and convenient, less side reactions, chromatographic purity of the product is high, it is easy to realize industrial production, it has good industrial application prospects. (by machine translation)

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 763111-47-3

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N806 – PubChem

Related Products of 763111-47-3, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 763111-47-3, 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, introducing its new discovery.

Compositions And Methods For In Vivo Imaging

This document relates to compounds useful for targeting PARP1. Also provided herein are methods for using such compounds to detect and image cancer cells.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 763111-47-3. In my other articles, you can also check out more blogs about 763111-47-3

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N810 – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one. Introducing a new discovery about 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

PARP-1-targeted radiotherapy in mouse models of glioblastoma

The DNA repair enzyme poly(ADP-ribose) polymerase 1 (PARP-1) is overexpressed in glioblastoma, with overall low expression in healthy brain tissue. Paired with the availability of specific small molecule inhibitors, PARP-1 is a near-ideal target to develop novel radiotherapeutics to induce DNA damage and apoptosis in cancer cells, while sparing healthy brain tissue. Methods: We synthesized an 131I-labeled PARP-1 therapeutic and investigated its pharmacology in vitro and in vivo. A subcutaneous tumor model was used to quantify retention times and therapeutic efficacy. A potential clinical scenario, intratumoral convection-enhanced delivery, was mimicked using an orthotopic glioblastoma model combined with an implanted osmotic pump system to study local administration of 131I-PARPi (PARPi is PARP inhibitor). Results: 131IPARPi is a 1(2H)-phthalazinone, similar in structure to the Food and Drug Administration-approved PARP inhibitor AZD-2281. In vitro studies have shown that 131I-PARPi and AZD-2281 share similar pharmacologic profiles. 131I-PARPi delivered 134.1 cGy/ MBq intratumoral injected activity. Doses to nontarget tissues, including liver and kidney, were significantly lower. Radiation damage and cell death in treated tumors were shown by p53 activation in U87-MG cells transfected with a p53-bioluminescent reporter. Treated mice showed significantly longer survival than mice receiving vehicle (29 vs. 22 d, P , 0.005) in a subcutaneous model. Convection-enhanced delivery demonstrated efficient retention of 131I-PARPi in orthotopic brain tumors, while quickly clearing from healthy brain tissue. Conclusion: Our results demonstrate 131IPARPi’s high potential as a therapeutic and highlight PARP’s relevance as a target for radionuclide therapy. Radiation plays an integral role in brain tumor therapy, and radiolabeled PARP therapeutics could ultimately lead to improvements in the standard of care.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, you can also check out more blogs about763111-47-3

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N821 – PubChem

763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, belongs to phthalazine compound, is a common compound. Computed Properties of C20H19FN4O2In an article, once mentioned the new application about 763111-47-3.

Synthesis and evaluation of a radioiodinated tracer with specificity for poly(ADP-ribose) polymerase-1 (PARP-1) in vivo

Interest in nuclear imaging of poly(ADP-ribose) polymerase-1 (PARP-1) has grown in recent years due to the ability of PARP-1 to act as a biomarker for glioblastoma and increased clinical use of PARP-1 inhibitors. This study reports the identification of a lead iodinated analog 5 of the clinical PARP-1 inhibitor olaparib as a potential single-photon emission computed tomography (SPECT) imaging agent. Compound 5 was shown to be a potent PARP-1 inhibitor in cell-free and cellular assays, and it exhibited mouse plasma stability but approximately 3-fold greater intrinsic clearance when compared to olaparib. An 123I-labeled version of 5 was generated using solid state halogen exchange methodology. Ex vivo biodistribution studies of [123I]5 in mice bearing subcutaneous glioblastoma xenografts revealed that the tracer had the ability to be retained in tumor tissue and bind to PARP-1 with specificity. These findings support further investigations of [123I]5 as a noninvasive PARP-1 SPECT imaging agent.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N836 – PubChem

Reference of 763111-47-3, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, molecular formula is C20H19FN4O2. In a Patent£¬once mentioned of 763111-47-3

A phthalazinone hydroxamic acid derivatives and its preparation method and application (by machine translation)

The invention discloses a has a plurality of poly adenosine diphosphate ribose polymerase (PARP) and/or histone deacetylase (HDAC) inhibitory activity of taitai qin alkone different hydroxy wo acid compounds and preparation method and application thereof. The taitai qin alkone different hydroxy wo acid compounds of the formula I as shown in the structural formula, wherein R1 Is a hydrogen atom or a halogen; R2 Is a hydrogen atom or a halogen; Y is an oxygen atom, methylene or fluorine substituted methylene; Z is or G bond is a chemical bond, methylene, fluoro methylene or double bond. In vitro cell proliferation experiment shows that, as shown in formula I compound well inhibit a variety of tumor cell proliferation. Poly adenosine diphosphate ribose polymerase (PARP) and histone deacetylase (HDAC) inhibition experiment I indicates the type compound is shown to poly adenosine diphosphate ribose polymerase (PARP) and/or histone deacetylase (HDAC) have good inhibitory activity of the compound. (by machine translation)

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Reference of 763111-47-3. In my other articles, you can also check out more blogs about 763111-47-3

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N805 – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one. Introducing a new discovery about 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl] -2H-phthalazin-1-one: A novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1

Poly(ADP-ribose) polymerase activation is an immediate cellular response to metabolic-, chemical-, or ionizing radiation-induced DNA damage and represents a new target for cancer therapy. In this article, we disclose a novel series of substituted 4-benzyl-2H-phthalazin-1-ones that possess high inhibitory enzyme and cellular potency for both PARP-1 and PARP-2. Optimized compounds from the series also demonstrate good pharmacokinetic profiles, oral bioavailability, and activity in vivo in an SW620 colorectal cancer xenograft model. 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl] -2H-phthalazin-1-one (KU-0059436, AZD2281) 47 is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Compound 47 is currently undergoing clinical development for the treatment of BRCA1- and BRCA2-defective cancers.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, you can also check out more blogs about763111-47-3

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N824 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, molecular formula is C20H19FN4O2

Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells

We report the antitumor effects of nitric oxide (NO) releasing derivatives of the PARP-1 inhibitor olaparib (1). Compound 5b was prepared by coupling the carboxyl group of 3b and the free amino group of arylated diazeniumdiolated piperazine 4. Analogue 5a has the same structure except that the F is replaced by H. Compound 13 is the same as 5b except that a Me2N-N(O)=NO- group was added para and ortho to the nitro groups of the dinitrophenyl ring. The resulting prodrugs are activated by glutathione in a reaction accelerated by glutathione S-transferase P1 (GSTP1), an enzyme frequently overexpressed in cancers. This metabolism generates NO plus a PARP-1 inhibitor simultaneously, consuming reducing equivalents, leading to DNA damage concomitant with inhibition of DNA repair, and in the case of 13 inducing cross-linking glutathionylation of proteins. Compounds 5b and 13 reduced the growth rates of A549 human lung adenocarcinoma xenografts with no evidence of systemic toxicity.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 763111-47-3, in my other articles.

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N823 – PubChem