Category: 2359-60-6

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Discovery of N-aryl-N?-pyrimidin-4-yl ureas as irreversible L858R/T790M mutant selective epidermal growth factor receptor inhibitors

A novel series of N-aryl-N?-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the EGFR L858R/T790M. The most representative compound 28 showed high activity against EGFR L858R/T790M kinase (IC50 = 4 nM) and 22-fold selectivity against wild type EGFR. Moreover, compound 28 potently inhibited EGFR L858R/T790M phosphorylation (IC50 = 41 nM) and cellular proliferation (IC50 = 37 nM) in the H1975 cell line, while being significantly less toxic to A431 cells. Further, compound 28 exhibited a great selectivity in a mini-panel of kinases.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of 4-Piperidinoaniline, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 2359-60-6, in my other articles.

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Piperidine – Wikipedia,
Piperidine | C5H10631N – PubChem

 

Chemistry is traditionally divided into organic and inorganic chemistry. SDS of cas: 2359-60-6. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 2359-60-6

Discovery and Rational Design of Pteridin-7(8H)-one-Based Inhibitors Targeting FMS-like Tyrosine Kinase 3 (FLT3) and Its Mutants

FLT3 has been validated as a therapeutic target for the treatment of acute myeloid leukemia (AML). In this paper, we describe for the first time, pteridin-7(8H)-one as a scaffold for potent FLT3 inhibitors derived from structural optimizations on irreversible EGFR inhibitors. The representative inhibitor (31) demonstrates single-digit nanomolar inhibition against FLT3 and subnanomolar KD for drug-resistance FLT3 mutants. In profiling of the in vitro tumor cell lines, it shows good selectivity against AML cells harboring FLT3-ITD mutations over other leukemia and solid tumor cell lines. The mechanism of action study illustrates that pteridin-7(8H)-one derivatives suppress the phosphorylation of FLT3 and its downstream pathways, thereby inducing G0/G1 cell cycle arrest and apoptosis in AML cells. In in vivo studies, 31 significantly suppresses the tumor growth in MV4-11 xenograft model. Overall, we provide a structurally distinct chemical scaffold with which to develop FLT3 mutants-selective inhibitors for AML treatment.

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.SDS of cas: 2359-60-6, you can also check out more blogs about2359-60-6

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Piperidine – Wikipedia,
Piperidine | C5H10595N – PubChem

 

Reference of 2359-60-6, 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. 2359-60-6, Name is 4-Piperidinoaniline, molecular formula is C11H16N2. In a Patent£¬once mentioned of 2359-60-6

SUBSTITUTED HETEROCYCLIC AMINE DERIVATIVES AS MULTIKINASE INHIBITORS FOR THE TREATMENT OF CANCER

The present invention relates to compounds of formula (I), their isotopic forms, stereoisomeric forms, tautomeric forms, pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs or N-oxides thereof. The present invention also relates to processes for the preparation of compounds of formula (I) and pharmaceutical compositions comprising the compounds of formula (I). The compounds and their pharmaceutical compositions are multikinase inhibitors and are useful in the treatment of proliferative disorders, such as cancers.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H10548N – PubChem