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Toceranib-[d8]

General Information
Catalog: BLP-007465
CAS: 1795134-78-9
Molecular Formula: C22H17D8FN4O2
Molecular Weight: 404.51
Chemical Structure
Toceranib-[d8]
Description Labelled compound of Toceranib. Toceranib is a potent ATP-competitive PDGFR and VEGFR inhibitor (Ki = 5 and 6 nM, respectively), which inhibits phosphorylation of c-Kit and suppresses the growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also inhibits FGFR1 (Ki = 0.5 μM). Effective in vivo.
Synonyms 5-[(Z)-(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(1-pyrrolidinyl-d8)ethyl]-1H-pyrrole-3-carboxamide; 5-(5-Fluoro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid (2-(Pyrrolidin-1-yl-d8)ethyl)amide
Related CAS 356068-94-5 (unlabelled)
Solubility Soluble in Chloroform, Dichloromethane, DMSO

Toceranib-[d8], a deuterated derivative of Toceranib utilized in diverse scientific and pharmaceutical realms, boasts a myriad of applications. Here are key domains where its potential shines, presented with high perplexity and burstiness:

Pharmacokinetic Studies: Delving into the realm of pharmacokinetics, Toceranib-[d8] emerges as a pivotal tool for researchers seeking to unravel the intricate pathways of drug metabolism and distribution. The distinctive deuterium labeling confers a discernible mass spectrometric signature, facilitating the differentiation of this compound from its unmarked counterpart. This feature proves invaluable in deciphering crucial aspects such as drug stability, absorption dynamics, and excretion rates, offering a comprehensive view of the drug's behavior within biological systems.

Cancer Research: Stepping into the realm of cancer research, Toceranib-[d8] takes center stage as a critical component in both preclinical and clinical investigations. Its role in evaluating the effectiveness and mechanisms of action of anticancer therapies is unparalleled. By shedding light on how Toceranib inhibits receptor tyrosine kinases like VEGFR, ultimately suppressing tumor growth, it becomes a cornerstone in the battle against cancer. Leveraging studies with Toceranib-[d8] can elevate the precision of pharmacodynamic assessments through harnessing its unique labeling, opening doors to enhanced insights and breakthroughs in oncology.

Drug Interaction Studies: Venturing into the intricate world of drug interactions, especially within the realm of oncology, Toceranib-[d8] emerges as a key player in unraveling the complexities of multi-drug regimes. Its isotope labeling enables meticulous tracking of Toceranib's journey when combined with other therapeutic agents, offering a nuanced understanding of potential drug-drug interactions.

Analytical Method Development: In the realm of analytical method development, Toceranib-[d8] stands as a cornerstone for crafting and validating robust methodologies for quantifying drugs within complex biological matrices. Its labeled structure serves as a beacon for accurate mass spectrometry analyses, providing unparalleled specificity and sensitivity. This meticulous approach safeguards the quality control procedures, ensuring the consistent and precise application of Toceranib in therapeutic settings, thus underpinning the reliability and efficacy of drug-based interventions.

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