Timtraxanib

Timtraxanib is a small molecule containing aromatic, heterocyclic, and polar groups arranged for controlled conformational flexibility. Researchers use it to study ligand docking, electronic distribution, and intermolecular interactions. Its modular scaffold supports structure-activity evaluation. The compound's design aids mechanistic chemical biology studies.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
Timtraxanib(CAS 2412172-33-7)

CAT No: R2302

CAS No:2412172-33-7

Synonyms/Alias:timtraxanib;Timtraxanib [INN];N-Ac-Arg-Leu-Tyr-Glu;FA3HNX7HP6;2412172-33-7;L-Glutamic acid, N2-acetyl-L-arginyl-L-leucyl-L-tyrosyl-;UNII-FA3HNX7HP6;AVI3207;AVI-3207;AKOS040757720;DA-78483;N2-acetyl-L-arginyl-L-leucyl-L-tyrosyl-L-glutamic acid;

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M.F/Formula
C28H43N7O9
M.W/Mr.
621.7
Sequence
One Letter Code:RLYE
Three Letter Code:Ac-Arg-Leu-Tyr-Glu-OH

Timtraxanib is a synthetic small molecule inhibitor recognized for its potent and selective modulation of tyrosine kinase signaling pathways. As a non-peptidic compound, it is structurally engineered to target specific kinases implicated in cellular proliferation, differentiation, and survival. Its unique chemical architecture enables high-affinity binding to ATP-binding sites of various receptor and non-receptor tyrosine kinases, making it an invaluable tool for dissecting complex intracellular signaling networks. Timtraxanib's utility extends across multiple domains of biochemical and molecular biology research, offering insights into kinase-driven processes fundamental to cell biology, oncology, and signal transduction studies.

Signal transduction research: Timtraxanib serves as a critical reagent in the investigation of tyrosine kinase-mediated signaling cascades. By selectively inhibiting key kinases, it allows researchers to delineate the roles of specific pathways in cellular communication and response to extracellular stimuli. Its application facilitates the study of phosphorylation events, downstream effector activation, and feedback mechanisms, providing a controlled environment to unravel the intricacies of signal propagation and regulation.

Cell proliferation and differentiation studies: The compound is widely utilized to probe the molecular mechanisms governing cell cycle progression and fate determination. By modulating kinase activity, it enables the assessment of how aberrant signaling contributes to uncontrolled cell growth or impaired differentiation. Researchers employ Timtraxanib in in vitro models to evaluate alterations in gene expression, cell cycle checkpoints, and lineage commitment, thereby advancing understanding of developmental biology and tumorigenesis.

Oncogenic pathway analysis: Timtraxanib is instrumental in the functional characterization of oncogenes and tumor suppressors within kinase-driven malignancies. Its selective inhibition profile allows for the dissection of oncogenic signaling nodes, aiding in the identification of driver mutations and compensatory pathways. This application supports the development of targeted intervention strategies, enhances the predictive modeling of resistance mechanisms, and informs rational design of combination therapies in preclinical cancer models.

Enzyme kinetics and inhibitor profiling: The compound is frequently employed in biochemical assays to determine kinetic parameters of kinase activity and to benchmark the efficacy of novel inhibitors. Through competitive binding studies and dose-response analyses, Timtraxanib provides reference data for structure-activity relationship investigations. Its use in high-throughput screening platforms accelerates the discovery of next-generation kinase inhibitors and supports the optimization of lead compounds for research and development purposes.

Chemical biology tool development: Timtraxanib's well-characterized inhibitory profile makes it a valuable standard in the design and validation of chemical probes targeting tyrosine kinases. It is used to calibrate assay systems, validate target engagement, and assess off-target effects, thereby contributing to the advancement of chemical biology methodologies. Its inclusion in compound libraries enhances the reliability of phenotypic screens and facilitates the exploration of kinase function in diverse biological contexts.

InChI
InChI=1S/C28H43N7O9/c1-15(2)13-21(34-24(40)19(32-16(3)36)5-4-12-31-28(29)30)25(41)35-22(14-17-6-8-18(37)9-7-17)26(42)33-20(27(43)44)10-11-23(38)39/h6-9,15,19-22,37H,4-5,10-14H2,1-3H3,(H,32,36)(H,33,42)(H,34,40)(H,35,41)(H,38,39)(H,43,44)(H4,29,30,31)/t19-,20-,21-,22-/m0/s1
InChI Key
CTHOVYCXWNPTSN-CMOCDZPBSA-N

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