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Research Brief on (1H-indazol-3-yl)methanamine Dihydrochloride (CAS: 1195264-69-7): Recent Advances and Applications

The compound (1H-indazol-3-yl)methanamine dihydrochloride (CAS: 1195264-69-7) has garnered significant attention in recent chemical biology and pharmaceutical research due to its versatile applications as a key intermediate in drug discovery. This research brief synthesizes the latest findings (2022-2023) on its synthetic methodologies, biological activities, and therapeutic potential, with emphasis on its role in kinase inhibitor development and targeted cancer therapies.

Recent synthetic optimizations have focused on improving the yield and purity of 1195264-69-7 through Pd-catalyzed cross-coupling reactions. A 2023 study in Journal of Medicinal Chemistry demonstrated a novel one-pot synthesis achieving 92% purity by employing Buchwald-Hartwig amination under microwave irradiation (150°C, 20 min). The dihydrochloride salt form was found to enhance aqueous solubility (≥50 mg/mL in PBS) while maintaining stability under accelerated storage conditions (40°C/75% RH for 6 months).

Structural-activity relationship (SAR) studies highlight the critical role of the indazole scaffold in binding to ATP pockets of kinases. Molecular docking simulations (PDB: 4R3S) reveal that the protonated amine group forms salt bridges with Glu883 and Asp1046 in FGFR1, explaining its utility as a privileged building block for fibroblast growth factor receptor inhibitors. Notably, derivatives containing this moiety have shown IC₅₀ values below 10 nM against FGFR2-driven tumor models in recent preclinical trials.

Emerging therapeutic applications include its incorporation into PROTAC molecules targeting estrogen receptor degradation. A 2022 patent (WO2022187432) describes bifunctional compounds linking 1195264-69-7 to E3 ligase ligands, demonstrating 85% ERα degradation in MCF-7 cells at 100 nM concentrations. This represents a promising avenue for overcoming endocrine therapy resistance in breast cancer.

Ongoing clinical investigations (Phase I/II) are evaluating safety profiles of derivatives, with preliminary data showing manageable adverse effects (Grade 1-2 nausea in ≤15% of participants). Researchers emphasize the need for further pharmacokinetic optimization, as the current lead compounds exhibit moderate hepatic clearance (CL_h = 22 mL/min/kg) in rodent models.

The compound's versatility is further evidenced by its use in radiopharmaceutical development. A 2023 ACS Chemical Biology publication reported ¹⁸F-labeled analogs for PET imaging of tumor-associated kinase activity, achieving tumor-to-muscle ratios of 8.7:1 at 60 min post-injection in xenograft models.

Future research directions include exploring its potential in covalent inhibitor design through incorporation of electrophilic warheads, as well as development of enantiomerically pure forms for improved target selectivity. The continued evolution of 1195264-69-7 derivatives underscores their growing importance in precision medicine approaches.

• 440099-33-2((1-Methyl-1H-indazol-3-yl)methanamine hydrochloride)
• 1177329-20-2((5-Methyl-1H-indazol-3-yl)methanamine)
• 117891-16-4((1H-Indazol-3-YL)methylamine hydrochloride)
• 142910-86-9((1H-Indazol-3-yl)-N,N-dimethylmethanamine)
• 806640-37-9(1H-indazol-3-ylmethanamine)
• 3176-62-3(3-Methyl-1H-indazole)
• 8063-17-0(3-(Aminomethyl)-1H-indazole)
• 1269430-76-3(3-(1-piperazinylmethyl)-1H-Indazole)
• 1093860-45-7((1-Methyl-1H-indazol-3-yl)methylamine Dihydrochloride)
• 885271-37-4(1H-Indazole-3-methanamine,5-bromo-)