649735-63-7

Basic information

• Product Name: Unii-U2Y5ofn795
• Synonyms: L-Alanine (1R)-2-[[4-[(4-fluoro-2-Methyl-1H-indol-5-yloxy)]-5-Methyl-1H-pyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]isopropyl ester;(2R)-1-({4-[(4-fluoro-2-Methyl-1H-indol-5-yl)oxy]-5-Methylpyrrolo[2,1-f][1,2,4]triazin-6-yl}oxy)propan-2-yl (2S)-2-aMinopropanoate;Brivanib alaninate BMS-540215;(1R)-2-((4-((4-Fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)-1-methylethyl L-alanine ester Brivanib alaninate (BMS-582664);[14C]-Brivanib alaninate;(S)-(R)-1-((4-((5-Fluoro-2-methyl-1H-indol-6-yl)oxy)-5-methylpyrrolo-[2,1-f][1,2,4]triazin-6-y;Bms 582664;Bms582664
• CAS NO: 649735-63-7
• Molecular Formula: C19H18FN4O3
• Molecular Weight: 369.3696232
• Product Categories: Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Anti-cancer & immunity;Inhibitors;Aromatics;Chiral Reagents
• Mol File: 649735-63-7.mol
• Article Data: 4

Chemical Properties

• Appearance: /
• Density: 1.42 g/cm³
• Solubility: ≥22.05 mg/mL in DMSO; insoluble in H2O; ≥10.03 mg/mL in EtOH
• PKA: 16.08±0.30(Predicted)
• CAS DataBase Reference: Unii-U2Y5ofn795(CAS DataBase Reference)
• NIST Chemistry Reference: Unii-U2Y5ofn795(649735-63-7)
• EPA Substance Registry System: Unii-U2Y5ofn795(649735-63-7)

Safety Data

• Hazardous Substances Data: 649735-63-7(Hazardous Substances Data)

Usage

Description

Unii-U2Y5ofn795 is a novel prodrug that functions as a dual vascular endothelial growth factor receptor-2 (VEGFR2) and fibroblast growth factor receptor-1 (FGFR1) kinase inhibitor. It is characterized by its ability to inhibit the activity of these receptors, which play a crucial role in angiogenesis and tumor growth.
Used in Pharmaceutical Industry:
Unii-U2Y5ofn795 is used as an oral VEGFR/FGFR inhibitor for VEGFR2, Flk1, VEGFR1, and FGFR1 with respective IC50 values of 25 nM, 89 nM, 380 nM, and 148 nM. This makes it a potential candidate for the treatment of various cancers by targeting the angiogenic pathways and inhibiting tumor growth.
Additionally, Unii-U2Y5ofn795 can be used in the development of drug delivery systems to improve the bioavailability and therapeutic outcomes of the prodrug. This can be achieved by employing various organic and metallic nanoparticles as carriers for Unii-U2Y5ofn795 delivery, enhancing its efficacy against cancer cells.

Upstream product

• 649736-41-4 (S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-(benzyloxycarbonylamino)propanoate 

Relevant articles and documents

Control Strategy for the Manufacture of Brivanib Alaninate, a Novel Pyrrolotriazine VEGFR/FGFR Inhibitor

This manuscript describes the control strategy for the commercial process to manufacture brivanib alaninate. The active pharmaceutical ingredient is a prodrug which is susceptible to hydrolysis. In addition to controlling hydrolysis, a robust strategy was

Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol- 5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth

A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound. These prodrugs were evaluated for their ability t