|
|
| | 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol Basic information |
| Product Name: | 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol | | Synonyms: | 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol;(R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yloxy)propan-2-ol;2-Propanol, 1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yl)oxy)-, (2R)-;Bms 540215;Bms540215;Unii-ddu33B674i;1-[4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-propan-2(R)-ol;(R)-1-(4-(4-Fluoro-2-Methyl-1H-indol-5-yloxy)-5-Methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol | | CAS: | 649735-46-6 | | MF: | C19H19FN4O3 | | MW: | 370.38 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 649735-46-6.mol | ![1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol Structure](CAS/GIF/649735-46-6.gif) |
| | 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol Chemical Properties |
| density | 1.42 | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥18.5 mg/mL in DMSO; ≥3.39 mg/mL in EtOH with ultrasonic | | form | Yellow powder. | | pka | 14.18±0.20(Predicted) |
| | 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol Usage And Synthesis |
| Uses | Brivanib is an ATP-competitive inhibitor against human VEGFR2 and FGFR with IC50 of 25 nM and 148 nM, respectively. | | Definition | ChEBI: Brivanib is a secondary alcohol resulting from the hydrolysis of the carboxylic ester group of brivanib alaninate. It is a dual VEGFR-2/FGFR-1 kinase inhibitor whose alanine prodrug, brivanib alaninate is currently under development as an oral agent for the treatment of cancer. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an angiogenesis inhibitor, an apoptosis inducer, a fibroblast growth factor receptor antagonist and a drug metabolite. It is a pyrrolotriazine, a fluoroindole, a diether, an aromatic ether and a secondary alcohol. | | Biological Activity | brivanib is an atp competitive inhibitor of human vegfr-2 with ic50 value of 25nm [1].brivanib is a selective rtk inhibitor that targets signaling via vegfr2 and 3, and fgfr1, 2 and 3. targeting both vegf and fgf signaling pathways inhibits tumor growth in rt2 mice, with vegf signaling predominating in initiation of tumor angiogenesis, currently, brivanib therapy is being evaluated in phase iii | | target | VEGFR-2 | | references | [1] rajeev s. bhide, zhen-wei cai, yong-zheng zhang, ligang qian, donna wei, stephanie barbosa, louis j. lombardo, robert m. borzilleri, xiaoping zheng, laurence i. wu, joel c. barrish, soong-hoon kim, kenneth leavitt, arvind mathur, leslie leith, sam chao, barri wautlet, steven mortillo, robert jeyaseelan sr., daniel kukral, john t. hunt, amrita kamath, aberra fura, viral vyas, punit marathe, celia d’arienzo, george derbin, and joseph fargnoli. discovery and preclinical studies of (r)-1-(4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol (bms-540215), an in vivo active potent vegfr-2 inhibitor. journal of medicinal chemistry. 2006, 49 (7): 2143-2146.
[2] elizabeth allen, ian b. walters, and douglas hanahan. brivanib, a dual fgf/vegf inhibitor, is active both first and second line against mouse pancreatic neuroendocrine tumors developing adaptive/evasive resistance to vegf inhibition. clinical cancer research. 2011 (17): 5299-5310. |
| | 1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol Preparation Products And Raw materials |
|