Brivanib

Bezeichnung:Brivanib

CAS-Nr649735-46-6

Englisch Name:Brivanib

CBNumberCB92484687

SummenformelC19H19FN4O3

Molgewicht370.38

MOL-Datei649735-46-6.mol

Brivanib physikalisch-chemischer Eigenschaften

Dichte	1.42
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; ≥18.5 mg/mL in DMSO; ≥3.39 mg/mL in EtOH with ultrasonic
Aggregatzustand	Yellow powder.
pka	14.18±0.20(Predicted)
Farbe	White to light brown

Gefahreninformationscode (GHS)

Brivanib Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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.
Biologische Aktivität
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
Einzelnachweise
[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.

Brivanib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

649735-46-6, Brivanib Verwandte Suche:

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