Vemurafenib

Vemurafenib, Free Base (PLX4032) CAS: 918504-65-1
N- [3 – [[5- (4-Clorofenil) -1 H-pirolo [2,3-b] piridin-3-il] carbonil] -2,4-difluorfenil] -1-propanesulfonamidă; PLX4032; RG7204; RO51-85426; Zelboraf

Vemurafenib inhibitor selectiv al kinazei BRAFV600E; un agent antitumoral. Vemurafenibul funcționează prin inhibarea proliferării și proteinei activate mitogen / kinază extracelulară kinază reglată (ERK) kinază și fosforilare ERK într-un panou de linii celulare tumorale, inclusiv linii celulare de melanom care exprimă BRAFV600E sau alte proteine ​​BRAF mutante modificate la codonul 600.

Aspect
Solid cristalin
Puritate
≥99% (HPLC) ≥99% (TLC)
Punct de topire
269-270,5 ° C
Metoda de determinare a identității
RMN proton (CD3OD și DMSO-d6), RMN 19F (CD3OD) Analiza spectroscopică și spectrometrică de masă
Solubilitate
Solubil în DMSO la 100 mg / ml; foarte slab solubil în etanol; foarte slab solubil în apă; solubilitatea maximă în apă plată este estimată la aproximativ 25-50 uM; tampoane, ser sau alți aditivi pot crește sau scădea solubilitatea apoasă
Depozitare
A se păstra la sau sub -20 ° C.
Notă
Începând din septembrie 2011, numărul CAS actual corect pentru vemurafenib, cunoscut și sub numele de PLX4032, este dat mai sus. Chemical Abstracts Service a anulat recent un alt număr CAS, 1029872-54-5, care fusese folosit anterior pentru vemurafenib sub denumirea sa mai veche, PLX4032. Cu toate acestea, acest număr anulat rămâne foarte utilizat și primește marea majoritate a accesărilor pe Google.
Sursă
Sintetic
Puritate
≥99% (HPLC), ≥99% (TLC)
Formă
Solid cristalin
Notă importantă
Acest produs furnizat este destinat numai pentru cercetare, nu pentru utilizare în aplicații umane, terapeutice sau diagnostice fără autorizația scrisă exprimată de United States Biological.
Vemurafenib
rezumat
Vemurafenib este un inhibitor al kinazei utilizat pentru tratarea pacienților cu boala Erdheim-Chester care au mutația BRAF V600 și melanom la pacienții care au mutația BRAF V600E.
Nume de marcă
Zelboraf
Nume generic
Vemurafenib
Număr de aderare la DrugBank
DB08881
fundal
Vemurafenib este un inhibitor de kinază competitiv cu activitate împotriva kinazei BRAF cu mutații precum V600E. 2 Își exercită funcția prin legarea la domeniul de legare ATP al mutantului BRAF. 3 Vemurafenib a fost co-dezvoltat de Roche și Plexxikon și a obținut aprobarea FDA pe 17 august 2011, sub compania Hoffmann La Roche. După aprobare, Roche, în colaborare cu Genentech, a lansat un program larg de dezvoltare. 8
Tip
Moleculă mică
Grupuri
Aprobat
Greutate
Medie: 489,922
Monoizotopic: 489,072546264
Formula chimica
C 23 H 18 ClF 2 N 3 O 3 S

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