Poziotinib
Lintlha tsa Sehlahisoa
Li-tag tsa Sehlahisoa
| Boholo ba Pakete | Ho fumaneha | Theko (USD) |
| 1g | E teng thepeng e teng ka lebenkeleng | 790 |
| Boholo bo Eketsehileng | Fumana Litlhaloso | Fumana Litlhaloso |
Lebitso la lik'hemik'hale:
1-(4-((4-(3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one
SMILES Khouto:
C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O
Khoutu ea InChi:
InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27- 12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27 ,28,29)
InChi Key:
LPFWVDIFUFFKJU-UHFFFAOYSA-N
Keyword:
Poziotinib, HM-781-36, HM-781-36B, NOV-1201,NOV-120101, 1092364-38-9
Sollubility:E qhibiliha ka DMSO
Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli)
Tlhaloso:
Poziotinib ke inhibitor e matla ea EGFR family kinases e nang le litekanyetso tsa IC50 tsa 3.2, 5.3, 23.5, 4.2, le 2.2 nM bakeng sa mofuta o hlaha oa EGFR, HER2, HER4, EGFRT790M, le EGFRL858R/T790M, ka ho latellana. E na le khetho e kholo ho feta 100- ho 1,000-fold bakeng sa EGFR kinases ho feta 30 e meng e lekiloeng ea kinase in vitro. Poziotinib e thibela ho hōla ha mefuta e hlaha le e feto-fetohang ea EGFR kinase-e itšetlehileng ka matšoafo, sefuba le lisele tsa kankere ea mala (GI50s = 0.6-5.7 nM) 'me e thibela phosphorylation ea EGFR le ho etsa hore apoptosis in vitro. Ka vivo, poziotinib e fokotsa boholo ba hlahala mofuteng oa HCC827 o seng o monyane oa mofetše oa matšoafo oa mouse xenograft. Mefuta e nang le poziotinib e ntse e etsoa lipatlisiso litekong tsa meriana bakeng sa phekolo ea EGFR-mutant lung adenocarcinoma.
Sepheo: EGFR
