Poziotinib

Izina ryimiti:

1- (4 - (((4 - (

Kode ya SMILES:

C = CC (N1CCC (OC2 = CC3 = C (NC4 = CC = C (Cl) C (Cl) = C4F) N = CN = C3C = C2OC) CC1) = O

InChi Code:

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 Urufunguzo:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Ijambo ryibanze:

Poziotinib, HM-781-36, HM-781-36B, NOV-1201, NOV-120101, 1092364-38-9

Gukemura:Gukemura muri DMSO

Ububiko:0 - 4 ° C mugihe gito (iminsi kugeza ibyumweru), cyangwa -20 ° C mugihe kirekire (amezi)

Ibisobanuro:

Poziotinib ninzitizi ikomeye ya kinase yumuryango wa EGFR ifite IC50 ifite agaciro ka 3.2, 5.3, 23.5, 4.2, na 2.2 nM kubwoko bwa EGFR, HER2, HER4, EGFRT790M, na EGFRL858R / T790M. Ifite inshuro zirenga 100- 1.000 guhitamo EGFR kinase irenga 30 ya kinase yapimwe muri vitro. Poziotinib ibuza gukura kwubwoko bwishyamba hamwe na mutant EGFR kinase iterwa nibihaha, amabere, hamwe na kanseri ya kanseri yo mu gifu (GI50s = 0,6-5.7 nM) kandi ikabuza fosifori ya EGFR kandi itera apoptose muri vitro. Muri vivo, poziotinib igabanya ubunini bwibibyimba muri HCC827 itari ntoya ya kanseri yibihaha ya kanseri yimbeba xenograft. Imiti irimo poziotinib irakurikiranwa mubigeragezo byamavuriro yo kuvura EGFR-mutant ibihaha adenocarcinoma.

Intego: EGFR