Poziotib

Magaca Kiimikada:

1- (4-(4- (3,4-dichloro-2-fluorophenyl)amino) -7-methoxyquinazolin-6-yl) oxy) piperidin-1-yl) prop-2-en-1-one

Koodhka dhoola cadeynta:

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

Koodhka 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)

Furaha InChi:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo)

Sharaxaad:

Poziotinib waa horjooge awood leh ee kinase qoyska EGFR oo leh IC50 qiyamka 3.2, 5.3, 23.5, 4.2, iyo 2.2 nM ee nooca duurjoogta ah EGFR, HER2, HER4, EGFRT790M, iyo EGFRL858R/T790M, Waxay leedahay wax ka badan 100-1,000-laab xulashada EGFR kinase in ka badan 30 kinases kale oo la tijaabiyay in vitro. Poziotinib waxay xakameysaa koritaanka nooca duurjoogta ah iyo mutant EGFR kinase-ku-tiirsan sambabada, naaska, iyo khadadka unugyada kansarka caloosha (GI50s = 0.6-5.7 nM) oo waxay joojisaa fosforyaalka EGFR waxayna keentaa apoptosis in vitro. In vivo, poziotinib waxay yaraynaysaa cabbirka burada HCC827 moodeelka xenograft ee kansarka sanbabada unug yar. Qaababka ay ku jiraan poziotinib ayaa lagu baarayaa tijaabooyinka kiliinikada ee daaweynta EGFR-mutant adenocarcinoma sambabada.

Hadafka: EGFR