Poziotib

Aha kemịkalụ:

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

Koodu Ọchịchọ:

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

Koodu 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)

Igodo InChi:

LPFWVDIFUFFKJU-UHFFFAOYSA-N

Okwu:

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

Solubility:Soluble na DMSO

Nchekwa:0 - 4 Celsius C maka obere oge (ụbọchị ruo izu), ma ọ bụ -20 Celsius maka ogologo oge (ọnwa)

Nkọwa:

Poziotinib bụ onye na-egbochi EGFR ezinụlọ kinases nwere ụkpụrụ IC50 nke 3.2, 5.3, 23.5, 4.2, na 2.2 nM maka ụdị anụ ọhịa EGFR, HER2, HER4, EGFRT790M, na EGFRL858R/T790M. O nwere ihe karịrị 100- ruo 1,000-fold selectivity maka EGFR kinases karịrị 30 ndị ọzọ nwalere kinases in vitro. Poziotinib na-egbochi uto nke ụdị anụ ọhịa na mutant EGFR kinase na-adabere na nku ume, ara, na eriri afọ cancer cancer (GI50s = 0.6-5.7 nM) ma na-egbochi EGFR phosphorylation ma na-ebute apoptosis in vitro. Na vivo, poziotinib na-ebelata nha etuto ahụ na ụdị HCC827 na-abụghị obere cell mouse xenograft. A na-enyocha usoro ndị nwere poziotinib n'ime ule ụlọ ọgwụ maka ọgwụgwọ EGFR-mutant lung adenocarcinoma.

Ebumnuche: EGFR