prenyl transferase

CAT #	Inoa Huahana	wehewehe
CPD3233	AZD-3409	ʻO AZD-3409 kahi mea paʻa prenyl transferase. Ua hōʻike ʻo AZD-3409 i ka mana kiʻekiʻe ma mua o lonafarnib. ʻO ka mean IC (50) no ka cytotoxicity o AZD3409 he 510 i loko o nā pūnaewele MEF, 10,600 i nā pūnaewele A549 a me 6,170 i nā pūnaewele MCF7, kēlā me kēia. I loko o kēia mau pūnaewele, ʻo ka IC (50) no ka hana FTase o AZD3409 mai 3.0 a 14.2 nM a me lonafarnib mai 0.26 a 31.3 nM. Kāohi ʻo AZD3409 i ka farnesylation i kahi kiʻekiʻe ma mua o ka geranylgeranylation. ʻAʻole hiki ke hoʻopili ʻia ka pale ʻana o ka farnesylation a me ka geranylgeranylation i ka hana antiproliferative o ka lāʻau. Hiki paha iā AZD3409 ke ʻeleu i ka maʻi maʻi maʻi umauma gefitinib.