CPD3233 | AZD-3409 | AZD-3409 jẹ apaniyan prenyl transferase ti o lagbara. AZD-3409 ṣe afihan agbara ti o ga ju lonafarnib. Itumọ IC (50) fun cytotoxicity ti AZD3409 jẹ 510 ni awọn sẹẹli MEF, 10,600 ni awọn sẹẹli A549 ati 6,170 ni awọn sẹẹli MCF7, lẹsẹsẹ. Ninu awọn sẹẹli wọnyi, IC (50) fun iṣẹ FTase ti AZD3409 wa lati 3.0 si 14.2 nM ati ti lonafarnib lati 0.26 si 31.3 nM. AZD3409 ṣe idiwọ farnesylation si iye ti o ga ju geranylgeranylation lọ. Mejeeji idinamọ ti farnesylation ati geranylgeranylation ko le ni ibatan si iṣẹ ṣiṣe antiproliferative ti oogun naa. AZD3409 le ṣiṣẹ ni carcinoma ọmu-sooro gefitinib. |